IDEAYA Biosciences, Inc. (IDYA) Business

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Item 1. Business.

Company Overview

We are a precision medicine oncology company committed to the discovery, development, and commercialization of transformative therapies for cancer. Our approach integrates expertise in small-molecule drug discovery, structural biology and bioinformatics with robust internal capabilities in identifying and validating translational biomarkers to develop tailored, potentially first-in-class targeted therapies aligned to the genetic drivers of disease. We have built a deep pipeline of product candidates focused on synthetic lethality and antibody-drug conjugates (ADCs) for molecularly defined solid tumor indications. Our clinical development strategy is to evaluate our product candidates in rational combinations, where appropriate, and earlier in the course of disease in the adjuvant and neoadjuvant settings, which we believe has the potential to maximize their impact. Our mission is to bring forth the next wave of precision oncology therapies that are more selective, more effective and deeply personalized with the goal of altering the course of disease and improving clinical outcomes for patients with cancer.

Pipeline – Overview and Program Goals

Our current clinical pipeline consists of nine potential first-in-class product candidates across four clinical focus areas: (1) Darovasertib for Uveal Melanoma; (2) ADC and DNA Damage Response (DDR) Combinations; (3) MTAP Pathway; and (4) Next Generation Therapies. We have selectively established collaborations with leading pharmaceutical companies to support our clinical development activities. Details of our pipeline are summarized in the chart below.

(1) Pursuant to Pfizer License Agreements

(2) Pursuant to Servier License Agreement

(3) Pursuant to Hengrui Pharma License Agreement

(4) Pursuant to Gilead Clinical Study Collaboration and Supply Agreement

Darovasertib for Uveal Melanoma

Darovasertib is an oral, potent and selective small molecule inhibitor of protein kinase C (PKC) and our most advanced clinical program. We are developing darovasertib for uveal melanoma (UM), a rare, aggressive form of ocular cancer in which approximately 95% of patients harbor activating mutations in GNAQ/11 GTPase proteins that drive downstream PKC signaling and tumor cell growth. We are conducting multiple clinical trials in the metastatic and pre-metastatic settings of UM, as described below.

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Metastatic UM (mUM). We are evaluating darovasertib in combination with crizotinib, Pfizer’s oral c-MET inhibitor, in a potentially registration-enabling, Phase 2/3 trial (OptimUM-02) for human leukocyte antigen-A*02:01 negative (HLA*A2(-)), patients with first line (1L) mUM. We expect to report topline data, including progression free survival (PFS) data, from this trial in the first quarter of 2026. Based on our discussions with the U.S. Food and Drug Administration (FDA), the PFS data from OptimUM-02 may enable an accelerated approval filing in the United States. Accelerated approval is intended to allow for earlier approval of drugs that treat serious conditions and fill an unmet medical need based on a demonstration of effectiveness on a surrogate endpoint, with the requirement to conduct one or more additional studies to confirm the anticipated clinical benefit to obtain full traditional approval. In December 2025, we completed full enrollment of 437 patients in OptimUM-02, and plan to submit overall survival (OS) data from these patients, when available, to support a full approval filing in this indication.

In October 2025, we reported positive data at the Society for Melanoma Research Congress (SMR) from our single-arm Phase 2 trial (OptimUM-01) of darovasertib in combination with crizotinib in 1L mUM patients, which included the first median OS data presented with the combination. Data were from a total of 44 1L mUM patients, including both HLA*A2(-) and HLA*A2:01 positive (HLA*A2(+)). Highlights of the data presented are shown below.

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In 41 efficacy-evaluable patients, confirmed objective response rate (ORR) of 34% (14/41) with a 9.0 month median duration of response (mDOR).

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Disease control rate (DCR) of 90% (37/41), with 85% (35/41) achieving ‘any reduction’ in target lesions.

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7.0 month median PFS and 21.1 month median OS across all patients.

(1) Khoja L, et al. J Clin Oncol. 2025;43 (suppl), Abstract 9539

(2) Rantala ES, et al. Melanoma Res. 2019; 29:561-568

Based on our data from the Phase 2 OptimUM-01 trial and our understanding of its mechanism of action, we believe darovasertib will have clinical activity in mUM independent of a patient’s HLA*A2 serotype. We are continuing to evaluate the combination of darovasertib and crizotinib in HLA*A2(+) patients in the OptimUM-01 trial and expect to complete enrollment of approximately 100 HLA*A2(+) patients by the second quarter of 2026. The data from OptimUM-01 may be used to support a potential future submission to the FDA to expand the labeled use for darovasertib and/or a national comprehensive cancer network (NCCN) compendia listing to enable use of the combination in these patients.

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Neoadjuvant UM. To explore its potential use beyond metastatic UM, we are also evaluating darovasertib as a monotherapy in the neoadjuvant setting of primary UM, where the goal of treatment is to prevent enucleation (surgical eye removal), preserve vision prior to and post-plaque brachytherapy and potentially delay or prevent progression to metastatic disease. In 2025, we initiated a randomized Phase 3 trial of darovasertib in the neoadjuvant setting (OptimUM-10), which will enroll approximately 450 patients across two cohorts of plaque brachytherapy-eligible (PB) and enucleation-eligible (EN) patients. We plan to complete enrollment in this trial by the first half of 2027.

In October 2025, we presented positive data at the European Society for Medical Oncology (ESMO) from our randomized, Phase 2 trial (OptimUM-09) of darovasertib in neoadjuvant UM. Data were from 95 patients, including 56 recommended for EN and 39 eligible for PB. Highlights of the data that were presented include:

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Ocular tumor shrinkage observed in ~83% (78/94) of patients assessed, the majority of whom achieved ≥20% tumor shrinkage.

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Among evaluable EN patients, the eye preservation rate was 57% (24/42), which increased to 95% (19/20) in patients achieving ≥20% tumor shrinkage.

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Among PB eligible patients, ~70% (26/37) achieved a reduction in predicted radiation dose to the eye from baseline, resulting in ~65% (24/37) having lower predicted risk of vision loss 3-years post-PB treatment.

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During neoadjuvant treatment with darovasertib, ~55% (29/53) of EN and ~61% (23/38) of PB patients showed an improvement in baseline visual acuity scores (VAS), with a mean gain of 17 and 10 letters, respectively.

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Adjuvant UM. We plan to initiate a global Phase 3 combination trial (OptimUM-11) of darovasertib and crizotinib in the adjuvant setting of primary UM in the first half of 2026. The trial is expected to enroll approximately 450 patients with high to medium-high risk of metastasis, randomized 1:1 to the combination of darovasertib and crizotinib or placebo. The primary endpoint of this trial is relapse-free survival (RFS).

Servier License Agreement

Uveal Melanoma patient population

We estimate the annual incidence of primary UM is 10,000 patients globally (including North America, Europe and Australia) and 3,000 patients in the United States. In metastatic UM, we estimate the annual incidence of newly diagnosed patients is between 4,000-5,000 globally and approximately 1,500 in the United States, which is based on data suggesting that approximately 50% of patients diagnosed in the primary setting ultimately progress to metastatic disease. Based on published data, we believe the majority of mUM patients are of the HLA*A2(-) serotype, representing between 60-65% of all mUM patients. In addition, several publications suggest there is clinical evidence of the loss of heterozygosity (LOH) of the HLA-alleles that could create discordance between a blood based versus tumor-based evaluation resulting in a potential over-reporting of HLA*A2(+) prevalence due to the loss of an allele with cancer progression. Currently, there are no FDA-approved systemic therapies for primary UM and no FDA-approved therapies for patients with HLA*A2(-) mUM.

Breakthrough Therapy Designation, Orphan Drug Designation and Fast Track Designation

In March 2025, the FDA granted Breakthrough Therapy designation (BTD) for darovasertib as a neoadjuvant treatment of adult patients with primary UM for whom enucleation has been recommended. BTD is designed to expedite the development and regulatory review of promising therapies for serious or life-threatening conditions where preliminary clinical evidence suggests substantial improvement over existing treatments. The designation facilitates more intensive FDA guidance, cross-disciplinary collaboration, and eligibility for potential rolling review and priority review of a future new drug application (NDA).

In November 2022, the FDA granted Fast Track designation to our development program investigating darovasertib in combination with crizotinib in adult patients being treated for mUM. The Fast Track designation makes our darovasertib and crizotinib development program eligible for various expedited regulatory review processes, including generally more frequent FDA interactions, such as meetings and written communications, potential eligibility for rolling review and priority review of an NDA.

In April 2022, the FDA designated darovasertib as an Orphan Drug in UM, including primary and metastatic disease. Under an Orphan Drug designation, darovasertib may be entitled to certain tax credits for qualifying clinical trial expenses, exemption from certain user fees and, subject to FDA approval of a NDA, for darovasertib in UM, eligibility for seven years of statutory marketing exclusivity during which the FDA is prohibited from approving a subsequent same drug for the same rare disease or condition except in limited circumstances, such as a subsequent drug that demonstrates clinical superiority. If approved for one or more designated indications, darovasertib may also be excluded from certain mandatory price negotiation provisions of the 2022 Inflation Reduction Act.

ADC / DDR Combinations

Our second area of clinical focus is to explore combinations of topoisomerase I inhibitor–based ADCs (TOP1 ADCs) and selective inhibitors of the DDR pathway. TOP1 ADCs have demonstrated meaningful clinical activity as monotherapies, however their broader application across solid tumors has been limited by challenges in achieving sufficient and durable tumor-selective payload delivery, particularly in the context of low or heterogeneous tumor-selective antigen expression. The DDR enzyme poly (ADP-ribose) glycohydrolase (PARG) plays a uniquely essential role in the repair of TOP1–mediated DNA damage, which leads to cell death when left unresolved. We believe pharmacologic inhibition of PARG has the potential to selectively amplify TOP1-induced DNA damage and enhance the antitumor activity of these agents. Our clinical pipeline within this focus area is summarized below.

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IDE849 / SHR-4849 is a potential first-in-class, DLL3 TOP1 ADC. DLL3 is expressed at high frequency in multiple solid tumor types, including approximately 85% of small-cell lung cancer (SCLC) and 64% of neuroendocrine carcinomas (NEC). Notably, DLL3 has limited extracellular expression in normal tissues, making it a promising therapeutic target in these tumor types for which there remains significant unmet medical need.

IDE849 is currently being evaluated by our partner, Hengrui Pharma, in a multi-site, open label Phase 1 clinical trial in China in patients with SCLC and NEC. In September 2025, Hengrui Pharma presented positive initial Phase 1 data at the International Association for the Study of Lung Cancer’s (IASLC) 2025 World Conference on Lung Cancer (WCLC) in Barcelona, Spain. Data were from a total of 100 patients, including 87 refractory (2L+) SCLC patients, who received IDE849 at doses between 0.8 mg/kg to 4.2 mg/kg with a once every 3-week dosing interval. Highlights of the data presented as of the cutoff date of June 20, 2025 are shown below.

Efficacy (n=71 evaluable SCLC patients treated with IDE849)

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Robust ORR and DCR were consistently observed across all expansion doses evaluated and in patients across all lines of therapy, with a modest reduction in ORR/DCR observed in later-line patients consistent with their more advanced stage of disease.

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14.1% (10/71) of patients across all doses 2.4 mg/kg are still pending confirmation, as well as multiple patients who have had limited follow-up (e.g. one post-baseline scan) highlighting the study has not yet achieved a fully mature confirmed ORR%.

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In patients with baseline brain metastasis, a confirmed ORR of 83.3% (5/6) and a DCR of 100% (6/6) was observed at the 2.4 mg/kg dose. Across all doses ≥2.4 mg/kg (n=18) with baseline brain metastasis, the confirmed ORR was 66.7% (12/18) with a DCR of 100% (18/18). A confirmation scan for one unconfirmed partial response is pending, which if confirmed, would increase the confirmed ORR to 72.2% (13/18).

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Median PFS was 6.7 months across all lines of treatment at doses of IDE849 ≥2.4 mg/kg (n=86); median PFS was not yet reached (NR) in 2L patients (n=42).

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As of the cut-off date of June 20, 2025, the median length of follow-up was 3.5 months.

Safety (n=100 SCLC and NEC patients treated with IDE849)

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Across all patients and all dose levels (n=100), Grade 3 or higher (Gr3+) treatment-related adverse events (TRAEs) occurred in 48% (48/100) and serious TRAEs in 16% (16/100) of patients. The most common TRAEs were white blood cell reduction (27% Gr3+), neutropenia (33% Gr3+), anemia (6% Gr3+) and nausea (0% Gr3+).

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TRAEs leading to dose reduction in 15% (15/100) of patients; treatment-related discontinuation rate of 2% (2/100) with no treatment-related deaths reported.

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Manageable safety profile observed across multiple expansion cohorts, including the 2.4 mg/kg, 3.0 mg/kg, and 3.5 mg/kg dose levels with a once every 3-week dosing interval.

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As of the cutoff date of June 20, 2025 referenced for the data in the presentation, at the 2.4 mg/kg dose, the Gr3+ TRAE rate was below 20%. A 7% (7/100) rate of interstitial lung disease was reported across all patients in the study, of which 1% was Grade 3. There were no Grade 4 or Grade 5 cases reported.

In April 2025 we received U.S. investigational new drug (IND) clearance from the FDA to begin a global

Phase 1 trial in patients with SCLC, NEC and other DLL3-overexpressing tumors. We plan to provide initial data from this trial and initiate a monotherapy registrational trial in the second line/refractory setting (2L+) of SCLC and/or NEC by the end of 2026. We are also targeting to initiate a Phase 1 clinical combination trial with IDE849 and IDE161, our proprietary PARG inhibitor, in the second quarter of 2026.

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IDE034 is a potential first-in-class, B7H3/PTK7 bispecific TOP1 ADC. B7H3/PTK7 has been found to be co-expressed in many solid tumor types, including in approximately 30-40% of lung, colorectal, breast and ovarian cancers, among others. We received IND clearance from the FDA in the fourth quarter of 2025 and expect to achieve first-patient-in in our Phase 1 dose-escalation trial in the first quarter of 2026. Dosing of the first patient with IDE034 will trigger a $5.0 million milestone payment to Biocytogen, pursuant to our Option and License Agreement. Based on our preclinical data, we believe IDE034 has the potential to be developed both as a monotherapy and in combination with programs in our pipeline targeting the DDR pathway, including our PARG inhibitor, IDE161.

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IDE161 is a potential first-in-class, oral small molecule poly (ADP-ribose) glycohydrolase (PARG) inhibitor. PARG is a novel target in a clinically validated biological pathway that functions as a regulator of DNA repair in the same biochemical pathway as PARP, however PARG is mechanistically distinct from PARP. We believe IDE161 has the potential to amplify TOP1-mediated DNA damage delivered in the context of an ADC to improve the efficacy and durability of these antitumor agents. As shown in the figure below, we have observed robust and durable tumor shrinkage in preclinical models with IDE161 in combination with IDE849 and IDE034 relative to either agent as a monotherapy, suggesting the combination may enhance the efficacy and durability of TOP1 ADCs.

Pending ongoing dose-finding work, we are targeting to initiate a Phase 1 clinical combination trial with IDE161 and IDE849 (DLL3) in SCLC, NEC and potentially other DLL3-overexpressing solid tumors in the second quarter of 2026. We may also evaluate clinical combinations of IDE161 with IDE034 (B7H3/PTK7) and potentially other TOP1 ADCs in collaboration with third parties.

We received Fast Track designations from the FDA in September 2023 for IDE161, specifically for the treatment of (i) adult, pretreated, platinum-resistant advanced or metastatic ovarian cancer patients having tumors with BRCA1/2 mutations and (ii) adult, pretreated, advanced or metastatic hormone receptor positive (HR+), human epidermal growth factor receptor 2 (Her2-) and BRCA1/2 mutant breast cancer patients. We own or control all commercial rights to IDE161, subject to certain economic obligations pursuant to our exclusive, worldwide license to certain PARG inhibitors, including IDE161, with CRT and University of Manchester.

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IDE705 is a potential first-in-class, oral small molecule inhibitor of the helicase domain of Pol Theta, an enzyme that is involved in a DNA repair process called microhomology mediated end joining that is utilized when homologous recombination mediated repair is compromised, as happens in the case of certain BRCA1 or BRCA2 mutations. Pol Theta is largely absent in normal cells but tends to be overexpressed in tumor cells harboring double strand break repair defects, such as those with BRCA1 or BRCA2 mutations, which results in a synthetic lethal vulnerability to Pol Theta inhibition.

We had been evaluating IDE705 in combination with niraparib, a selective inhibitor of PARP, in collaboration with GlaxoSmithKline (GSK) pursuant to the terms of our 2020 Collaboration, Option and License Agreement. In December 2025, GSK notified us of its intention to terminate the Agreement, which will be effective 90 days following the date of GSK’s notice, or March 9, 2026. During the ninety-day transition period, GSK will transfer the Pol Theta (IDE705) clinical program to us in accordance with the applicable provisions of the Agreement.

Once effective, we do not intend to continue clinical development of IDE705 in combination with niraparib or other PARP inhibitors and instead plan to begin preclinical studies evaluating the potential of IDE705 to enhance the efficacy of TOP1 ADCs in solid tumors, as we are doing with IDE161, within our focus area of ADC/DDR combinations.

MTAP Pathway

Our third area of clinical focus is on solid tumors with methylthioadenosine phosphorylase (MTAP) gene deletions. MTAP-deleted cells lack the ability to metabolize 5-methylthioadenosine (MTA) which is an essential step in a biochemical pathway involved in salvaging the metabolite S-adenosyl methionine (SAM). Increased levels of MTA partially inhibit the methyltransferase PRMT5, for which SAM is the methyl-donor substrate for methylation of essential proteins. The partial inhibition of PRMT5 by increased levels of MTA renders MTAP-deleted cells more dependent on the activity of MAT2A, an enzyme that is responsible for the synthesis of SAM. Therefore, increased dependence on MAT2A results in a synthetic lethal vulnerability when MAT2A is pharmacologically inhibited in MTAP-deleted tumors.

Our clinical strategy is based on evaluating rational combinations designed to inhibit key nodes in the MTAP pathway to drive deep and durable antitumor responses in MTAP-deleted tumors. The backbone of these combinations is IDE397, a potent and selective inhibitor of MAT2A. Our clinical pipeline within this focus area is described below.

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IDE397 is a potential first-in-class, oral, small molecule inhibitor of MAT2A. We are conducting a Phase 1/2 clinical trial pursuant to a Clinical Study Collaboration and Supply Agreement (CSCSA) with Gilead to evaluate IDE397 in combination with Trodelvy® (sacituzumab govitecan-hziy), Gilead’s Trop-2 directed ADC, in patients with MTAP-deletion urothelial cancer (UC) and non-small cell lung cancer (NSCLC). Both we and Gilead retain full commercial rights to our respective programs.

In September 2025, we presented initial Phase 1/2 data from the combination in MTAP-deleted UC patients. The data was from a total of 19 patients with late-line MTAP-deleted UC who received the combination of IDE397 and Trodelvy at one of two dose levels (DL1; IDE397: 15 mg/kg; Trodelvy: 10 mg/kg; or DL2; IDE397: 30mg/kg; Trodelvy: 7.5 mg/kg). Of the 19 patients, 16 were evaluable for efficacy having received at least one post-baseline tumor assessment per RECIST v1.1. Highlights of the data presented are in the figure below.

Data as of Aug 29, 2025 (based on preliminary analysis of unlocked database). One patient not included as MTAP status was determined to be WT by central IHC testing. 1 PR confirmed 27 days instead of 28 days or later after initial scan showing response.

# Patient confirmed response after the data cut-off; * Patient missed ~50% of dosing prior to 1st scan, + Patient still on treatment as of cutoff date; ^ Patient developed new lesions.

As of the cutoff date, median PFS and DOR had not been reached. The safety profile of the combination was manageable and consistent with known adverse events of both drugs as single agents, with no treatment related serious adverse events observed at the IDE397 30mg and Trodelvy 7.5 mg/kg expansion dose. The most common Gr3+ TRAEs observed in DL1 were anemia and neutropenia, and in DL2 were anemia, asthenia, and diarrhea. We have selected DL2 as the go-forward dose in UC and are targeting to share additional data from this combination trial in MTAP-deleted UC at a medical conference in 2026. We are also continuing to enroll MTAP-deleted NSCLC patients in the trial, however data from these patients is still immature.

In addition to the combination with Trodelvy described above, IDE397 is the backbone of two additional clinical combination strategies intended to amplify metabolic liabilities and genomic instability conferred by loss of MTAP in tumor cells:

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MAT2A + PRMT5 inhibition. Accumulation of MTA in MTAP-deleted tumors partially inhibits PRMT5 activity, which increases cell dependence on MAT2A and results in a synthetic lethal vulnerability in such tumors when MAT2A is pharmacologically inhibited. As described below, we intend to evaluate the combination of IDE397 with our proprietary MTA-cooperative PRMT5 inhibitor, IDE892, in MTAP-deleted lung cancer.

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MAT2A + Co-alterations of MTAP. We are exploring other potential combination opportunities for our MTAP-related programs with agents that target common co-alterations of MTAP, such as RAS/KRAS and CDKN2A, the most common co-alteration of MTAP. The CDKN2A locus is commonly co-deleted with MTAP, resulting in loss of important tumor suppressor proteins that lead to tumor growth. We plan to nominate a development candidate for the CDKN2A program in the second half of 2026 followed by submission of an IND application to the U.S. FDA in the first half of 2027.

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IDE892 is a potential first-in-class, oral small molecule MTA-cooperative PRMT5 inhibitor. IDE892 was discovered through our iterative physics-based ligand design and optimization platform and is a highly potent and selective MTA-cooperative PRMT5 inhibitor with favorable drug-like properties. IDE892 together with IDE397 enables the evaluation of a wholly-owned clinical combination of the PRMT5 and MAT2A mechanisms, which may synergize to provide deeper, more durable responses in certain MTAP-deleted tumors. As shown below, IDE892 has demonstrated selective antiproliferative activity in MTAP-deleted tumor cell models as well as durable complete responses in combination with IDE397 in challenging MTAP-deletion preclinical models.

We received IND clearance from the FDA in the third quarter of 2025 and expect to begin a Phase 1 dose escalation trial in the first quarter of 2026 with the goal of advancing into combination trials with IDE397 in MTAP-deleted NSCLC in the second quarter of 2026.

MTAP-deleted solid tumor patient population

There are currently no approved therapies for patients with MTAP-deleted solid tumors, highlighting the unmet medical need in this setting. MTAP-deletion occurs in approximately 15% of all solid tumors, including 15% of NSCLC and 25% of UC, based on The Cancer Genome Atlas database. We estimate the U.S. annual incidence of MTAP-deleted tumors is approximately 62,000 patients across our priority tumor types of UC, NSCLC and pancreatic cancer, based on the 2024 Surveillance, Epidemiology, and End Results database.

Next Generation Therapies

Our fourth area of clinical focus is on the development of next generation therapies designed to intercept the fundamental dependencies underpinning tumor driver pathways. These targets potentially overcome the genetic and epigenetic tumor heterogeneity that otherwise limits the efficacy and durability of cancer therapies.

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IDE574 is a potential first-in-class, oral small molecule equipotent dual inhibitor of the lysine acetyltransferase (KAT) 6 and 7, both of which have been shown to support cancer cell survival. IDE574 selectively inhibits both KAT6 and KAT7, while sparing other structurally similar KAT molecules such as KAT5 and KAT8 that are required for normal cell function. KAT6 and KAT7 are mechanistically intertwined epigenetic modulators of cell identity and lineage commitment programs that are corrupted by oncogenic transformation. Dual KAT6/7 inhibition delivers robust and durable anti-tumor activity, superior to KAT6 inhibition alone, in preclinical tumor models with 8p11 amplifications, as well as in selected indications dependent upon lineage-specific transcription factor activity.

In January 2026, we received IND clearance from the FDA and are targeting to begin a Phase 1 dose escalation trial in patients with breast, lung, prostate and colorectal cancers in the first quarter of 2026.

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IDE275 is a potential first-in-class, oral small molecule inhibitor of the helicase domain of the Werner protein (WRN), a RecQ enzyme involved in the maintenance of genome integrity. Germline loss of function mutations in WRN lead to premature aging and pre-disposition to cancer. We have published preclinical data showing that the helicase functional domain of WRN is responsible for a synthetic lethal vulnerability in MSI-High tumor models. Microsatellite instability (MSI) refers to the change in a tumor cell’s DNA content, as the number of repeated microsatellites, or short repeated sequences of DNA, differs as the cells divide. Tumors classified as MSI-High represent approximately 3-4% of all cancers, including approximately 28% of endometrial and 10% of ovarian cancers and 15% of gastrointestinal tumors, including 22% of stomach adenocarcinoma.

In October 2024, GSK initiated a Phase 1 clinical trial with IDE275 in patients with MSI-High tumors pursuant to our 2020 Collaboration, Option and License Agreement. In December 2025, GSK notified us of its intention to terminate the Agreement, which will be effective 90 days following the date of GSK’s notice, or March 9, 2026. GSK will transfer the WRN (IDE275) IND back to us in accordance with the applicable provisions of the Agreement. Once complete, we intend to complete the dose expansion portion of the Phase 1 trial to inform the next phase of development.

Our Drug Discovery Engine in Precision Medicine Oncology

We have built a fully integrated platform to deliver a renewable pipeline of potential first-in-class programs. Highlights of our discovery and development capabilities are described below.

Precision Medicine Research Platform

We have established a robust precision medicine research platform with capabilities for identification and validation of new targets and biomarkers, drug discovery and translational biology. Our approach integrates small molecule drug discovery with extensive capabilities in identifying and validating translational biomarkers to develop targeted therapies for select patient populations that are most likely to benefit from these targeted therapies. Our small molecule drug discovery expertise includes discovery and development of small molecule therapeutics.

Our discovery platform includes our proprietary chemical library, INQUIRE™, structure-based drug design enabled by extensive structural biology and crystallography capabilities with over 200,000 chemical compounds, and our proprietary content-based machine-learning engine, HARMONY™, providing effective and efficient molecular design and structure-activity-relationship cycles.

DECIPHER™ Dual CRISPER Synthetic Lethality Library – UCSD

We have constructed our DECIPHER Dual CRISPR library for synthetic lethality target and biomarker discovery in collaboration with the University of California, San Diego, and bioinformatics analysis and validation are ongoing. The DECIPHER 1.0 library is focused on DDR targets across various tumor suppressor genes and oncogenes of interest that were selected based on their known prevalence and role in solid tumors, enabling evaluation of approximately 50,000 independent gene knockout combinations of DDR pathway-related drug targets across known tumor suppressor genes.

PAGEO™ Paralogous Gene Evaluation in Ovarian Cancer and Dep Map Consortium

We have an ongoing strategic collaboration with the Broad Institute focused on discovery of synthetic lethality targets and biomarkers. This collaboration uses the large-scale CRISPR paralog screening platform developed at the laboratory of William R. Sellers, M.D., Core Institute Member, Broad Institute, to evaluate functionally redundant paralogous genes across ovarian cancer subtypes and to generate novel target and biomarker hypotheses. Dr. Sellers, who also serves on our Scientific Advisory Board, is the principal investigator for the strategic collaboration. We have also become a member of the Broad DepMap (Cancer Dependency Map) consortium led by the Broad Institute to further enhance our efforts in bioinformatics and cell-based screening for synthetic lethality target and biomarker discovery and validation.

Strategy

Our mission is to bring forth the next wave of precision oncology therapies that are more selective, more effective, and deeply personalized with the goal of altering the course of disease and improving clinical outcomes for patients with cancer. Our current clinical pipeline consists of nine potential first-in-class product candidates focused across four strategic areas. We seek to treat patients earlier in their course of disease, whether first line or in the adjuvant and neo-adjuvant settings, and use rational combinations to drive deeper and more durable outcomes. Such combinations may be with proprietary assets in our pipeline or with assets obtained through collaborations and partnerships. We have also established relationships with diagnostics companies developing cutting-edge technologies for developing biomarkers and patient selection strategies for our product candidates. The principal components of our strategy are to:

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Develop and commercialize darovasertib for patients across all stages of uveal melanoma. Our most advanced product candidate, darovasertib, is an oral, potent and selective PKC inhibitor currently in multiple clinical trials in both the metastatic and pre-metastatic settings of UM. Approximately 95% of uveal melanoma patients have activating mutations in either GNA11 or GNAQ, resulting in overactivation of PKC and tumor cell growth. We are targeting to report topline results from the darovasertib and crizotinib combination in our registrational Phase 2/3 OptimUM-02 trial in 1L patients with HLA*A2(-) mUM in the first quarter of 2026. Data from this trial, if positive, will be used to support an accelerated approval filing in the United States. In parallel, we are advancing commercial readiness activities in the United States and globally with our partner, Servier, to make this treatment available to mUM patients in need around the world. Darovasertib is anticipated to be in three randomized, Phase 3 registrational trials across all stages of UM by the first half of 2026, including the Phase 2/3 OptimUM-02 trial in metastatic UM, our Phase 3 OptimUM-10 trial in the neoadjuvant setting and the planned Phase 3 OptimUM-11 trial in the adjuvant setting, which we are targeting to initiate in the second quarter of 2026. We believe data from these trials, if positive, will support the use of darovasertib in the majority of patients with UM.

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Prioritize and advance potentially first-in-class, differentiated precision oncology therapies and rational combinations for patients with solid tumors. Our current clinical pipeline consists of nine potential first-in-class product candidates across four clinical focus areas. Beyond darovasertib and crizotinib in UM, we are focused on evaluating the potential synergy between TOP1 ADCs and inhibitors of the DDR pathway, where our most advanced programs are IDE849, a DLL3 TOP1 ADC, and IDE161, an oral PARG inhibitor, that we are developing for patients with SCLC, NEC and other DLL3-overexpressing tumors. The TOP1-inhibitor payload induces replication stress in tumor cells, which is then amplified by the introduction of the systemic PARG inhibitor, resulting in mitotic catastrophe, and cell death. For patients with MTAP-deleted solid tumors we are exploring multiple combination strategies with IDE397, a selective MAT2A inhibitor, given as the backbone of therapy with Trodelvy, a Trop-2 TOP1 ADC, or IDE892, an MTA-cooperative PRMT5 inhibitor, where there is strong mechanistic rationale for the combination to drive deeper, more durable responses than either agent alone. Lastly, we have begun advancing a pipeline of next generation therapies focused on disrupting the key pathways that underpin tumor heterogeneity, drug resistance mechanisms and lineage addiction, led by IDE574, an equipotent dual inhibitor of KAT6/7. We believe our product portfolio offers a number of compelling

opportunities, either as monotherapies or in combinations, to improve the standard of care for patients with solid tumors.

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Leverage our core development capabilities to broaden our precision therapy pipeline. We are continuing our target identification and validation activities for advancing new targets and associated biomarkers, with active programs for several high-value targets. For example, we are planning to nominate a development candidate by the first half of 2026 for a novel program targeting the most common co-alteration of MTAP, CDKN2A, which we believe has strong combination potential with our existing clinical-stage assets in this area, IDE397 and IDE892. We will continue investing in our core functional and development capabilities, including target and drug discovery, bioinformatics and translational biology, to establish a deep clinical-stage pipeline of potentially first-in-class, differentiated precision therapies for patients with cancer.

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Selectively establish relationships with third parties to accelerate our pipeline development, strengthen our capital resources and maximize the commercial potential of our product candidates. We have established multiple value-accretive collaborations with leading pharmaceutical companies to support our clinical development activities, expand our pipeline and broaden our global commercial reach. We are collaborating with Pfizer and Gilead on the clinical development of darovasertib in UM and IDE397 for MTAP-deleted UC and NSCLC, respectively. We also entered into exclusive in-license agreements with Hengrui Pharma for IDE849 and Biocytogen for IDE034, which added two potentially first-in-class TOP1 ADCs to our internally-discovered pipeline. Most recently, we entered into an exclusive license agreement with Servier to develop and commercialize darovasertib outside of the United States, for which we received an upfront payment of $210.0 million and potential future milestones of $320.0 million. We will continue to evaluate future collaborations, where appropriate, to complement our pipeline, accelerate or enhance our clinical development efforts and provide additional sources of capital to support our business.

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Collaborate with leaders in the field of diagnostics to enable the identification of defined patient populations for our product candidates. Our precision medicine approach leverages the availability or development of companion diagnostics to identify the right patients for which our product candidates may be most effective. We have established relationships with leading companies in the diagnostic space, including Foundation Medicine, Guardant Health and Tempus, to ensure our clinical programs are developed for patient groups most likely to benefit based on the genetics or expression profile of their disease. We are also incorporating new genetic testing technologies, such as next-generation sequencing of circulating tumor DNA, to solidify these efforts in our clinical development.

Competition

Our industry is very competitive and subject to change based on ongoing advances in technology. Although we believe that our approach, strategy, scientific capabilities, knowledge and experience provide us with competitive advantages, we expect to have substantial competition from major pharmaceutical companies, specialty pharmaceutical companies and biotechnology companies worldwide. Many of our competitors have significantly greater financial, technical and human resources. Smaller and early-stage companies may also prove to be significant competitors, particularly through collaborative arrangements with large and established companies. As a result, our competitors may discover, develop, license or commercialize products before or more successfully than we do. We face competition with respect to product candidates in our pipeline and will face competition with respect to future product candidates, from segments of the pharmaceutical, biotechnology and other related markets that pursue targeted approaches to addressing activating genetic and other molecular alterations in cancer.

For darovasertib, we are not aware of other companies actively developing clinical-stage therapeutics directed to PKC as a target for solid tumors. Varsity Pharma is preclinically evaluating a PKC inhibitor in CLL, and Aquilon has nominated PKC theta as a target for preclinical development. Additionally, Windtree Therapeutics is advancing a preclinical-stage atypical PKC iota inhibitor, including both topical and oral formulations, for potential treatment of Basal Cell Carcinoma. We are aware of several other companies conducting research and development of potential therapies for primary UM or for mUM based on other targets and approaches. Replimune has initiated a potentially registration-enabling trial for RP-2, an oncolytic immunotherapy. iOnctura has initiated a Phase 2 trial for Roginolisib, an allosteric PI3K delta inhibitor, in 2L+ mUM. Other programs in development for mUM include Novartis’ DYP688, an ADC, with a GNAQ-11 inhibitor payload in a Phase 1/2 clinical trial, and Immatics’ anzu-cel/IMA203, a PRAME-targeting TCR-based, T cell therapy. Aura Biosciences is developing bel-sar, a virus-like drug conjugate (VDC), as local treatment for early-stage choroidal melanoma. Additionally, Immunocore has commercialized Tebentafusp, also known under its branded name as Kimmtrak, for the treatment of adult patients with HLA*A2(+), unresectable or metastatic UM.

For IDE849, our competitors include companies developing DLL3-targeting therapies using various therapeutic modalities, including bispecific T-cell engagers (BiTEs), ADCs, chimeric antigen receptor (T-cell) therapies, and radiopharmaceuticals. Amgen received accelerated approval from the FDA in May 2024 for Tarlatamab (branded name Imdelltra), a DLL3-CD3 BiTE. Zelgen, Boehringer Ingelheim and Daiichi Sankyo are developing drugs with a similar mechanism of action, in Phase 3 or Phase 2 studies. We are aware of several companies developing DLL3 ADCs with Topoisomerase I inhibitor payloads. Zai Lab recently initiated a Phase 3 trial for ZL-1310 in relapsed SCLC and Roche, Zhang Jiang, and Baili are conducting Phase 1 studies. In radiopharmaceuticals, Abdera, Molecular Partners, and Novartis are conducting Phase 1 clinical trials and several other companies are pursuing preclinical development of DLL3-targeting radiotherapies.

For IDE034, we are not aware of any other companies developing bi-specific ADCs targeting both B7H3 and PTK7, however many companies are developing mono-antigen ADCs targeting either B7H3 or PTK7. Merck, Hansoh/GSK, Medilink, and Minghui are evaluating B7H3 ADCs in Phase 3 clinical trials. Several other companies have B7H3 ADCs in earlier phases of clinical development, including BeOne, Duality, Innovent, Mabwell and MacroGenics. Furthermore, Day One, Kelun, Kivu and Lilly are evaluating PTK7 ADCs in Phase 1 studies.

For IDE161, 858 Therapeutics is conducting a Phase 1 clinical trial for its small molecule PARG inhibitor, ETX-19477. Several other companies have more recently initiated Phase 1 studies for PARG inhibitors, including Danatlas, Evopoint, FoRx, and SynRx. Additionally, several companies are conducting preclinical research to develop PARG inhibitors, including Aigen, Alivexis, Azkarra, Nodus Oncology, Satya Pharma Innovations, and QuantX.

For IDE705, Artios Pharma is developing a Pol Theta inhibitor, designated as ART-6043, in a Phase 1/2 study. Several other companies have initiated Phase 1 studies for Pol Theta inhibitors, including Danatlas, Gilead, Moma Therapeutics, Simcere, and SynRx. Additionally, Breakpoint Therapeutics and QuantX have Pol Theta inhibitors in IND-enabling studies.

For IDE397, Servier is evaluating a small molecule MAT2A inhibitor designated as S095035 in a Phase 1/2 trial. Insilico Medicine and BeOne Medicines have also initiated Phase 1 trials for their small molecule MAT2A inhibitors called ISM3412 and BG-89894, respectively. Additionally, Genhouse Bio, Hanmi, ScinnoHub, SK Biopharma and Shouyao have small molecule MAT2A inhibitors in preclinical development.

For IDE892, we are aware of many companies developing PRMT5 inhibitors in both clinical and preclinical stages. Bristol Myers Squibb (BMS) has initiated Phase 2/3 trials for navlimetostat (BMS-986504) in first line MTAP-deleted NSCLC and pancreatic ductal adenocarcinoma. The next most advanced assets include AMG-193 from Amgen, AZD-3470 from AstraZeneca, BGB-58067 from BeOne, and vopimetostat (TNG462) from Tango, which are all in Phase 1/2 studies. At least ten other companies have initiated Phase 1 clinical trials and more than ten companies are advancing preclinical PRMT5 inhibitors.

For IDE574, Pfizer is evaluating a KAT6/7 dual inhibitor in a Phase 1 clinical trial in addition to KAT6A inhibitor prifetrastat (PF-07248144) in a Phase 3 clinical trial. Several other companies are also developing drugs directed to KAT6 only, including Hengrui, Menarini and Olema, which are conducting Phase 1 trials. Additionally, Isosterix, Prelude, Qubit and several others are developing preclinical KAT6 inhibitors.

For IDE275, Vividion is developing a covalent WRN inhibitor designated as VVD-133214 in a Phase 1 trial. Novartis and Nimbus Therapeutics are evaluating non-covalent WRN inhibitors, called HRO-761 and NDI-219216 respectively, in Phase 1 trials. Eikon and MOMA Therapeutics also more recently initiated Phase 1 trials for WRN inhibitors. Additionally, several companies are conducting preclinical research to develop WRN inhibitors, including Genhouse, Insilico, and Puhe, among others.

For our preclinical pipeline of synthetic lethality therapeutics, potential competition includes established companies as well as earlier-stage emerging biotechnology companies. Multiple established companies have been involved with research and development in synthetic lethality, such as AstraZeneca (Lynparza), Pfizer (Talzenna), GSK (Zejula) and Roche. Additionally, several other early-stage companies are developing synthetic lethality therapeutics, including 858 Therapeutics, Artios, Breakpoint Therapeutics, Eikon, FoRx Therapeutics, Repare Therapeutics, Ryvu Therapeutics, Tango, Vividion, and Xpose.

Intellectual Property

Intellectual property, including patents, trade secrets, trademarks and copyrights, is important to our business. We endeavor to establish, maintain and enforce intellectual property rights that protect our business interests.

Our patent portfolio, including patents owned by or exclusively licensed to us, is built on a program-by-program basis with a goal of establishing broad protection that generally includes, for each product candidate compound and for selected alternative back-up compounds, claims directed to composition of matter, pharmaceutical compositions, and methods of treatment using such pharmaceutical compositions. For some programs, our portfolio may also include claims directed to methods of treatment involving biomarker-enabled patient identification or selection, methods of treatment involving particular dosing approaches, polymorphs, formulations and/or methods of synthesis. We are seeking and maintaining patent protection in the United States and key foreign jurisdictions.

As of January 30, 2026, we own or exclusively in-license patents and patent applications, comprising approximately 71 distinct patent families, protecting our technology across our pipeline. Excluding applications that we are not currently prosecuting, our portfolio consists of approximately 21 issued U.S. patents, approximately 37 pending U.S. applications, 15 pending applications under the Patent Cooperation Treaty (PCT) 65 issued foreign patents and approximately 185 pending foreign applications in approximately 40 foreign jurisdictions, including without limitation countries included in major markets in North America, Europe, and Asia, each having expiration dates ranging from 2035 to 2046. The nominal expiration of our patents and patent applications does not account for any applicable patent term adjustments or extensions.

As of January 30, 2026, as relating to our PKC program, including darovasertib, we own or have exclusively in-licensed from Novartis patents and patent applications comprising approximately seven issued U.S. patents, approximately 34 issued foreign patents, approximately eight pending U.S. applications, approximately two pending PCT application, and approximately 48 pending applications in approximately 20 foreign jurisdictions which we are currently prosecuting, including without limitation countries included in major markets in North America, Europe, and Asia. These in-licensed patents and applications are directed to composition of matter, pharmaceutical compositions and methods of treatment, including treatment of UM. These solely owned or in-licensed patent applications, if granted, would expire between 2035 and 2045, without taking into account any applicable patent term adjustments or extensions. In addition, the PKC program portfolio includes two U.S. patent application, which are jointly owned with Pfizer directed to methods of treatment for certain combination treatments.

As of January 30, 2026, as relating to our MAT2A program, including IDE397, we own patents and patent applications comprising approximately five issued U.S. patents, approximately nine issued foreign patent, approximately 11 pending U.S. applications, approximately three pending PCT applications and approximately 69 pending foreign applications in approximately 26 foreign jurisdictions which we are currently prosecuting, including without limitation countries included in major markets in North America, Europe, and Asia. These solely owned or in-licensed patent applications, if granted, would expire between 2039 and 2045, without taking into account any applicable patent term adjustments or extensions. In addition, the MAT2A program portfolio also includes one pending US application and nine pending foreign applications directed to methods of treatment of cancer which are jointly owned with GSK; one pending US application, one pending PCT application, and five foreign applications directed to methods of treatment of cancer which are jointly owned with Amgen pursuant to the Amgen CTCSA; and one pending PCT application directed to methods of treatment of cancer which is jointly owned with Gilead pursuant to the Gilead CSCSA.

As of January 30, 2026, as relating to our PARG program, including IDE161, we own or have exclusively in-licensed from Cancer Research UK and University of Manchester, patents and patent applications comprising approximately four issued U.S. patents, approximately 17 issued foreign patents, approximately eight pending U.S. application, and approximately 67 pending foreign applications in approximately 37 foreign jurisdictions which we are currently prosecuting, including without limitation countries included in major markets in North America, Europe, and Asia. These solely owned or in-licensed patent applications, if granted, would expire between 2035 and 2044, without taking into account any applicable patent term adjustments or extensions.

Our patent portfolio also supports programs in our synthetic lethality preclinical pipeline, including U.S. patent applications directed to composition of matter, pharmaceutical compositions and/or methods of treatment of cancer for each of our Pol Theta (HR), WRN (MSI-High), PRMT5, KAT6A/7, ADC (DLL3), ADC (B7H3/PTK7), and certain next-generation SLT programs.

Strategic Relationships

We own or control all commercial rights within the United States for our most advanced program, darovasertib. We own or control all commercial rights worldwide for IDE397 and IDE161. We have entered into strategic relationships for these programs – for example, to in-license certain intellectual property rights or to enable evaluation of combination therapies, such as through combination drug supply or clinical trial collaborations to evaluate combinations. For darovasertib, we have an exclusive license agreement with Novartis and separately, we have established clinical trial collaboration and supply agreements with Pfizer in support of our clinical evaluation of darovasertib in combination with crizotinib in mUM. We have also granted an exclusive license to Servier to develop and commercialize darovasertib outside the United States. For IDE397, we entered into the Gilead CSCSA and the Second Gilead CSCSA to clinically evaluate IDE397 in combination with Trodelvy, the Gilead Trop-2 directed ADC, in patients with MTAP-deleted UC and NSCLC, respectively. For IDE161, we have an exclusive in-license agreement with Cancer Research UK and University of Manchester.

In 2020, we entered into a strategic partnership and collaboration with GSK for our synthetic lethality programs targeting Pol Theta (IDE705) and Werner Helicase (IDE275), pursuant to the GSK Collaboration, Option and License Agreement. GSK delivered written notice of its intention to terminate the collaboration in December 2025 and these programs will be transferred to us in accordance with the applicable provisions of the agreement.

We own all commercial rights to our earlier next-generation synthetic lethality programs, including IDE892 and IDE574, for which our small molecule compounds are being discovered and/or developed internally with our own resources, supplemented by certain service providers, such as CROs.

In 2024, we entered into two in-license agreements for ADCs with topoisomerase-I-inhibitor-payloads to enable combinations with our synthetic lethality programs. Pursuant to the Biocytogen Option and License Agreement, we obtained an option to in-license IDE034, a preclinical B7H3/PTK7 bispecific ADC, and we subsequently exercised the option to obtain worldwide commercial rights to the molecule. We also entered into the Hengrui Pharma License Agreement for global development and commercial rights to IDE849, a DLL3-targeting ADC, outside of Greater China. Under the terms of the Biocytogen Option and License Agreement and the Hengrui Pharma License Agreement, Biocytogen and Hengrui Pharma provide development manufacturing services for the ADCs.

We have established collaborative relationships with other companies for access to their proprietary database of patient samples, and/or for their genetic screening services on their proprietary platform. We have established certain development manufacturing and service relationships with contract manufacturing organizations (CMOs) for darovasertib, IDE397, and IDE161, as well as our early clinical candidates IDE892 and IDE574. We have an agreement with STA Pharmaceutical Hong Kong Limited Pharmaceutical (STA Pharmaceutical), and Yuhan Corporation for the synthesis of the API for darovasertib, and agreements with STA Pharmaceutical and Patheon Inc. for formulation and manufacturing of darovasertib drug product. We have an agreement with STA Pharmaceutical for the synthesis of the API, formulation and manufacturing of IDE397 drug product. We have an agreement with Pharmaron for the synthesis of the API, and with STA Pharmaceutical for the formulation and drug product manufacturing of IDE161, IDE892 and IDE574. We have established arrangements with CMOs as well for packaging, labeling and distribution of darovasertib, IDE397, and IDE161. We also have established clinical services relationship with CROs to support our conduct of clinical trials for our darovasertib, IDE397, and IDE161 programs.

In addition to these existing strategic license relationships, existing and planned development manufacturing and service arrangements, and existing and planned clinical services arrangements, we have various existing agreements and relationships with service providers, such as CROs, which are enabling execution of various research and development activities for each of our pipeline programs. In particular, such agreements are directed to chemistry and compound synthesis, compound analysis and characterization, structural biology, computational biology, biological assay and model development, in vitro screening, in vivo screening, translational biomarker diagnostic development, bioinformatics, toxicology and formulation, among other activities.

We may also evaluate future strategic opportunities to accelerate development timelines and maximize the commercial potential of our product candidates. We plan to selectively evaluate strategic collaborations with biopharmaceutical partners whose research, development, commercial, marketing, and geographic capabilities complement our own.

Agreements

Clinical Trial Collaboration and Supply Agreements with Pfizer for Darovasertib

In March 2020, we entered into a Clinical Trial Collaboration and Supply Agreement with Pfizer, Inc., as amended in September 2020, April 2021, September 2021 and May 2023 (the Pfizer Agreement). Pursuant to the Pfizer Agreement, Pfizer supplies us with their MEK inhibitor, binimetinib, and their cMET inhibitor, crizotinib, to evaluate combinations of darovasertib independently with each of the Pfizer compounds, in patients with tumors harboring activating GNAQ or GNA11 mutations. Under the Pfizer Agreement, we are the sponsor of the combination studies and will provide darovasertib and pay for the costs of the combination studies. Pfizer will provide binimetinib and crizotinib for use in the clinical trial at no cost to us. The Pfizer Agreement provides that we and Pfizer will jointly own clinical data generated from the clinical trial and will also jointly own inventions, if any, relating to the combined use of darovasertib and binimetinib, or independently, to the combined use of darovasertib and crizotinib. We and Pfizer have formed a joint development committee responsible for coordinating all regulatory and other activities under the agreement.

In March 2022, we and Pfizer entered into a Second Clinical Trial Collaboration and Supply Agreement (as amended in May 2023) (the Second Pfizer Agreement), pursuant to which we are evaluating darovasertib and crizotinib as a combination therapy in mUM in a planned Phase 2/3 potential registration-enabling clinical trial. Pursuant to the Second Pfizer Agreement, we are the sponsor of the combination trial and we will provide darovasertib and pay for the costs of the combination trial; Pfizer will provide crizotinib for the planned combination trial at no cost to us for up to an agreed-upon number of mUM patients. We and Pfizer will jointly own clinical data from the planned combination trial and all inventions relating to the combined use of darovasertib and crizotinib. We and Pfizer have formed a joint development committee responsible for coordinating all regulatory and other activities under the Second Pfizer Agreement.

Separately, in March 2022, we and Pfizer also entered into a Third Clinical Trial Collaboration and Supply Agreement (the Third Pfizer Agreement), pursuant to which we could, subject to preclinical validation and FDA feedback and guidance, evaluate darovasertib and crizotinib, as a combination therapy in cMET-driven tumors such as NSCLC and/or HCC in a Phase 1 clinical trial. Pursuant to the Third Pfizer Agreement, we would have been the sponsor of the planned combination trial, and we would provide darovasertib and pay for the costs of the combination trial; Pfizer would provide crizotinib for the planned combination trial at no cost to us. Pursuant to Amendment No. 1 to the Second Pfizer Agreement, as described below, we and Pfizer terminated the Third Pfizer Agreement.

In May 2023, we continued our relationship with Pfizer by entering into Amendment No. 4 to the Pfizer Agreement relating to the supply of crizotinib in support of this Phase 2 clinical trial, pursuant to which Pfizer will continue to provide us with an additional defined quantity of crizotinib at no cost.

We also expanded our relationship with Pfizer in May 2023 under an Amendment No. 1 to the Second Pfizer Agreement to support the Phase 2/3 registrational trial to evaluate darovasertib and crizotinib as a combination therapy in mUM. Under the as-amended Second Pfizer Agreement, Pfizer will provide us with a first defined quantity of crizotinib at no cost, as well as an additional second defined quantity of crizotinib at a lump-sum cost. The Third Pfizer Agreement has been terminated by us and Pfizer under Amendment No. 1 to the Second Pfizer Agreement.

In December 2024, we entered into Amendment No. 5 to the Pfizer Agreement for the supply of crizotinib in the Phase 1/2 clinical trial for Pfizer to provide us a defined quantity of crizotinib at defined costs.

Exclusive License Agreement with Novartis for Darovasertib

In September 2018, we entered into a license agreement with Novartis to develop and commercialize Novartis’ LXS196 (also known as IDE196), a Phase 1 PKC inhibitor, for the treatment of cancers with GNAQ and GNA11 mutations. We renamed Novartis’ LXS196 oncology as IDE196, and which has a non-proprietary name of darovasertib. Under the license agreement, Novartis granted to us a worldwide, exclusive, sublicensable license to research, develop, manufacture, and commercialize certain defined compounds and products, including IDE196 and certain other PKC inhibitors, as well as companion diagnostic products, collectively referred to as the licensed products, for any purpose.

All inventions, know-how, data and results resulting from our activities under the license agreement, including activities relating to our own clinical trials, will be exclusively owned by us. All inventions, know-how, data and results resulting from Novartis’ activities connected with Novartis’ ongoing Phase 1 clinical trial for IDE196 will be exclusively owned by Novartis, and subject to the license to us. Ownership of all other inventions and know-how will be determined according to U.S. patent law, with Novartis’ interest subject to the license to us.

We control the prosecution and maintenance of the patents exclusively licensed to us, with Novartis retaining step-in rights if we do not continue such prosecution and maintenance. If we fail to maintain or prosecute any exclusively licensed patent and Novartis exercises this step-in right, our license to the relevant patents will terminate in the relevant country. We have the first right to enforce any exclusively licensed patents, while Novartis retains the right to representation. If we do not

bring an action to enforce any exclusively licensed patent, Novartis has the right to bring such action, and we will have the right to representation.

We paid Novartis an upfront payment of $2.5 million and issued 263,615 shares of our Series B redeemable convertible preferred stock concurrently with the execution of the license agreement. Subject to completion of certain clinical and regulatory development milestones, we agreed to make milestone payments in the aggregate of up to $9.0 million, and subject to achievement of certain commercial sales milestones, we agreed to make milestone payments in the aggregate of up to $20.0 million. We also agreed to pay mid to high single-digit tiered royalty payments based on annual worldwide net sales of licensed products, payable on a licensed product-by-licensed product and country by country basis until the latest of the expiration of the last to expire exclusively licensed patent, the expiration of regulatory exclusivity, and the ten year anniversary of the first commercial sale of such product in such country. The royalty payments are subject to reductions for lack of patent coverage, loss of market exclusivity, and payment obligations for third-party licenses.

In March 2025, the FDA granted Breakthrough Therapy designation (“BTD”) for darovasertib, a potential first-in-class PKC inhibitor, for the neoadjuvant treatment of adult patients with primary uveal melanoma (“UM”) for whom enucleation has been recommended. Under the license agreement with Novartis, the Company paid Novartis a $1.0 million milestone payment in April 2025.

License Agreement with Servier for Darovasertib outside of the United States

In August 2025, we entered into an exclusive license agreement with Servier, pursuant to which we granted to Servier an exclusive license under certain intellectual property rights controlled by us relating to darovasertib to develop and commercialize products in all countries worldwide except for the United States for all diagnostic, prophylactic and therapeutic uses in humans. We received an upfront payment of $210.0 million and are eligible to receive development and regulatory milestone payments of up to an aggregate of $100.0 million, commercial milestone payments of up to an aggregate of $220.0 million, clinical trial cost sharing and clinical trial cost reimbursement, and royalties on net sales of products outside of the United States ranging from mid-teens to low-twenties percentages. Servier will be responsible for the regulatory and commercial activities for darovasertib outside the United States. We and Servier will collaborate on the development of darovasertib and share the associated costs. We retain all rights to darovasertib in the United States. The Servier license agreement will remain in effect on a product-by-product and country-by-country basis until expiration of royalty obligations. Either party may terminate for uncured material breach or insolvency of the other. We may terminate the Servier license agreement if (i) Servier ceases development or commercialization in certain countries for a specified period, or (ii) Servier, its affiliates, or its sublicensees challenge licensed patents, subject to certain exceptions. Servier may terminate at will upon specified prior notice. The Servier license agreement contains various representations, warranties, covenants, dispute resolution mechanisms, indemnities and other provisions customary for transactions of this nature.

Clinical Study Collaboration and Supply Agreement with Gilead for IDE397

In November 2023, we entered into the Gilead CSCSA to clinically evaluate IDE397 in combination with Trodelvy (sacacituzumab-govitecan-hziy), a Trop-2 directed ADC, in patients having MTAP-deletion UC, in a Phase 1 clinical trial. Under the mutually non-exclusive Gilead CSCSA, we will receive Trodelvy drug supply from Gilead and will sponsor the Phase 1 clinical combination trial evaluating ID397 and Trodelvy. Gilead will bear internal or external costs incurred in connection with its supply of Trodelvy. We will bear all internal and external costs and expenses associated with the conduct of the combination study. We and Gilead will jointly oversee clinical development of the combination therapy through a Joint Steering Committee responsible for coordinating all regulatory and other activities under the Gilead CSCSA. We and Gilead each retain commercial rights to its respective compounds, including with respect to use as a monotherapy agent or combination agent.

On February 12, 2025, we entered into the Second Gilead CSCSA with Gilead pursuant to which we and Gilead will collaborate on a portion of our Phase 1 study for the clinical evaluation of IDE397 in combination with Trodelvy (the Combination Study), in certain patients with advanced solid tumors in lungs. Pursuant to the Second Gilead CSCSA, we are the sponsor of the Combination Study, and we will provide the IDE397 compound and pay for the costs of the Combination Study. Gilead will provide Trodelvy for the Combination Study at no cost to us. We and Gilead will jointly own clinical data from the Combination Study and all inventions relating to the combined use of IDE397 and Trodelvy. Each party retains commercial rights to its respective compounds, including with respect to use as a monotherapy or combination agent. We and Gilead will form a joint steering committee responsible for coordinating all regulatory and other activities under the Second Gilead CSCSA.

Exclusive Option and License Agreement with Cancer Research UK and University of Manchester for IDE161

In April 2017, we entered into the CRUK/Manchester Agreement with Cancer Research UK and University of Manchester, which was amended on April 24, 2019 and on March 3, 2020, for the development and commercialization of licensed products comprising pharmaceutical preparations of PARG inhibitors for all therapeutic uses.

Under this agreement, Cancer Research UK and University of Manchester have granted to us, and we have in turn granted to Cancer Research UK and University of Manchester, non-exclusive, sublicensable, royalty-free licenses to carry out non-clinical research during the research term, which ended with our exercise of our option described below. The non-clinical research was governed by a joint research committee comprised of representatives from each party. During the research term, no party was to undertake a drug discovery program in PARG inhibitors other than under this agreement.

Cancer Research UK also granted us the exclusive option to obtain an exclusive, sublicensable, worldwide, royalty-bearing license, under certain Cancer Research UK background intellectual property and Cancer Research UK’s interest in any intellectual property jointly developed under the agreement, to research, develop, manufacture, and commercialize licensed products, as well as a non-exclusive, sublicensable, royalty-free, freedom-to-operate license under related intellectual property. Cancer Research UK and University of Manchester retain certain rights under the licensed intellectual property for academic, non-commercial research and teaching.

In January 2022, we exercised our option for an exclusive worldwide license covering a broad class of PARG inhibitors from Cancer Research Technology Ltd. (CRT), and the University of Manchester, and in connection therewith, paid a one-time option exercise fee of £250,000.

Following our option exercise, we gained sole control and responsibility for the research, development, manufacture, and commercialization of the licensed PARG inhibitors. Cancer Research UK also transferred its know how relating to the research, development or manufacturing of the licensed PARG inhibitors to us. We are obligated to develop a PARG inhibitor for the treatment of a cancer indication now that we exercised the option.

Each party is the sole owner of any intellectual property it develops solely under the agreement, and the parties will be joint owners of any jointly developed intellectual property. Each party grants the other a non-exclusive, fully-paid, royalty free, irrevocable, sublicensable, perpetual license to its rights in such jointly created intellectual property to make, use and sell inventions claimed in the joint patents, except for those joint patents exclusively licensed to us under the agreement following our exercise of the option.

A total of up to £19.5 million in payments to CRT upon the achievement of specific development and regulatory approval events for development of a PARG inhibitor in oncologic diseases are payable under the agreement. We will also pay low single-digit tiered royalties, and potentially also sales-based milestones, to CRT based on net sales of licensed products. In addition, in the event we sublicense the intellectual property, we will also be obligated to pay CRT a specified percentage of any sublicense revenue.

In April 2023, we incurred an obligation to pay milestone payments in an aggregate amount of £750,000 to CRT based upon the achievement of certain milestones relating to first and second tumor histologies in connection with the Phase 1 portion of the Phase 1/2 clinical trial in oncologic diseases.

Collaboration, Option and License Agreement with GSK for Pol Theta and Werner Helicase

In June 2020, we entered into the GSK Collaboration Agreement with GSK, pursuant to which we and GSK entered into a collaboration for its synthetic lethality programs targeting MAT2A, Pol Theta and WRN. On July 27, 2020, we and GSK received Hart-Scott-Rodino Antitrust Improvements Act clearance, and the GSK Collaboration Agreement became effective. Pursuant to the GSK Collaboration Agreement, GSK held a global, exclusive license to develop and commercialize Pol Theta products arising out of the Pol Theta program and WRN products arising out of the WRN program. We and GSK collaborated on preclinical research for the Pol Theta and WRN programs.

In December 2025, GSK notified us of its intention to terminate the Collaboration, Option and License Agreement, dated June 15, 2020. Pursuant to the terms of the Agreement, such termination will be effective 90 days following the date of GSK’s notice, which is March 9, 2026. During the ninety-day transition period, GSK will transfer the Werner Helicase (IDE275) and Pol Theta (IDE705) clinical programs to us in accordance with the applicable provisions of the Agreement.

Option and License Agreement with Biocytogen for IDE034

In July 2024, we entered into the Biocytogen Option and License Agreement with Biocytogen, pursuant to which Biocytogen granted us an option for an exclusive worldwide license to develop and commercialize products in connection with a potential first-in-class B7H3/PTK7 topoisomerase-I-inhibitor-payload BsADC program (the Option). Under the terms

of the Biocytogen Option and License Agreement, we paid Biocytogen an upfront fee and, upon our exercise of the Option, an exercise fee totaling $6.5 million.

In November 2024, we announced the selection of IDE034, a potential first-in-class B7H3/PTK7 topo-I-payload BsADC, as a development candidate and the exercise of the Option. Pursuant to our exercise of the Option, Biocytogen is eligible to receive additional development and regulatory milestone payments and commercial milestone payments, as well as low to mid-single-digit royalties on net sales. Total potential milestone payments equal an aggregate of $400.0 million, including development and regulatory milestone payments of up to $100.0 million. Our royalty obligations continue with respect to each country and each product until the later of (i) the date on which such product is no longer covered by certain intellectual property rights in such country and (ii) the 10th anniversary of the first commercial sale of such product in such country.

We will have the right to terminate the Biocytogen Option and License Agreement for any reason or no reason upon 90 days written notice to Biocytogen. Upon any termination of the Biocytogen Option and License Agreement after the exercise of the Option, the license granted to us will automatically terminate. We will have the right to sell any or all of the inventory of Licensed Products held by us as of the date of termination for a period of 12 months following such termination.

License Agreement with Hengrui Pharma for IDE849 (SHR-4849)

In December 2024, we entered into the Hengrui Pharma License Agreement with Hengrui Pharma, pursuant to which Hengrui Pharma granted us an exclusive worldwide license outside of Greater China to develop and commercialize SHR-4849, a novel DLL3-targeting topo-I-payload antibody drug conjugate.

Pursuant to the Hengrui Pharma License Agreement, Hengrui Pharma is eligible to receive upfront and milestone payments totaling $1.045 billion, including a $75.0 million upfront fee, up to $200.0 million in development and regulatory milestone payments, plus commercial success-based milestones. Hengrui Pharma is also eligible to receive mid-single to low-double digit royalties on net sales outside of Greater China.

In October 2025, the initiation of the first Phase 1 clinical trial, or first dosing of first patient, was achieved for IDE849 (SHR-4849). Under the license agreement with Hengrui Pharma, we paid Hengrui Pharma a $2.0 million milestone payment.

The Hengrui Pharma License Agreement will continue in effect on a product-by-product and country-by-country basis until the expiration of the obligation to make payments under the Hengrui Pharma License Agreement with respect to such product in each country, unless earlier terminated by either party pursuant to its terms. Either party may terminate the Hengrui Pharma License Agreement upon mutual agreement or for the other party’s insolvency or certain uncured material breaches. We may terminate the Hengrui Pharma License Agreement for any reason upon certain notice to Hengrui Pharma.

Sales and Marketing

We intend to become a fully integrated, commercial stage biopharmaceutical company focused on delivering transformative medicines to patients in need. We currently hold commercialization rights for darovasertib within the United States, worldwide commercialization rights for IDE397, IDE892, IDE034, IDE161, IDE574, IDE275, IDE705, and own or control all commercial rights outside of greater China for IDE849. Given our current stage of development, we have not yet fully built our commercialization capabilities. However, we have initiated planning and preparation for potential commercial operations, including for sales, marketing and market access capabilities, subject to the results of our Phase 2/3 clinical trial for darovasertib (OptimUM-02) and required regulatory approvals.

To enable our delivery of any approved medicines to patients, we plan to build our own sales force to commercialize them in the United States and potentially in Europe and other selected foreign countries for pipeline products beyond darovasertib. We believe a moderately sized specialty sales force, supported by effective marketing and sales management organizations, would enable us to reach healthcare professionals who specialize in the care of the patient populations for darovasertib and our other product candidates. We may also enter into distribution and other marketing or commercialization arrangements with third parties for any of our approved medicines to support their safe and effective use in appropriate patients.

Manufacturing

We currently rely, and expect to continue to rely, on third parties for the manufacture of our product candidates and our biomarker diagnostics for preclinical and clinical testing, as well as for future commercial manufacture of any drugs and

diagnostics that we may commercialize. We do not own or operate, and currently have no plans to establish, any manufacturing facilities.

In general, we plan to establish agreements with CMOs for synthesis of the active pharmaceutical ingredient (API) manufacturing of drug product comprising such API, as well as packaging, labeling and distribution.

We have also established supply arrangements with one or more CMOs for each of our small molecule development programs and with Biocytogen and Hengrui Pharma for our in-licensed ADCs in support of our current clinical development needs.

Our lead product candidates darovasertib, IDE397, IDE849, IDE161, IDE275, IDE705, IDE892, IDE034 and IDE574 are either small molecules or antibody drug conjugates that can be manufactured in reliable and reproducible processes. We believe the biochemical or synthetic processes are amenable to scale-up using standard manufacturing equipment and processes. We expect that the compounds being discovered and developed for our other pipeline programs and other future programs, can be produced at contract manufacturing facilities.

In many cases, we anticipate that the biomarker diagnostic may be commercially available on an existing third-party diagnostic panel or assay. In cases where such biomarker diagnostic is not already commercially available, we generally expect to establish agreements with strategic partners for clinical supply of companion diagnostics for biomarkers associated with the targeted therapeutics we are developing.

Government Regulation

Government authorities in the United States, at the federal, state and local level, and in other countries extensively regulate, among other things, the research, development, testing, manufacture, quality control, approval, labeling, packaging, storage, record-keeping, promotion, advertising, distribution, marketing and export and import of products such as those we are developing. A new drug must be approved by the FDA through the NDA process before it may be legally marketed in the United States.

U.S. Drug Development Process

In the United States, the FDA regulates drugs under the Federal Food, Drug, and Cosmetic Act (FDCA), and its implementing regulations. The process of obtaining regulatory approvals and the subsequent compliance with appropriate federal, state, local and foreign statutes and regulations require the expenditure of substantial time and financial resources. Failure to comply with the applicable U.S. requirements at any time during the product development process, approval process or after approval may subject an applicant to administrative or judicial sanctions. These sanctions could include the FDA’s refusal to approve pending applications, withdrawal of an approval, a clinical hold, warning letters, product recalls, product seizures, total or partial suspension of production or distribution, injunctions, fines, refusals of government contracts, restitution, disgorgement or civil or criminal penalties. Any agency or judicial enforcement action could have a material adverse effect on us.

The process required by the FDA before a drug may be marketed in the United States generally involves the following:

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completion of preclinical laboratory tests, animal studies and formulation studies in accordance with good laboratory practice (GLP), regulations and other applicable regulations;

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submission to the FDA of an IND, which must become effective before clinical trials in humans may begin;

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approval by an independent institutional review board (IRB), at each clinical site before each clinical trial may be initiated;

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performance of adequate and well-controlled human clinical trials in accordance with good clinical practice (GCP) regulations to establish the safety and efficacy of the proposed drug for its intended use;

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submission to the FDA of an NDA;

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satisfactory completion of an FDA advisory committee review, if applicable;

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satisfactory completion of an FDA inspection of the manufacturing facility or facilities at which the drug is produced to assess compliance with current good manufacturing practice (cGMP), regulations to assure that the facilities, methods and controls are adequate to preserve the drug’s identity, strength, quality and purity; and

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FDA review and approval of the NDA.

Once a pharmaceutical product candidate is identified for development, it enters the preclinical testing stage. Preclinical tests include laboratory evaluations of product chemistry, toxicity and formulation, as well as animal studies. An IND sponsor must submit the results of the preclinical tests, together with manufacturing information and analytical data, to the FDA as part of the IND. The sponsor will also include a protocol detailing, among other things, the objectives of the first phase clinical trial, the parameters to be used in monitoring safety, and the effectiveness criteria to be evaluated, if the first phase lends itself to an efficacy evaluation. Some preclinical testing may continue even after the IND is submitted. The IND automatically becomes effective 30 days after receipt by the FDA, unless the FDA, within the 30-day time period, places the clinical trial on a clinical hold. In such a case, the IND sponsor and the FDA must resolve any outstanding concerns before the clinical trial can begin. A clinical hold also may be imposed by the FDA at any time during a clinical trial due to safety concerns or non-compliance with specific FDA requirements, and the clinical trial may not continue until the FDA notifies the sponsor that the hold has been lifted.

All clinical trials must be conducted under the supervision of one or more qualified investigators in accordance with GCP regulations, which include the requirement that all research subjects provide their informed consent in writing for their participation in any clinical trial. They must be conducted under protocols detailing the objectives of the clinical trial, dosing procedures, subject selection and exclusion criteria and the safety and effectiveness criteria to be evaluated. Each protocol must be submitted to the FDA as part of the IND. An IRB at each institution participating in the clinical trial must review and approve each protocol before a clinical trial commences at that institution and must also approve the information regarding the clinical trial and the consent form that must be provided to each clinical trial subject or his or her legal representative, monitor the clinical trial until completed and otherwise comply with IRB regulations.

Human clinical trials are typically conducted in three sequential phases that may overlap or be combined:

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Phase 1: The product candidate is initially introduced into healthy human subjects and tested for safety, dosage tolerance, absorption, metabolism, distribution and excretion and, if possible, to gain an early indication of its effectiveness. In the case of some products for severe or life-threatening diseases, such as cancer, especially when the product may be too inherently toxic to ethically administer to healthy volunteers, the initial human testing is often conducted in patients. Sponsors sometimes designate their Phase 1 clinical trials as Phase 1a or Phase 1b. Phase 1b clinical trials are typically aimed at confirming dosing, pharmacokinetics and safety in a larger number of patients. Some Phase 1b studies evaluate biomarkers or surrogate markers that may be associated with efficacy in patients with specific types of diseases.

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Phase 2: This phase involves clinical trials in a limited patient population to identify possible adverse effects and safety risks, to preliminarily evaluate the efficacy of the product for specific targeted diseases and to determine dosage tolerance and appropriate dosage.

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Phase 3: Clinical trials are undertaken to further evaluate dosage, clinical efficacy and safety in an expanded patient population, generally at geographically dispersed clinical trial sites. These clinical trials are intended to establish the overall risk-benefit ratio of the product candidate and provide, if appropriate, an adequate basis for product labeling.

Post-approval trials, sometimes referred to as Phase 4 clinical trials, may be conducted after initial marketing approval. These clinical trials are used to gain additional experience from the treatment of patients in the intended therapeutic indication. In certain instances, the FDA may mandate the performance of Phase 4 clinical trials as a condition of approval of an NDA.

The FDA or the sponsor may suspend a clinical trial at any time on various grounds, including a finding that the research subjects or patients are being exposed to an unacceptable health risk. Similarly, an IRB can suspend or terminate approval of a clinical trial at its institution if the clinical trial is not being conducted in accordance with the IRB’s requirements or if the drug has been associated with unexpected serious harm to patients. In addition, some clinical trials are overseen by an independent group of qualified experts organized by the sponsor, known as a data safety monitoring board or committee. Depending on its charter, this group may determine whether a clinical trial may move forward at designated check points based on access to certain data from the clinical trial.

During the development of a new drug, sponsors are given opportunities to meet with the FDA at certain points. These points may be prior to submission of an IND, at the end of Phase 2, and before an NDA is submitted. Meetings at other times may be requested. These meetings can provide an opportunity for the sponsor to share information about the data gathered to date, for the FDA to provide advice, and for the sponsor and the FDA to reach agreement on the next phase of development. Sponsors typically use the meetings at the end of the Phase 2 clinical trial to discuss Phase 2 clinical results and present plans for the pivotal Phase 3 clinical trials that they believe will support approval of the new drug.

Concurrent with clinical trials, companies may conduct additional animal studies and also develop additional information about the chemistry and physical characteristics of the drug and finalize a process for manufacturing the product in commercial quantities in accordance with cGMP requirements. The manufacturing process must be capable of consistently producing quality batches of the product candidate and, among other things, the manufacturer must develop methods for testing the identity, strength, quality and purity of the final drug. In addition, appropriate packaging must be selected and tested, and stability studies must be conducted to demonstrate that the product candidate does not undergo unacceptable deterioration over its shelf life.

While the IND is active and before approval, progress reports summarizing the results of the clinical trials and nonclinical studies performed since the last progress report must be submitted at least annually to the FDA, and written IND safety reports must be submitted to the FDA and investigators for serious and unexpected suspected AEs, findings from other studies suggesting a significant risk to humans exposed to the same or similar drugs, findings from animal or laboratory testing suggesting a significant risk to humans, and any clinically important increased incidence of a serious suspected adverse reaction compared to that listed in the protocol or investigator brochure.

There are also requirements governing the reporting of ongoing clinical trials and completed clinical trial results to public registries. Sponsors of certain clinical trials of FDA-regulated products are required to register and disclose specified clinical trial information, which is publicly available at www.clinicaltrials.gov. Information related to the product, patient population, phase of investigation, clinical trial sites and investigators and other aspects of the clinical trial is then made public as part of the registration. Sponsors are also obligated to discuss the results of their clinical trials after completion. Disclosure of the results of these clinical trials can be delayed until the new product or new indication being studied has been approved.

U.S. Review and Approval Process

The results of product development, preclinical and other non-clinical studies and clinical trials, along with descriptions of the manufacturing process, analytical tests conducted on the chemistry of the drug, proposed labeling and other relevant information are submitted to the FDA as part of an NDA requesting approval to market the product. The submission of an NDA is subject to the payment of substantial user fees; a waiver of such fees may be obtained under certain limited circumstances. The FDA reviews an NDA to determine, among other things, whether a product is safe and effective for its intended use and whether its manufacturing is cGMP-compliant to assure and preserve the product’s identity, strength, quality and purity. The FDA conducts a preliminary review of all NDAs within the first 60 days after submission, before accepting them for filing, to determine whether they are sufficiently complete to permit substantive review. The FDA may request additional information rather than accept an NDA for filing. In this event, the NDA must be resubmitted with the additional information. The resubmitted application also is subject to review before the FDA accepts it for filing. Under the Prescription Drug User Fee Act (PDUFA) the FDA has agreed to certain performance goals in the review of NDAs through a two-tiered classification system, standard review and priority review. According to the current PDUFA performance goals for new molecular entity NDAs, the FDA endeavors to review and act on applications within ten months of the 60-day filing date under standard review, and within six months of the 60-day filing date under priority review.

The FDA may refer an application for a novel drug to an advisory committee. An advisory committee is a panel of independent experts, including clinicians and other scientific experts, that reviews, evaluates and provides a recommendation as to whether the application should be approved and under what conditions. The FDA is not bound by the recommendations of an advisory committee, but it considers such recommendations carefully when making decisions. Before approving an NDA, the FDA will inspect the facility or facilities where the product is manufactured. The FDA will not approve an application unless it determines that the manufacturing processes and facilities are in compliance with cGMP requirements and adequate to assure consistent production of the product within required specifications. Additionally, before approving an NDA, the FDA may inspect one or more clinical trial sites to assure compliance with GCP requirements.

After the FDA evaluates an NDA, it will issue an approval letter or a Complete Response Letter. An approval letter authorizes commercial marketing of the drug with prescribing information for specific indications. A Complete Response Letter indicates that the review cycle of the application is complete and the application will not be approved in its present form. A Complete Response Letter usually describes the specific deficiencies in the NDA identified by the FDA and may require additional clinical data, such as an additional pivotal Phase 3 clinical trial or other significant and time-consuming requirements related to clinical trials, nonclinical studies or manufacturing. If a Complete Response Letter is issued, the sponsor must resubmit the NDA, addressing all of the deficiencies identified in the letter, or withdraw the application. Even if such data and information are submitted, the FDA may decide that the NDA does not satisfy the criteria for approval.

If a product receives regulatory approval, the approval may be significantly limited to specific diseases and dosages or the indications for use may otherwise be limited, which could restrict the commercial value of the product. In addition, the FDA may require a sponsor to conduct Phase 4 testing, which involves clinical trials designed to further assess a drug’s safety and effectiveness after NDA approval, and may require testing and surveillance programs to monitor the safety of approved products which have been commercialized. The FDA may also place other conditions on approval, including the requirement for a risk evaluation and mitigation strategy (REMS), to assure the safe use of the drug. If the FDA concludes a REMS is needed, the sponsor of the NDA must submit a proposed REMS. The FDA will not approve the NDA without an approved REMS, if required. A REMS could include medication guides, physician communication plans or elements to assure safe use, such as restricted distribution methods, patient registries and other risk minimization tools. Any of these limitations on approval or marketing could restrict the commercial promotion, distribution, prescription or dispensing of products. Marketing approval may be withdrawn for non-compliance with regulatory requirements or if problems occur following initial marketing.

Pediatric Use

Even when not pursuing a pediatric indication, under the Pediatric Research Equity Act (PREA), an NDA or supplement thereto must contain data that is adequate to assess the safety and effectiveness of the drug product for the claimed indications in all relevant pediatric subpopulations, and to support dosing and administration for each pediatric subpopulation for which the product is safe and effective. In addition, any sponsor planning to submit an NDA or supplement subject to PREA must submit an initial pediatric study plan (iPSP), to the IND early in development. The iPSP must contain an outline of the proposed pediatric trials the sponsor plans to conduct, including trial objectives and design, any deferral or waiver requests, and other information required by regulation. The FDA must then review the information submitted, consult with the sponsor, and agree upon a final plan. The FDA or the sponsor may request an amendment to the plan at any time. The FDA may, on its own initiative or at the request of the applicant, grant deferrals for submission of some or all pediatric data until after approval of the product for use in adults, or full or partial waivers from the pediatric data requirements.

Separately, the FDA may issue a Written Request for pediatric studies relating to a drug product if it has determined that information related to the use of the drug in the pediatric population may produce health benefits. If the sponsor conducts the studies pursuant to the Written Request and submits the study reports within the specified timeline, the drug may be entitled to pediatric exclusivity. Pediatric exclusivity is a type of non-patent marketing exclusivity which, if granted, provides for the attachment of an additional six months of marketing protection to the term of any existing exclusivity. Sponsors may submit a proposal asking the FDA to issue a Written Request for this purpose.

U.S. Orphan Drug Designation

Under the Orphan Drug Act, the FDA may grant orphan drug designation to a drug intended to treat a rare disease or condition, which is a disease or condition that affects fewer than 200,000 individuals in the United States or, if it affects more than 200,000 individuals in the United States, there is no reasonable expectation that the cost of developing and making the drug product available in the United States for the disease or condition will be recovered from sales of the product in the United States. Orphan drug designation must be requested before submitting an NDA. After the FDA grants orphan drug designation, the identity of the therapeutic agent and its designated orphan use are disclosed publicly by the FDA. Orphan drug designation conveys certain financial incentives, including opportunities for grant funding, tax credits for certain clinical trial costs and certain user-fee waivers. Orphan designation does not convey any advantage in or shorten the duration of the regulatory review and approval process.

If a product that has orphan drug designation subsequently receives the first FDA approval for the disease or condition for which it has such designation, the product is entitled to orphan drug exclusivity, which means that the FDA may not approve any other application to market the same drug for the same indication for seven years, except in limited circumstances, such as a subsequent product demonstration of clinical superiority to the product with orphan drug exclusivity. Competitors may receive approval of different drugs for the indication for which the orphan product has exclusivity or obtain approval for the same drug but for a different indication from that for which the orphan product has exclusivity. Our product candidates could also be blocked from approval if a competitor obtains approval of the same drug for the same rare disease or condition before we do.

A designated orphan drug may not receive orphan drug exclusivity if it is approved for a use that is broader than the indication for which it received orphan designation. In addition, exclusive marketing rights in the United States may also be

lost if the FDA later determines that the request for designation was materially defective or if the manufacturer is unable to assure sufficient quantities of the product to meet the needs of patients with the rare disease or condition.

In April 2022, the FDA designated darovasertib as an orphan drug for the treatment of UM, including mUM, and we may seek orphan drug designation for additional product candidates in the future. Orphan drug designation does not guarantee that any product candidate will be approved for the designated rare disease or condition, if at all.

U.S. Expedited Development and Review Programs

The FDA offers a number of expedited development and review programs for qualifying product candidates intended to treat serious or life-threatening diseases or conditions.

New drug products are eligible for fast track designation if they are intended to treat a serious or life-threatening disease or condition and demonstrate the potential to address unmet medical needs for the disease or condition. Fast track designation applies to the combination of the product and the specific indication for which it is being studied. The sponsor of a fast track product has opportunities for frequent interactions with the review team during product development and, once an NDA is submitted, the product may be eligible for priority review. A fast track product may also be eligible for rolling review, where the FDA may consider for review sections of the NDA on a rolling basis before the complete application is submitted, if the sponsor provides a schedule for the submission of the sections of the NDA, the FDA agrees to accept sections of the NDA and determines that the schedule is acceptable, and the sponsor pays any required user fees upon submission of the first section of the NDA.

A product intended to treat a serious or life-threatening disease or condition may also be eligible for breakthrough therapy designation to expedite its development and review. A product can receive breakthrough therapy designation if preliminary clinical evidence indicates that the product may demonstrate substantial improvement over existing therapies on one or more clinically significant endpoints, such as substantial treatment effects observed early in clinical development. The designation includes all of the fast track program features, as well as more intensive FDA interaction and guidance beginning as early as Phase 1 and an organizational commitment to expedite the development and review of the product, including involvement of senior managers.

After an NDA is submitted for a product, including a product with a fast track designation and/or breakthrough therapy designation, the NDA may be eligible for priority review. A product is eligible for priority review if it has the potential to provide a significant improvement in the treatment or prevention of a serious disease or condition compared to marketed products. If the drug contains a new molecular entity, priority review designation means the FDA’s goal is to take an action on the marketing application within six months of the 60-day filing date, compared with ten months under standard review.

Additionally, products studied for their safety and effectiveness in treating serious or life-threatening diseases or conditions may receive accelerated approval upon a determination that the product has an effect on a surrogate endpoint that is reasonably likely to predict clinical benefit, or on a clinical endpoint that can be measured earlier than irreversible morbidity or mortality, that is reasonably likely to predict an effect on irreversible morbidity or mortality or other clinical benefit, taking into account the severity, rarity, or prevalence of the condition and the availability or lack of alternative treatments. As a condition of accelerated approval, the FDA will require the sponsor to perform one or more adequate and well-controlled post-marketing confirmatory trials to verify and describe the anticipated effect on irreversible morbidity or mortality or other clinical benefit. In addition, the FDA currently requires as a condition for accelerated approval pre-approval of promotional materials, which could adversely impact the timing of the commercial launch of the product. The FDA may withdraw approval of a drug or indication approved under the accelerated approval pathway if a trial required to verify the predicted clinical benefit fails to verify such benefit or if the applicant fails to conduct any required post-approval trial with due diligence. Recently, the Food and Drug Omnibus Reform Act (FDORA) enacted as part of the year-end omnibus spending bill in December 2022, included several reforms intended to expand the FDA’s ability to regulate products receiving accelerated approval, including by increasing the FDA’s oversight over the conduct of confirmatory trials.

Even if a product qualifies for one or more of these expedited development and review programs, the FDA may later decide that the product no longer meets the conditions for qualification or decide that the time period for FDA review or approval will not be shortened. In November 2022, the FDA granted fast track designation to darovasertib in combination with crizotinib for treatment of adult patients with mUM, and in September 2023, the FDA granted two fast track designations to IDE161 for specific ovarian and breast cancer indications. We also expect to pursue breakthrough therapy designation and accelerated approval for darovasertib and may explore some of these opportunities for our other product candidates as appropriate.

U.S. Post-approval Requirements

Once an approval is granted, the FDA may withdraw the approval if compliance with regulatory standards is not maintained or if problems occur after the product reaches the market. Later discovery of previously unknown problems with a product may result in restrictions on the product or even complete withdrawal of the product from the market. After approval, some types of changes to the approved product, such as adding new indications, certain manufacturing changes and additional labeling claims, are subject to further FDA review and approval. Drug manufacturers and other entities involved in the manufacture and distribution of approved drugs are required to register their establishments with the FDA and certain state agencies, and are subject to periodic unannounced inspections by the FDA and certain state agencies for compliance with cGMP regulations and other laws and regulations. In addition, the FDA may impose a number of post-approval requirements as a condition of approval of an NDA. For example, the FDA may require post-marketing testing, including Phase 4 clinical trials, and surveillance to further assess and monitor the product’s safety and effectiveness after commercialization.

Any drug products manufactured or distributed by us or our partners pursuant to FDA approvals will be subject to continuing regulation by the FDA, including, among other things, record-keeping requirements, reporting of adverse experiences with the drug, providing the FDA with updated safety and efficacy information, drug sampling and distribution requirements, complying with certain electronic records and signature requirements, and complying with FDA promotion and advertising requirements. The FDA strictly regulates labeling, advertising, promotion and other types of information on products that are placed on the market and imposes requirements and restrictions on drug manufacturers, such as those related to direct-to-consumer advertising, the prohibition on promoting products for uses or in patient populations that are not described in the product’s approved labeling (known as “off-label use”), industry-sponsored scientific and educational activities, and promotional activities involving the internet. Discovery of previously unknown problems or the failure to comply with the applicable regulatory requirements may result in restrictions on the marketing of a product or withdrawal of the product from the market, as well as possible civil or criminal sanctions. Failure to comply with the applicable U.S. requirements at any time during the product development process, approval process or after approval, may subject an applicant or manufacturer to administrative or judicial civil or criminal sanctions and adverse publicity. FDA sanctions could include refusal to approve pending applications, withdrawal of an approval, clinical holds on post-approval clinical trials, warning or untitled letters, product recalls, product seizures, total or partial suspension of production or distribution, injunctions, fines, refusals of government contracts, mandated corrective advertising or communications with doctors, debarment, restitution, disgorgement of profits, or civil or criminal penalties.

U.S. Marketing Exclusivity

Market exclusivity provisions under the FDCA can delay the submission or the approval of certain marketing applications. The FDCA provides a five-year period of non-patent marketing exclusivity within the United States to the first applicant to obtain approval of an NDA for a new chemical entity (NCE). A drug is a new chemical entity if the FDA has not previously approved any other drug containing the same active moiety, which is the molecule or ion responsible for the action of the drug substance. During the exclusivity period, the FDA may not approve or even accept for review an abbreviated new drug application (ANDA), or an NDA submitted under Section 505(b)(2) of the FDCA, or 505(b)(2) NDA, submitted by another company for another drug that contains the same active moiety. However, an application may be submitted after four years if it contains a certification of patent invalidity or non-infringement to one of the patents listed with the FDA by the NCE NDA holder.

The FDCA alternatively provides three years of marketing exclusivity for a change to a previously approved drug, such as a new indication or condition of use, submitted in an NDA, or supplement to an existing NDA, if one or more new clinical investigations, other than bioavailability or bioequivalence studies, that were conducted or sponsored by the applicant are deemed by the FDA to be essential to the approval of the application. This three-year exclusivity covers only the modification for which the drug received approval on the basis of the new clinical investigations and does not prohibit the FDA from approving ANDAs or 505(b)(2) NDAs for drugs containing the active agent for the original indication or condition of use.

Five-year and three-year exclusivity will not delay the submission or approval of a full NDA. However, an applicant submitting a full NDA would be required to conduct or obtain a right of reference to all of the preclinical studies and adequate and well-controlled clinical trials necessary to demonstrate safety and effectiveness.

Other types of non-patent exclusivity include seven-year orphan drug exclusivity and six-month pediatric exclusivity (each discussed above).

FDA Regulation of Companion Diagnostics

We are collaborating or expect to collaborate with strategic partners or CMOs to manufacture and supply in vitro diagnostics to identify patients with biomarkers associated with the targeted therapeutics we are developing. These diagnostics, often referred to as companion diagnostics, are regulated as medical devices. In the United States, the FDCA and its implementing regulations, and other federal and state statutes and regulations govern, among other things, medical device design and development, preclinical and clinical testing, premarket clearance or approval, registration and listing, manufacturing, labeling, storage, advertising and promotion, sales and distribution, export and import, and post-market surveillance.

Under the FDCA, medical devices are classified into one of three classes – Class I, Class II or Class III – depending on the degree of risk associated with each medical device and the extent of control needed to provide reasonable assurances with respect to safety and effectiveness. Class I devices are those for which safety and effectiveness can be reasonably assured by adherence to a set of regulations, referred to as General Controls, which require compliance with the applicable portions of the FDA’s Quality Management System Regulation (QMSR), facility registration and product listing, reporting of AEs and malfunctions, and appropriate, truthful and non-misleading labeling and promotional materials. Class II devices are those that are subject to General Controls, as well as Special Controls, which can include performance standards, guidelines and postmarket surveillance. Most Class II devices are subject to premarket review and clearance by the FDA under Section 510(k) of the FDCA. Under the 510(k) process, the manufacturer must submit to the FDA a premarket notification, demonstrating that the device is “substantially equivalent” to a predicate device. To be “substantially equivalent,” the proposed device must have the same intended use as the predicate device, and either have the same technological characteristics as the predicate device or have different technological characteristics that do not raise different questions of safety or effectiveness than the predicate device. Class III devices include devices deemed by the FDA to pose the greatest risk such as life-supporting or life-sustaining devices, or implantable devices, in addition to new devices deemed not substantially equivalent following the 510(k) process. The safety and effectiveness of Class III devices cannot be reasonably assured solely by General Controls and Special Controls. Therefore, these devices are generally subject to the premarket approval (PMA), application process, which is generally more costly and time-consuming than the 510(k) process.

Alternatively, a device might be the subject of a de novo classification request, which seeks marketing authorization and reclassification as a lower-risk Class I or Class II device for a new device that otherwise would automatically be regulated as a Class III device requiring a PMA approval. Specifically, medical device types that the FDA has not previously classified as Class I, II or III are automatically classified into Class III regardless of the level of risk they pose. The Food and Drug Administration Modernization Act of 1997 established a new route to market for low to moderate risk medical devices that are automatically placed into Class III due to the absence of a predicate device, called the “Request for Evaluation of Automatic Class III Designation,” or the de novo classification procedure. This procedure allows a manufacturer whose novel device is automatically classified into Class III to request down-classification of its medical device into Class I or Class II on the basis that the device presents low or moderate risk, rather than requiring the submission and approval of a PMA application.

If the use of a companion diagnostic is essential to the safe and effective use of a drug product, then the FDA generally will require approval or clearance of the diagnostic contemporaneously with the approval of the therapeutic product. In July 2014, the FDA issued a final guidance document addressing the development and approval process for in vitro companion diagnostic devices. According to the guidance, for novel product candidates such as ours, a companion diagnostic device and its corresponding drug candidate should be approved or cleared contemporaneously by the FDA for the use indicated in the therapeutic product labeling. The guidance also explains that a companion diagnostic device used to make treatment decisions in clinical trials of a drug generally will be considered an investigational device, unless it is employed for an intended use for which the device is already approved or cleared. If used to make critical treatment decisions, such as patient selection, the diagnostic device generally will be considered a significant risk device under the FDA’s Investigational Device Exemption (IDE) regulations. Thus, the sponsor of the diagnostic device will be required to submit an IDE application for clinical testing of the device and comply with the applicable IDE requirements. According to the guidance, if a diagnostic device and a drug are to be studied together to support their respective approvals, both products can be studied in the same investigational study, if the study meets both the requirements of the IDE regulations and the IND regulations. The guidance provides that depending on the details of the study plan and subjects, a sponsor may seek to submit an IND alone, or both an IND and an IDE. In July 2016, the FDA issued a draft guidance document intended to further assist sponsors of therapeutic products and sponsors of in vitro companion diagnostic devices on issues related to co-development of these products. In December 2018, the FDA issued another draft guidance document to facilitate class labeling on in vitro companion diagnostic devices for oncology therapeutic products, under which a companion diagnostic’s labeling may identify a specific group or class of therapeutic products, rather than specific products, where scientifically appropriate.

The FDA generally requires sponsors developing companion diagnostics intended to select patients who will respond to a specific cancer treatment to obtain approval of a PMA for that diagnostic contemporaneously with approval of the therapeutic, though 510(k) clearance or de novo classification are also possible. The FDA’s review of an in vitro companion diagnostic in conjunction with its review of a cancer therapeutic involves coordination between the FDA’s Center for Drug Evaluation and Research and the FDA’s Center for Devices and Radiological Health. The PMA process, including the gathering of clinical and preclinical data and the submission to and review by the FDA, can take several years or longer than the 510(k) or de novo processes. PMAs must generally include the results from extensive preclinical and adequate and

well-controlled clinical trials to establish the safety and effectiveness of the device for each indication for which FDA approval is sought. In particular, for a diagnostic, the applicant must demonstrate that the diagnostic produces reproducible results when the same sample is tested multiple times by multiple users at multiple laboratories. As part of the PMA review, the FDA will typically inspect the manufacturer’s facilities for compliance with the QMSR, which imposes elaborate testing, control, documentation and other quality assurance requirements.

If the FDA evaluations of both the PMA application and the manufacturing facilities are favorable, the FDA will either issue an approval letter or an approvable letter, which usually contains a number of conditions that must be met in order to secure the final approval of the PMA, such as changes in labeling, or specific additional information, such as submission of final labeling, in order to secure final approval of the PMA. If the FDA concludes that the applicable criteria have been met, the FDA will issue a PMA for the approved indications, which can be more limited than those originally sought by the applicant. The PMA can include post-approval conditions that the FDA believes necessary to ensure the safety and effectiveness of the device, including, among other things, restrictions on labeling, promotion, sale and distribution.

If the FDA’s evaluation of the PMA or manufacturing facilities is not favorable, the FDA will deny approval of the PMA or issue a not approvable letter. A not approvable letter will outline the deficiencies in the application and, where practical, will identify what is necessary to make the PMA approvable. The FDA may also determine that additional clinical trials are necessary, in which case the PMA approval may be delayed for several months or years while the clinical trials are conducted and then the data submitted in an amendment to the PMA. Once granted, PMA approval may be withdrawn by the FDA if compliance with post approval requirements, conditions of approval or other regulatory standards is not maintained or problems are identified following initial marketing. PMA approval is not guaranteed, and the FDA may ultimately respond to a PMA submission with a not approvable determination based on deficiencies in the application and require additional clinical trials or other data that may be expensive and time-consuming to generate and that can substantially delay approval.

If a companion diagnostic is the subject of a de novo classification request in lieu of a PMA, the FDA is required to classify the device within 120 days following receipt of the de novo submission. If the manufacturer seeks reclassification into Class II, the manufacturer must include a draft proposal for special controls sufficient to ensure a reasonable assurance of the safety and effectiveness of the medical device. The FDA may reject the reclassification petition if it identifies a legally marketed predicate device that would be appropriate for a 510(k) or determines that the device is not low to moderate risk or that general controls would be inadequate to control the risks and special controls cannot be developed. If the de novo request is granted, the new device may be legally marketed (in compliance with applicable regulatory controls), a new classification regulation for the device type will be established, and the device may serve as a predicate device for 510(k) submissions for future devices of the same type.

After a device is placed on the market, it remains subject to significant regulatory requirements. Medical devices may be marketed only for the uses and indications for which they are cleared or approved. Device manufacturers must also establish registration and device listings with the FDA. A medical device manufacturer’s manufacturing processes and those of its suppliers are required to comply with the applicable portions of the QMSR, which cover the methods and documentation of the design, testing, production, processes, controls, quality assurance, labeling, packaging and shipping of medical devices. Domestic facility records and manufacturing processes are subject to periodic unscheduled inspections by the FDA. The FDA also may inspect foreign facilities that export products to the United States.

Regulation Outside the United States

To the extent that any of our product candidates, once approved, are sold in a foreign country, we would be subject to numerous and varying foreign laws and regulations regarding safety and efficacy and governing, among other things, clinical trials, marketing authorization (MA), commercial sales and distribution of our products, and may include, for instance, applicable post-marketing requirements, including safety surveillance, anti-fraud and abuse laws and implementation of corporate compliance programs and reporting of payments or other transfers of value to healthcare professionals. The foreign regulatory approval process includes all of the risks associated with FDA approval set forth above, as well as additional country-specific regulation.

Whether or not we obtain FDA approval for a product, we must obtain approval of a product by the comparable regulatory authorities of foreign countries before we can commence clinical trials or marketing of the product in those countries. Approval by one regulatory authority does not ensure approval by regulatory authorities in other jurisdictions. The approval process varies from country to country, can involve additional testing beyond that required by FDA, and may be longer or shorter than that required for FDA approval. The requirements governing the conduct of clinical trials, product licensing, pricing, promotion, and reimbursement vary greatly from country to country.

Non-clinical Studies and Clinical Trials

Similarly to the United States, the various phases of non-clinical and clinical research in the European Union (EU) are subject to significant regulatory controls.

Non-clinical studies are performed to demonstrate the health or environmental safety of new chemical or biological substances. Non-clinical (pharmaco-toxicological) studies must be conducted in compliance with the principles of good laboratory practice (GLP), as set forth in EU Directive 2004/10/EC (unless otherwise justified for certain particular medicinal products, e.g., radio-pharmaceutical precursors for radio-labeling purposes). In particular, non-clinical studies, both in vitro and in vivo, must be planned, performed, monitored, recorded, reported and archived in accordance with the GLP principles, which define a set of rules and criteria for a quality system for the organizational process and the conditions for non-clinical studies. These GLP standards reflect the Organization for Economic Co-operation and Development requirements.

Clinical trials of medicinal products in the EU must be conducted in accordance with EU and national regulations and the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) guidelines on GCP, as well as the applicable regulatory requirements and the ethical principles that have their origin in the Declaration of Helsinki. If the sponsor of the clinical trial is not established within the EU, it must appoint an EU entity to act as its legal representative. The sponsor must take out a clinical trial insurance policy, and in most EU member states, the sponsor is liable to provide ‘no fault’ compensation to any study subject injured in the clinical trial.

The regulatory landscape related to clinical trials in the EU has been subject to recent changes. The EU Clinical Trials Regulation (CTR) which was adopted in April 2014 and repeals the EU Clinical Trials Directive, became applicable on January 31, 2022. Unlike directives, the CTR is directly applicable in all EU member states without the need for member states to further implement it into national law. The CTR notably harmonizes the assessment and supervision processes for clinical trials throughout the EU via a Clinical Trials Information System, which contains a centralized EU portal and database.

While the EU Clinical Trials Directive required a separate CTA to be submitted in each member state in which the clinical trial takes place, to both the competent national health authority and an independent ethics committee, much like the FDA and IRB respectively, the CTR introduces a centralized process and only requires the submission of a single application for multi-center trials. The CTR allows sponsors to make a single submission to both the competent authority and an ethics committee in each member state, leading to a single decision per member state. The CTA must include, among other things, a copy of the trial protocol and an investigational medicinal product dossier containing information about the manufacture and quality of the medicinal product under investigation. The assessment procedure of the CTA has been harmonized as well, including a joint assessment by all member states concerned, and a separate assessment by each member state with respect to specific requirements related to its own territory, including ethics rules. Each member state’s decision is communicated to the sponsor via the centralized EU portal. Once the CTA is approved, clinical study development may proceed.

The CTR transition period ended on January 31, 2025, and all clinical trials (and related applications) are now fully subject to the provisions of the CTR.

Medicines used in clinical trials must be manufactured in accordance with Good Manufacturing Practice (GMP). Other national and EU-wide regulatory requirements may also apply.

Marketing Authorization

In order to market our future products in the EU and many other foreign jurisdictions, we must obtain separate regulatory approvals. More concretely, in the EU, medicinal product candidates can only be commercialized after obtaining a MA. To obtain regulatory approval of a product candidate under EU regulatory systems, we must submit a MA application (MAA). There are two types of MAs:

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“Centralized MAs” are issued by the European Commission through the centralized procedure based on the opinion of the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA), and are valid throughout the entire territory of the EU. The centralized procedure is mandatory for certain types of medicinal products, such as (i) medicinal products derived from biotechnological processes, (ii) designated orphan medicinal products, (iii) advanced therapy medicinal products (ATMPs) (such as gene therapy, somatic cell therapy and tissue engineered products) and (iv) medicinal products containing a new active substance indicated for the treatment of certain diseases, such as AIDS/HIV, cancer, neurodegenerative disorders, diabetes, auto-immune and viral diseases and other immune dysfunctions. The centralized procedure is optional for products containing a new active substance not yet authorized in the EEA, or for products that constitute a significant therapeutic, scientific or technical innovation or which are in the interest of public health in the EU; and

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“National MAs” are issued by the competent authorities of the EU member states, only cover their respective territory, and are available for products not falling within the mandatory scope of the centralized procedure. Where a product has already been authorized for marketing in an EU member states, this national MA can be recognized in another member state through the mutual recognition procedure. If the product has not received a national MA in any member state at the time of application, it can be approved simultaneously in various member state through the decentralized procedure. Under the decentralized procedure an identical dossier is submitted to the competent authorities of each of the member states in which the MA is sought, one of which is selected by the applicant as the reference member state.

Under the centralized procedure the maximum timeframe for the evaluation of a MAA by the EMA is 210 days, excluding clock stops.

In exceptional cases, the CHMP might perform an accelerated review of a MAA in no more than 150 days (not including clock stops). Innovative products that target an unmet medical need and are expected to be of major public health interest may be eligible for a number of expedited development and review programs, such as the PRIority MEdicines (PRIME), scheme, which provides incentives similar to the breakthrough therapy designation in the United States. In March 2016, the EMA launched an initiative, the PRIME scheme, a voluntary scheme aimed at enhancing the EMA’s support for the development of medicines that target unmet medical needs. It is based on increased interaction and early dialogue with companies developing promising medicines, to optimize their product development plans and speed up their evaluation to help them reach patients earlier. Product developers that benefit from PRIME designation can expect to be eligible for accelerated assessment but this is not guaranteed. Many benefits accrue to sponsors of product candidates with PRIME designation, including but not limited to, early and proactive regulatory dialogue with the EMA, frequent discussions on clinical trial designs and other development program elements, and accelerated MAA assessment once a dossier has been submitted. Importantly, a dedicated contact and rapporteur from the CHMP is appointed early in the PRIME scheme facilitating increased understanding of the product at EMA’s committee level. An initial meeting initiates these relationships and includes a team of multidisciplinary experts at the EMA to provide guidance on the overall development and regulatory strategies.

Moreover, in the EU, a “conditional” MA may be granted in cases where all the required safety and efficacy data are not yet available. The conditional MA is subject to conditions to be fulfilled for generating the missing data or ensuring increased safety measures. It is valid for one year and has to be renewed annually until fulfillment of all the conditions. Once the pending studies are provided, it can become a “standard” MA. However, if the conditions are not fulfilled within the timeframe set by the EMA, the MA ceases to be renewed. Furthermore, MA may also be granted “under exceptional circumstances” when the applicant can show that it is unable to provide comprehensive data on the efficacy and safety under normal conditions of use even after the product has been authorized and subject to specific procedures being introduced. This may arise in particular when the intended indications are very rare and, in the present state of scientific knowledge, it is not possible to provide comprehensive information data on the efficacy and safety under normal conditions of use even after the product has been authorized and subject to specific procedures being introduced. This may arise in particular when the intended indications are very rare and, in the present state of scientific knowledge, it is not possible to provide comprehensive information, or when generating data may be contrary to generally accepted ethical principles. This MA is close to the conditional MA as it is reserved to medicinal products to be approved for severe diseases or unmet medical needs and the applicant does not hold the complete data set legally required for the grant of a MA. However, unlike the conditional MA, the applicant does not have to provide the missing data and will never have to. Although the MA “under exceptional circumstances” is granted definitively, the risk-benefit balance of the medicinal product is reviewed annually and the MA is withdrawn in case the risk-benefit ratio is no longer favorable.

Under the above described procedures, before granting the MA, the EMA or the competent authorities of the EU member states make an assessment of the risk-benefit balance of the product on the basis of scientific criteria concerning its quality, safety and efficacy. MAs have an initial duration of five years. After these five years, the authorization may be renewed on the basis of a reevaluation of the risk-benefit balance.

Data and Marketing Exclusivity

In the EU, new products authorized for marketing, or reference products, generally receive eight years of data exclusivity and an additional two years of market exclusivity upon MA. If granted, the data exclusivity period prevents generic or biosimilar applicants from relying on the preclinical and clinical trial data contained in the dossier of the reference product when applying for a generic or biosimilar MA in the EU during a period of eight years from the date on which the reference product was first authorized in the EU. The market exclusivity period prevents a successful generic or biosimilar applicant from commercializing its product in the EU until 10 years have elapsed from the initial MA of the reference product in the EU. The overall 10-year market exclusivity period can be extended to a maximum of eleven years if, during the first eight

years of those 10 years, the MA holder obtains an authorization for one or more new therapeutic indications which, during the scientific evaluation prior to their authorization, are held to bring a significant clinical benefit in comparison with existing therapies. However, there is no guarantee that a product will be considered by the EU’s regulatory authorities to be a new chemical or biological entity, and products may not qualify for data exclusivity.

Pediatric Development

In the EEA, MAAs for new medicinal products have to include the results of studies conducted in the pediatric population, in compliance with a pediatric investigation plan (PIP) agreed with the EMA’s Pediatric Committee (PDCO). The PIP sets out the timing and measures proposed to generate data to support a pediatric indication of the drug for which MA is being sought. The PDCO can grant a deferral of the obligation to implement some or all of the measures of the PIP until there are sufficient data to demonstrate the efficacy and safety of the product in adults. Further, the obligation to provide pediatric clinical trial data can be waived by the PDCO when these data are not needed or appropriate because the product is likely to be ineffective or unsafe in children, the disease or condition for which the product is intended occurs only in adult populations, or when the product does not represent a significant therapeutic benefit over existing treatments for pediatric patients. Once the MA is obtained in all EU member states and study results are included in the product information, even when negative, the product is eligible for six months’ supplementary protection certificate extension (if any is in effect at the time of approval) or, in the case of orphan pharmaceutical products, a two year extension of the orphan market exclusivity is granted.

Orphan Medicinal Products

The criteria for designating an “orphan medicinal product” in the EU are similar in principle to those in the United States. A medicinal product can be designated as an orphan if its sponsor can establish that: (1) the product is intended for the diagnosis, prevention or treatment of a life-threatening or chronically debilitating condition; (2) either (a) such condition affects not more than five in ten thousand persons in the EU when the application is made, or (b) the product, without the benefits derived from the orphan status, would not generate sufficient return to justify the necessary investment; and (3) there exists no satisfactory method of diagnosis, prevention or treatment of the condition in question that has been authorized for marketing in the EU or, if such method exists, the drug will be of significant benefit to those affected by that condition.

In the EU, an application for designation as an orphan product can be made any time prior to the filing of a MAA. An EU orphan designation entitles a party to incentives such as reduction of fees or fee waivers, protocol assistance, and access to the centralized procedure. Upon grant of a MA, orphan medicinal products are entitled to a ten-year period of market exclusivity for the approved indication. During this market exclusivity period, competent authorities cannot accept another MAA, or grant a MA, or accept an application to extend a MA for a similar medicinal product for the same indication. The period of market exclusivity is extended by two years for orphan medicines that have also complied with an agreed PIP. No extension to any supplementary protection certificate can be granted on the basis of pediatric studies for orphan indications. Orphan designation does not convey any advantage in, or shorten the duration of, the regulatory review and approval process.

The orphan exclusivity period may, however, be reduced to six years if, at the end of the fifth year, it is established that the product no longer meets the criteria for orphan designation, for example because the product is sufficiently profitable not to justify market exclusivity, or where the prevalence of the condition has increased above the threshold. Additionally, MA may be granted to a similar product for the same indication at any time if (i) the applicant consents to a second orphan medicinal product application, (ii) the applicant cannot supply sufficient quantities of the product, or (iii) the second applicant can establish that its product, although similar, is safer, more effective or otherwise clinically superior.

The aforementioned EU rules are generally applicable in the European Economic Area (EEA), which consists of the 27 EU member states plus Norway, Liechtenstein and Iceland.

Failure to comply with EU and member state laws that apply to the conduct of clinical trials, manufacturing approval, MA of medicinal products and marketing of such products, both before and after grant of the MA, manufacturing of pharmaceutical products, statutory health insurance, bribery and anti-corruption or with other applicable regulatory requirements may result in administrative, civil or criminal penalties. These penalties could include delays or refusal to authorize the conduct of clinical trials, or to grant MA, product withdrawals and recalls, product seizures, suspension, withdrawal or variation of the MA, total or partial suspension of production, distribution, manufacturing or clinical trials, operating restrictions, injunctions, suspension of licenses, fines and criminal penalties.

Regulation of Companion Diagnostics

In the EU, in vitro diagnostic medical devices (IVD MDs), were regulated by the EU Directive on in vitro diagnostic medical devices (Directive No. 98/79/EC, as amended) (IVDD), which regulated the placing on the market, the CE marking, the essential requirements, the conformity assessment procedures, the registration obligations for manufacturers and devices, as well as the vigilance procedure. IVD MDs had to comply with the requirements provided for in the IVDD, and with further requirements implemented at national level (as the case may be).

The regulation of companion diagnostics is subject to further requirements since Regulation (EU) No 2017/746 (IVDR) became applicable on May 26, 2022 but there is a tiered system extending the grace period for many devices (depending on their risk classification) before they have to be fully compliant with the Regulation. The IVDR introduced a new classification system for companion diagnostics which are now specifically defined as diagnostic tests that support the safe and effective use of a specific medicinal product, by identifying patients that are suitable or unsuitable for treatment. Companion diagnostics will have to undergo a conformity assessment by a notified body. Before it can issue an EU certificate, the notified body must seek a scientific opinion from the EMA on the suitability of the companion diagnostic to the medicinal product concerned if the medicinal product falls exclusively within the scope of the centralized procedure for the authorization of medicines, or the medicinal product is already authorized through the centralized procedure, or a MAA for the medicinal product has been submitted through the centralized procedure. For other substances, the notified body can seek the opinion from a national competent authorities or the EMA.

The aforementioned EU rules are generally applicable in the EEA.

Healthcare Reform

In the United States and certain foreign jurisdictions, there have been, and we expect there will continue to be, a number of legislative and regulatory changes to the healthcare system that could affect our future results of operations as we begin to directly commercialize our products. In March 2010, the Patient Protection and Affordable Care Act (ACA) was signed into law which substantially changed the way healthcare is financed by both governmental and private insurers in the United States and significantly affected the pharmaceutical industry. The ACA contains a number of provisions, including those governing enrollment in federal healthcare programs, reimbursement adjustments and fraud and abuse changes. Additionally, the ACA increases the minimum level of Medicaid rebates payable by manufacturers of brand name drugs from 15.1% to 23.1%; requires collection of rebates for drugs paid by Medicaid managed care organizations; imposes a non-deductible annual fee on pharmaceutical manufacturers or importers who sell “branded prescription drugs” to specified federal government programs, implemented a new methodology by which rebates owed by manufacturers under the Medicaid Drug Rebate Program are calculated for drugs that are inhaled, infused, instilled, implanted, or injected, expands of eligibility criteria for Medicaid programs, creates a new Patient-Centered Outcomes Research Institute to oversee, identify priorities in, and conduct comparative clinical effectiveness research, along with funding for such research and establishes a Center for Medicare and Medicaid Innovation at CMS to test innovative payment and service delivery models to lower Medicare and Medicaid spending, potentially including prescription drug spending.

Since its enactment, there have been judicial, executive and Congressional challenges to certain aspects of the ACA. On June 17, 2021, the U.S. Supreme Court dismissed the most recent judicial challenge to the ACA brought by several states without specifically ruling on the constitutionality of the ACA.

Other legislative changes have been proposed and adopted since the ACA was enacted, including aggregate reductions of Medicare payments to providers, which will remain in effect through 2032, with the exception of a temporary suspension from May 1, 2020 through March 31, 2022, unless additional Congressional action is taken. In addition, on March 11, 2021, the American Rescue Plan Act of 2021 was signed into law, which eliminates the statutory Medicaid drug rebate cap, beginning January 1, 2024. The rebate was previously capped at 100% of a drug’s average manufacturer price.

Moreover, there has recently been heightened governmental scrutiny over the manner in which manufacturers set prices for their marketed products, which has resulted in several Congressional inquiries and proposed and enacted legislation designed, among other things, to bring more transparency to product pricing, review the relationship between pricing and manufacturer patient programs and reform government program reimbursement methodologies for drug products. On August 16, 2022, the Inflation Reduction Act of 2022 (IRA) was signed into law. Among other things, the IRA requires manufacturers of certain drugs to engage in price negotiations with Medicare, imposes rebates under Medicare Part B and Medicare Part D to penalize price increases that outpace inflation (first due in 2023), and replaces the Part D coverage gap discount program with a new discounting program (which began in 2025). The IRA permits the Secretary of the Department of Health and Human Services to implement many of these provisions through guidance, as opposed to regulation, for the initial years. CMS has published the negotiated prices for the initial ten drugs, which went into effect in 2026, and the subsequent 15 drugs, which will first be effective in 2027, although the drug price negotiation program is currently subject to legal challenges. For that and other reasons, it is currently unclear how the IRA will be effectuated.

The One Big Beautiful Bill Act, which was enacted in July 2025, imposes significant reductions in the funding of the Medicaid program. Such reductions are expected to decrease the number of persons enrolled in Medicaid and reduce the services covered by Medicaid, which could adversely affect our sales of any product candidate that we commercialize.

The Trump administration is pursuing a two-fold strategy to reduce drug costs in the U.S. While it is unclear whether and how the Trump proposals will be implemented, the Trump policies are likely to have a negative impact on the pharmaceutical industry and on our ability to receive adequate revenues for any product candidate that we commercialize. On the one hand, President Trump has threatened to impose significant tariffs on pharmaceutical manufacturers that do not adopt pricing policies such as most favored nation pricing, which would tie the price for drugs in the U.S. to the lowest price in a group of other countries. In response, multiple manufacturers have reportedly entered into confidential pricing agreements with the federal government. On the other hand, the Trump administration is pursuing traditional regulatory pathways to impose drug pricing policies, and published two proposed regulations in December 2025, referred to as Globe and Guard. If finalized, these regulations would implement mandatory payment models under which manufacturers of eligible drugs would be required to pay rebates to the federal government on a portion of the units of their drugs that are reimbursed by Medicare, with the rebate amount based on most favored nation pricing. Imposing a rebate in the U.S. that is based on drug prices outside the U.S. would mark a drastic and unprecedented shift in the U.S. pharmaceutical market, and while the impact of the Globe and Guard proposed regulations, if finalized, cannot yet be determined, it is likely to be significant. Even if such initiatives are modified, delayed, or challenged, the uncertainty surrounding these policy proposals may impair our ability to forecast revenues, plan commercial launch activities, negotiate favorable contracts with payors, or make investment decisions regarding manufacturing scale-up and commercialization infrastructure.

Individual states in the United States have also become increasingly active in implementing regulations designed to control pharmaceutical product pricing, including price or patient reimbursement constraints, discounts, restrictions on certain product access, marketing cost disclosure, drug price reporting and other transparency measures. Some U.S. states have enacted legislation creating so-called prescription drug affordability boards, and to date one state has used its prescription drug affordability board to impose an upper payment limit. Some states are also seeking to implement general, across the board price caps for pharmaceuticals, or are seeking to regulate drug distribution. Some measures are also designed to encourage importation from other countries. These types of initiatives may result in additional reductions in Medicare, Medicaid, and other healthcare funding, and may otherwise affect the prices we may obtain or the frequency with which any drug candidate that we commercialize is prescribed or used.

We expect that additional state and federal healthcare reform measures will be adopted in the future, any of which could limit the amounts that federal and state governments will pay for healthcare product candidates and services, which could result in reduced demand for our product candidates once approved or additional pricing pressures.

In the EU, similar developments may affect our ability to profitably commercialize our products, if approved. On December 13, 2021, Regulation No 2021/2282 on Health Technology Assessment (HTA), amending Directive 2011/24/EU, was adopted. The Regulation entered into force in January 2022 and has been applicable since January 2025, with phased implementation based on the type of product, i.e. oncology and advanced therapy medicinal products as of 2025, orphan medicinal products as of 2028, and all other medicinal products by 2030. The Regulation intends to boost cooperation among EU member states in assessing health technologies, including new medicinal products, as well as certain high-risk medical devices, and provide the basis for cooperation at the EU level for joint clinical assessments in these areas. It will permit EU member states to use common HTA tools, methodologies, and procedures across the EU, working together in four main areas, including joint clinical assessment of the innovative health technologies with the highest potential impact for patients, joint scientific consultations whereby developers can seek advice from HTA authorities, identification of emerging health technologies to identify promising technologies early, and continuing voluntary cooperation in other areas. Individual EU member states will continue to be responsible for assessing non-clinical (e.g., economic, social, ethical) aspects of health technology, and making decisions on pricing and reimbursement.

Other Healthcare Laws

Pharmaceutical companies are subject to additional healthcare regulation and enforcement by the federal government and by authorities in the states and foreign jurisdictions in which they conduct their business. Such laws include, without limitation, state and federal anti-kickback, fraud and abuse, false claims, and transparency laws and regulations with respect to drug pricing and payments and other transfers of value to physicians and other healthcare providers, as well as similar foreign laws in the jurisdictions outside the United States. If their operations are found to be in violation of any of such laws or any other governmental regulations that apply, they may be subject to penalties, including, without limitation, civil and criminal penalties, damages, fines, additional reporting obligations and oversight if we become subject to a corporate integrity agreement or other agreement to resolve allegations of non-compliance with these laws, the curtailment or restructuring of operations, exclusion from participation in governmental healthcare programs and imprisonment.

Data Privacy and Security Laws

Pharmaceutical companies may be subject to numerous federal, state, and foreign laws, regulations and standards which govern the collection, use, disclosure and protection of health-related and other personal information, and could apply now or in the future to our operations or the operations of our partners. In the United States, numerous federal and state laws and regulations, including data breach notification laws, health information privacy and security laws and consumer protection laws and regulations govern the collection, use, disclosure, and protection of health-related and other personal information. In addition, certain foreign laws govern the privacy and security of personal data, including health-related data. Privacy and security laws, regulations, and other obligations are constantly evolving, may conflict with each other to complicate compliance efforts, and can result in investigations, proceedings, or actions that lead to significant civil and/or criminal penalties and restrictions on data processing.

Coverage and Reimbursement

Sales of any product depend, in part, on the extent to which such product will be covered by third-party payors, such as federal, state and foreign government healthcare programs, commercial insurance and managed healthcare organizations, and the level of reimbursement for such product by third-party payors. Decisions regarding the extent of coverage and amount of reimbursement to be provided are made on a plan-by-plan basis. These third-party payors are increasingly reducing reimbursements for medical products, drugs and services. In addition, the U.S. government, state legislatures and foreign governments have continued implementing cost-containment programs, including price controls, restrictions on coverage and reimbursement and requirements for substitution of generic products. Adoption of price controls and cost-containment measures, and adoption of more restrictive policies in jurisdictions with existing controls and measures, could further limit sales of any product. Decreases in third-party reimbursement for any product or a decision by a third-party payor not to cover a product could reduce physician usage and patient demand for the product and also have a material adverse effect on sales.

In addition, in many countries, the proposed pricing for a drug must be approved before it may be lawfully marketed. The requirements governing drug pricing and reimbursement vary widely from country to country. In the EU, governments influence the price of products through their pricing and reimbursement rules and control of national healthcare systems that fund a large part of the cost of those products to consumers. Member states are free to restrict the range of pharmaceutical products for which their national health insurance systems provide reimbursement, and to control the prices and reimbursement levels of pharmaceutical products for human use. Some jurisdictions operate positive and negative list systems under which products may only be marketed once a reimbursement price has been agreed to by the government. Member states may approve a specific price or level of reimbursement for the pharmaceutical product, or alternatively adopt a system of direct or indirect controls on the profitability of the company responsible for placing the pharmaceutical product on the market, including volume-based arrangements, caps and reference pricing mechanisms. To obtain reimbursement or pricing approval, some of these countries may require the completion of clinical trials that compare the cost effectiveness of a particular product to currently available therapies. Other member states allow companies to fix their own prices for medicines, but monitor and control company profits. There can be no assurance that any country that has price controls or reimbursement limitations for pharmaceutical products will allow favorable reimbursement and pricing arrangements for any of our products. The downward pressure on healthcare costs in general, particularly prescription products, has become very intense. As a result, increasingly high barriers are being erected to the entry of new products. In addition, in some countries, cross border imports from low-priced markets exert a commercial pressure on pricing within a country.

We may face competition for our product candidates from lower-priced products in foreign countries that have placed price controls on pharmaceutical products. In addition, there may be importation of foreign products that compete with our own products, which could negatively impact our profitability. Furthermore, there can be no assurance that our products will be considered medically reasonable and necessary for a specific indication, that our products will be considered cost-effective by third-party payors, that an adequate level of reimbursement will be established even if coverage is available or that the third-party payors’ reimbursement policies will not adversely affect our ability to sell our products profitably.

Human Capital

At IDEAYA, we view our employees as among our most valuable assets. Our ability to hire and retain highly skilled professionals remains an important element to our success in discovering and developing targeted therapeutics. Our employees are at the heart of our values of passionate commitment, fearless innovation, courageous integrity, respectful teamwork, objective decision-making and empowered accountability. We offer our employees a challenging work

environment, ongoing skills development, attractive career advancement, and a culture that rewards entrepreneurial initiative and exceptional execution.

We have assembled a team of cancer biologists, drug discovery chemists, translational biologists and drug development professionals with broad experience at leading oncology organizations. Our team is led by our Chief Executive Officer, Yujiro S Hata. We are also guided by a renowned scientific advisory board made up of key scientific and clinical thought leaders.

We established an internal human resources department as part of our commitment to our human resources programs and our employee work experience, and we seek to hire and retain a highly qualified workforce in compliance with applicable federal and other laws and regulations. We draw from the largest pools of talent to help find the best people for our company. We believe the variety of experiences and perspectives that our employees bring to their work every day makes us stronger and more successful. As of December 31, 2025, females make up 48% of our workforce, 23% of our executive team, and 29% of our board of directors.

As of December 31, 2025, we had a total of 145 employees. Of these employees, 112 were primarily engaged in research and development activities and 33 were primarily engaged in general and administrative activities. Of our total employees, 110 hold biology, chemistry or other relevant scientific degrees, including 55 Ph.D.s. None of our employees are represented by labor unions or covered by collective bargaining agreements. We consider our relationship with our employees to be good.

Corporate Information

We were founded in June 2015 as a Delaware corporation. Our principal executive offices are located at 5000 Shoreline Court, Suite 300, South San Francisco, California 94080, and our telephone number is (650) 443-6209. Our website address is www.ideayabio.com.

We file electronically with the Securities and Exchange Commission (SEC) our annual reports on Form 10-K, quarterly reports on Form 10-Q and current reports on Form 8-K pursuant to Section 13(a) or 15(d) of the Securities Exchange Act of 1934, as amended. Our SEC filings are available to the public on the SEC’s website at www.sec.gov. At our corporate website, www.ideayabio.com, we make available free of charge a variety of information for investors, including copies of these reports, and any amendments to these reports, as soon as reasonably practicable after we electronically file such material with, or furnish it to, the SEC. The information on, or that can be accessed through, our website is not part of this report and is not incorporated by reference herein. We have included our website address as an inactive textual reference only. We also use our website as a means of disclosing material non-public information and for complying with our disclosure obligations under Regulation FD.

We use IDEAYA Biosciences, Inc.®, the IDEAYA logo, and other marks as trademarks in the United States and other countries. This Annual Report on Form 10-K contains references to our trademarks and service marks and to those belonging to other entities. Solely for convenience, trademarks and trade names referred to in this Annual Report on Form 10-K, including logos, artwork and other visual displays, may appear without the ® or ™ symbols, but such references are not intended to indicate in any way that we will not assert, to the fullest extent under applicable law, our rights or the rights of the applicable licensor to these trademarks and trade names. We do not intend our use or display of other entities’ trade names, trademarks or service marks to imply a relationship with, or endorsement or sponsorship of us by any other entity.