Crizotinib

As biomarker testing and the demand for tumor-agnostic therapies rise, ROZLYTREK can potentially target a specialized yet valuable market segment. While competition from other TRK inhibitors, such as larotrectinib (VITRAKVI), may influence growth, its ability to penetrate the CNS provides a distinct advantage. LAS VEGAS, March 12, 2025 /PRNewswire/ -- DelveInsight's " ROZLYTREK Market Size, Forecast, and Market Insight Report" highlights the details around ROZLYTREK, an inhibitor of the tropomyosin receptor tyrosine kinases (TRK) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1, and ALK with IC50 values of 0.1 to 2 nM. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of ROZLYTREK. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan]. Roche's ROZLYTREK (entrectinib) Overview ROZLYTREK is a tumor-agnostic therapy that introduces a novel approach to cancer treatment. Its active ingredient, entrectinib, inhibits tropomyosin receptor tyrosine kinases (TRKA, TRKB, and TRKC), which are encoded by the NTRK1, NTRK2, and NTRK3 genes. It also targets ROS1 and ALK, with IC50 values ranging from 0.1 to 2 nM, while showing weaker inhibition of JAK2 and TNK2 (IC50 > 5 nM). The primary active metabolite, M5, exhibits similar inhibitory activity against TRK, ROS1, and ALK. Fusion proteins involving TRK, ROS1, or ALK kinase domains can promote tumor growth by excessively activating downstream signaling pathways, leading to uncontrolled cell proliferation. Entrectinib has demonstrated both in vitro and in vivo efficacy in inhibiting cancer cell lines across multiple tumor types carrying NTRK, ROS1, or ALK fusions. Additionally, it achieves steady-state brain-to-plasma concentration ratios between 0.4 and 2.2 in animal studies (mice, rats, and dogs) and has shown anti-tumor effects in mice with intracranial tumors driven by TRKA and ALK. ROZLYTREK is an orally administered, once-daily treatment approved for NTRK fusion-positive solid tumors and ROS1-positive NSCLC in several countries, including Australia, Canada, the EU, Israel, Japan, New Zealand, South Korea, Taiwan, and the US, with additional regulatory reviews ongoing worldwide. The recommended ROZLYTREK dosage for ROS1-positive NSCLC is 600 mg once daily, with or without food, until disease progression or unacceptable toxicity. For NTRK fusion-positive solid tumors, the ROZLYTREK dosage guidelines are as follows: Adults and pediatric patients with a body surface area (BSA) of ≥1.51 m²: 600 mg once daily Pediatric patients older than 6 months: 300 mg/m² to a maximum of 600 mg Pediatric patients between 1 month and 6 months: 250 mg/m² once daily Learn more about ROZLYTREK projected market size for ROS1 NSCLC @ ROZLYTREK Market Potential Receptor Tyrosine Kinase (ROS1) is an essential transmembrane receptor protein that regulates key cellular functions such as apoptosis, survival, differentiation, proliferation, migration, and transformation. It plays a pivotal role in various cancers, including glioblastoma, colorectal cancer, gastric adenocarcinoma, inflammatory myofibroblastic tumor, ovarian cancer, angiosarcoma, and NSCLC. A ROS1 inhibitor is a drug designed to block the activity of abnormal ROS1 fusion proteins present in certain cancer cells. By inhibiting this protein, these inhibitors help restrict cancer cell growth and metastasis. As a type of targeted therapy, ROS1 inhibitors also act on multiple kinases, including Anaplastic Lymphoma Kinase (ALK) and Mesenchymal Epithelial Transition (MET), alongside ROS1. These inhibitors specifically target the kinase domain of ROS1, with conventional kinases classified into DFG-in (active, type I) and DFG-out (inactive, type II) based on their domain structure. For patients with stage IV ROS1-positive NSCLC, treatment with a ROS1 tyrosine kinase inhibitor (TKI) is recommended. ROS1 inhibitors have demonstrated remarkable efficacy in treating NSCLC, encompassing both approved therapies and emerging treatments under development. They have significantly advanced NSCLC management, establishing themselves as a crucial therapeutic approach. The current market for ROS1-positive NSCLC is largely dominated by TKIs such as XALKORI. According to DelveInsight's analysis, the market size for ROS1 inhibitors in NSCLC across the 7MM was valued at approximately USD 290 million in 2023, with the United States contributing the largest share. The market for ROS1 inhibitors is projected to experience substantial growth in the coming years. This expansion is driven by rising biomarker testing rates, a growing number of cancer diagnoses, increased awareness of ROS1 mutations, and the introduction of next-generation ROS1 TKIs. These advanced therapies offer improved CNS penetration and a broader range of coverage against ROS1 resistance mutations compared to first-generation TKIs. Discover more about the ROS1 inhibitors market in detail @ ROS1 Inhibitors Market Report Emerging Competitors of ROZLYTREK The promising ROS1 inhibitors in the pipeline that will give tough competition to Roche's ROZLYTREK include DOVBLERON (taletrectinib/AB-106/IBI-344) (Nuvation Bio/Innovent Biologics/Daiichi Sankyo/Nippon Kayaku), Zidesamtinib (NVL-520) (Nuvalent), ANS03 (Avistone Biotechnology), Zanidatamab (Jazz Pharmaceuticals), PT-112 (Promontory Therapeutics), and others. In December 2024, Nuvation Bio announced that the US FDA had granted the application Priority Review and assigned a Prescription Drug User Fee Act (PDUFA) goal date of June 2025. The company is preparing for a launch as early as mid-2025. To know more about the number of competing drugs in development, visit @ ROZLYTREK Market Positioning Compared to Other Drugs Key Milestones of ROZLYTREK In October 2023, the US FDA granted accelerated approval to ROZLYTREK in new oral pellet form for pediatric patients older than 1 month with solid tumors that have an NTRK gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory standard therapy. In August 2020, the EC granted conditional marketing authorization for ROZLYTREK for the treatment of adult and pediatric patients 12 years of age and older with solid tumors expressing an NTRK gene fusion, who have a disease that is locally advanced, metastatic, or where surgical resection is likely to result in severe morbidity, and who have not received a prior NTRK inhibitor, who have no satisfactory treatment options. The EC also approved ROZLYTREK for the treatment of adults with ROS1-positive, advanced NSCLC not previously treated with ROS1 inhibitors. In February 2020, Chugai obtained approval for an additional indication of ROZLYTREK for the treatment of ROS1 fusion-positive, unresectable, advanced, or metastatic NSCLC from the MHLW. In September 2019, Chugai Pharmaceutical announced the launch of ROZLYTREK 100 mg and 200 mg capsules, for the treatment of NTRK fusion-positive advanced or recurrent solid tumors. In August 2019, the US FDA approved ROZLYTREK to treat adults with ROS1-positive, metastatic NSCLC. The FDA has also granted accelerated approval to ROZLYTREK for the treatment of adult and pediatric patients 12 years of age and older with solid tumors that have an NTRK gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory alternative therapy. In June 2019, the MHLW approved ROZLYTREK for treating adult and pediatric patients with NTRK fusion-positive, advanced recurrent solid tumors. In February 2019, the US FDA issued a priority review designation letter to ROZLYTREK adult patients with metastatic NSCLC whose tumors are ROS1–positive. In December 2018, ROZLYTREK received ODD in Japan with the intended indication of NTRK fusion-positive, locally advanced, or metastatic solid tumors. In September 2018, ROZLYTREK received SAKIGAKE designation for the treatment of adult and pediatric patients with NTRK gene fusion-positive, locally advanced, or metastatic solid tumors who have progressed following prior therapies or have no acceptable standard therapies. In July 2018, Chugai entered into a license agreement with Roche for entrectinib. Under the terms of the agreement, Chugai obtains exclusive rights for the development and marketing of entrectinib in Japan and will make upfront and milestone payments to Roche. In December 2017, Roche and Ignyta entered a definitive merger agreement for Roche to fully acquire Ignyta for USD 27.00 per share in an all-cash transaction. In October 2017, ROZLYTREK was awarded PRIME status for treating NTRK fusion-positive, locally advanced, or metastatic solid tumors in adult and pediatric patients who have either progressed following prior therapies or have no acceptable standard therapy by EMA. In May 2017, ROZLYTREK was granted BTD for the treatment of NTRK fusion-positive, locally advanced, or metastatic solid tumors in adult and pediatric patients who have either progressed following prior therapies or who have no acceptable standard therapies by the US FDA. In February 2015, the US FDA granted ODD to ROZLYTREK for treating TrkA-positive, TrkB-positive, TrkC-positive, ROS1-positive or ALK-positive NSCLC. Discover how ROZLYTREK is shaping the ROS1 NSCLC treatment landscape @ Roche ROZLYTREK ROZLYTREK Market Dynamics ROZLYTREK competitive positioning in the market is driven by its tumor-agnostic approval, allowing it to cater to multiple rare cancers with a single therapy. The drug has gained regulatory approval in major markets, including the US, Europe, and Japan, benefiting from an increasing emphasis on biomarker-driven oncology treatments. Its key competitor, Bayer's VITRAKVI (larotrectinib), has a similar mechanism of action but differs in pharmacokinetics and tolerability, creating a nuanced competitive landscape. Market adoption of ROZLYTREK is influenced by the growing use of comprehensive genomic profiling (CGP) in oncology, which facilitates the identification of eligible patients with NTRK or ROS1 fusions. However, its commercial success is partially constrained by the rarity of these genetic alterations, which limits the addressable patient population. Additionally, the high cost of precision oncology therapies and reimbursement challenges in certain healthcare systems can impact uptake. Nonetheless, increasing awareness and advancements in diagnostic infrastructure are expected to support market growth. From a strategic perspective, Roche has leveraged partnerships and real-world evidence to expand the drug's adoption. The company is actively working on label expansions and combination strategies to maximize ROZLYTREK's commercial potential. Additionally, the growing use of next-generation sequencing (NGS) panels in routine cancer diagnostics may boost the identification rate of eligible patients, driving future market penetration. The competitive landscape could see further evolution with the potential entry of new TRK/ROS1 inhibitors, particularly next-generation agents designed to address resistance mutations. However, ROZLYTREK's strong clinical efficacy, broad tissue-agnostic approval, and Roche's global oncology expertise position it well in the precision medicine segment. As personalized oncology continues to gain traction, the drug's long-term success will depend on physician awareness, diagnostic advancements, and favorable pricing and reimbursement strategies. Dive deeper to get more insight into ROZLYTREK's strengths & weaknesses relative to competitors @ ROZLYTREK Market Drug Report Table of Contents Related Reports ROS1 Inhibitors Market ROS-1 Inhibitors Market Size, Target Population, Competitive Landscape & Market Forecast – 2034 report deliver an in-depth understanding of the market trends, market drivers, market barriers, and key ROS1 inhibitors companies, including AnHeart Therapeutics, Nuvalent, Bristol Myers Squibb, Genentech, Pfizer, among others. Non-small Cell Lung Cancer Market Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key NSCLC companies including Daiichi Sankyo, AstraZeneca, Gilead Sciences, BieGene, AbbVie, Roche, Merck, Novartis, Pfizer, Takeda Pharmaceuticals, Eli Lilly, BerGenBio, GlaxoSmithKline, Duality biologics, among others. Non-small Cell Lung Cancer Pipeline Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key non-small cell lung cancer companies, including BridgeBio Pharma, Daiichi Sankyo, EMD Serono, Merck, BridgeBio Pharma, Abbvie, Pfizer, Eli Lilly and Company BioNTech SE, Shenzhen TargetRx, Taiho Pharmaceutical, Chong Kun Dang, Bristol Myers Squibb, Innovent Biologics, Xuanzhu Biopharmaceutical, Bayer, GeneScience Pharmaceuticals, InventisBio, Apollomics, Imugene, Ono Pharmaceutical, Pierre Fabre, Jiangsu Hengrui Medicine Co., Bristol-Myers Squibb, Surface Oncology, Inhibrx, Sinocelltech, Mirati Therapeutics, REVOLUTION Medicines, Yong Shun Technology Development, Iovance Biotherapeutics, Galecto Biotech, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Over 230 patients enrolled in potential registration-enabling trial in 1L HLA-A2-negative MUM, and median PFS readout targeted by year-end 2025 95 patients enrolled in neoadjuvant UM trial and targeting clinical data and regulatory update(s) in H1 2025, including vision data in plaque brachytherapy patients Targeting median OS readout in ~40 1L MUM patients in 2025 Targeting expansion of study in Q1 2025 of IDE397 in combination with Trodelvy® (sacituzumab govitecan-hziy) in MTAP-deletion UC and clinical data update in 2025; expanded clinical study collaboration into NSCLC Targeting to enable wholly owned IDE397 and IDE892 (IDEAYA PRMT5) clinical combination in H2 2025; IDEAYA and Amgen mutually agree to wind down the IDE397 and AMG 193 clinical combination study Clinical expansion doses selected for DLL3 TOP1i ADC IDE849 by collaboration partner Hengrui, and targeting clinical data update and combo initiation with IDE161 in 2025 Ph1 initiated for Werner Helicase IDE275 (GSK959) and received $7 million milestone from GSK, and targeting medical conference update in H1 2025 Targeting IDE161 expansion with KEYTRUDA® (pembrolizumab), Merck's anti-PD-1 therapy, and combo(s) with TOP1i ADCs in solid tumors in 2025 Targeting 2025 INDs: IDE892 (PRMT5); IDE034 (B7H3/PTK7 ADC); IDE251 (KAT6/7) ~$1.1 billion of cash, cash equivalents and marketable securities as of December 31, 2024, anticipated to fund operations into at least 2028 SOUTH SAN FRANCISCO, Calif., Feb. 13, 2025 /PRNewswire/ -- IDEAYA Biosciences, Inc. (Nasdaq: IDYA), a precision medicine oncology company committed to the discovery and development of targeted therapeutics, announced financial results for the quarter and full year ended December 31, 2024, and provided a business update. "We are excited to be targeting multiple clinical data readouts and program updates across our clinical pipeline in 2025, including the darovasertib neoadjuvant UM data update in the first half and median PFS readout in HLA-A2 negative 1L MUM by year-end, update on the Werner Helicase inhibitor program IDE275 at a major medical conference in the first half, clinical combination results from the IDE397 and Trodelvy combination in MTAP-deletion UC where the Gilead collaboration has expanded to evaluate both UC and NSCLC, among others. Next, we are excited to target a clinical data update for potential first-in-class DLL3 TOP1 ADC IDE849 in SCLC in 2025, including potentially at a medical conference, and we believe the clinical profile observed supports a potential monotherapy regulatory path in SCLC," said Yujiro S. Hata, President and Chief Executive Officer, IDEAYA Biosciences. "We had multiple positive clinical updates across our pipeline throughout the past year that were presented at major medical conferences, including compelling results such as tumor shrinkage and eye preservation for neoadjuvant darovasertib which was presented as an oral presentation at ASCO 2024, and evidence for monotherapy activity with IDE397 which delivered a high disease control rate and multiple confirmed RECIST 1.1 responses in MTAP-deletion lung and urothelial cancer, which was presented as a late breaker oral presentation at ENA 2024. Next, we believe we have generated important proof-of-concept preclinically and preliminary clinical data for the MAT2A and PRMT5 combination in the MTAP-deletion setting and are excited to advance IDEAYA's wholly-owned IDE397 and IDE892 combination that we are targeting to have in the clinic in the second half of 2025," commented Darrin Beaupre, M.D., Ph.D., Chief Medical Officer, IDEAYA Biosciences. "Additionally, in the last several quarters we made significant progress in enhancing our potential first-in-class clinical pipeline with the in-licensing of the Phase 1 DLL3 TOP1i ADC IDE849 and FDA clearance of the Phase 1 trial for the Werner Helicase inhibitor IDE275. We are also advancing three programs into IND-enabling studies: our PRMT5 inhibitor IDE892, the B7H3/PTK7 ADC IDE034 and a KAT6/7 inhibitor IDE251," said Michael White, Ph.D., Chief Scientific Officer, IDEAYA Biosciences. Recent Key Developments and Upcoming Milestones Research and Clinical Development Darovasertib, a potential first-in-class Phase 2/3 PKC inhibitor for the treatment of metastatic uveal melanoma (MUM) and neoadjuvant uveal melanoma (UM). MUM Independent Data Monitoring Committee (IDMC) recommended move-forward dose and the completion of the Part 2a dose optimization for the potential registration-enabling trial of darovasertib and crizotinib in first line (1L) HLA-A2-negative MUM. Targeting median progression free survival (PFS) readout for Phase 2/3 registration-enabling trial of the darovasertib and crizotinib combination in 1L HLA-A2-negative MUM by year-end 2025. Rapid enrollment in the trial continues with over 230 patients as of February 7, 2025. Phase 2 median overall survival (OS) readout from study IDE196-001 in ~40 1L MUM patients targeted in 2025. Neoadjuvant UM A clinical update in over 75 patients in the Company-sponsored Phase 2 trial and regulatory update(s) is targeted for the first half of 2025, including vision data in plaque brachytherapy patients. 95 patients enrolled as of December 31, 2024 in the Company-sponsored Phase 2 trial. Initiation of the Phase 3 registration-enabling trial for darovasertib in neoadjuvant UM is targeted for the first half of 2025. IDE397, a potential first-in-class Phase 2 MAT2A Inhibitor for the treatment of MTAP-Deletion Solid Tumors. Encouraging Phase 1 expansion results of IDE397 in MTAP-deletion urothelial cancer (UC) and non-small cell lung cancer (NSCLC) patients were presented as a late-breaking oral presentation at the 36th EORTC-NCI-AACR Symposium (ENA 2024). Additional preclinical data on the anti-tumor activity of IDE397 and in combination with the PRMT5 inhibitors AMG 193 and BMS-986504 in MTAP-deleted tumors were presented as a poster. Targeting Phase 1/2 expansion in the first quarter of 2025 and clinical data update for IDE397 in combination with Trodelvy® in MTAP-deletion UC in 2025. Entered into a Clinical Study Collaboration and Supply Agreement with Gilead to evaluate IDE397 in combination with Trodelvy® in MTAP-deletion NSCLC. IDEAYA plans to enable wholly-owned IDE397 combination with IDE892 in patients with MTAP-deletion non-small cell lung cancer (NSCLC) in the second half of 2025. IDEAYA and Amgen mutually agreed to wind down the IDE397 and AMG 193 clinical combination study in February 2025, and will not pursue dose expansion. IDE849 (SHR-4849), a potential first-in-class Phase 1 DLL3 TOP1i antibody drug conjugate (ADC) targeting small cell lung cancer (SCLC) and neuroendocrine tumors (NETs). IDEAYA entered into an exclusive global license agreement for IDE849 outside of Greater China with Jiangsu Hengrui Pharmaceuticals Co., Ltd. (Hengrui Pharma) in December 2024. IDE849 is currently being evaluated by Hengrui Pharma in an ongoing Phase 1 trial in China in SCLC patients. In preliminary results from the trial with a data cut-off date of December 10, 2024, 8 out of 11 evaluable patients achieved partial response by RECIST 1.1, resulting in an overall response rate of ~73% (including both confirmed and unconfirmed responses, all unconfirmed responses were pending further evaluation). As of the data cut-off date, treatment related adverse events (TRAEs) were predominantly Grade 1 or 2. The most common TRAEs observed were white blood cell count decreased, anemia, neutrophil count decreased, nausea and platelet count decreased. In January 2025, Hengrui Pharma selected expansion doses for the Phase 1 trial. IDEAYA plans to submit a U.S. IND for the evaluation of IDE849 as a monotherapy in SCLC in the first half of 2025. Targeting to initiate the evaluation in combination with IDE161 and in NETs in the second half of 2025. Clinical data update targeted in 2025. IDE275 (GSK959), a potential first-in-class and best-in-class Phase 1 Werner Helicase inhibitor for the treatment of high microsatellite instability (MSI-High) tumors. Received FDA IND clearance for a Phase 1 trial in MSI-High tumors and earned a $7.0 million milestone payment from GSK. Data highlighting IDE275's differentiated potential best-in-class profile will be presented with GSK at a medical conference in the first half of 2025. IDE161, a potential first-in-class Phase 1 PARG inhibitor for the treatment of solid tumors. Selected initial Phase 1/2 expansion dose for IDE161 monotherapy in endometrial cancer, based on AE profile and preliminary clinical efficacy observed. Phase 1 monotherapy dose optimization is ongoing to confirm a move-forward Phase 2 expansion dose. First patient dosed in the Phase 1 trial evaluating IDE161 in combination with KEYTRUDA in patients with MSI-High and microsatellite stable (MSS) endometrial cancer. Targeting Phase 1 expansion in 2025. Highlighted preclinical data of IDE161 and antibody drug conjugate (ADC) combination rationale at a poster presentation at ENA 2024. Targeting clinical combination(s) of IDE161 with TOP1i ADCs in solid tumors in 2025. IDE705 (GSK101), a potential first-in-class Phase 1 Pol Theta Helicase Inhibitor in combination with PARP inhibitor for the treatment of HRD solid tumors. Targeting Phase 2 expansion in HRD solid tumors, which would trigger a potential $10 million milestone payment from GSK. Announced three development candidates for the treatment of solid tumors: IDE892, a potential best-in-class MTA-cooperative PRMT5 inhibitor to enable wholly-owned combination with IDE397. IND filing targeted for mid-year 2025. IDE034, a potential first-in-class B7H3/PTK7 TOP1i bispecific ADC with combination potential with IDE161. IND filing targeted for the second half of 2025. IDE251, a potential first-in-class KAT6/7 dual inhibitor development candidate with combination opportunities with multiple programs in the Company's pipeline. IND filing targeted for the second half of 2025. Corporate Development Appointed Joshua Bleharski, Ph.D., as Chief Financial Officer. Dr. Bleharski to join IDEAYA from J.P. Morgan, serving most recently as Managing Director and Global Co-Head of Biopharma in the Healthcare Investment Banking group. Josh spent nearly 17 years at J.P. Morgan advising clients in the biopharma sector on capital markets transactions, corporate strategy and other investment banking services representing more than $65 billion of value for biotechnology companies worldwide. Appointed Stu Dorman as Chief Commercial Officer. Mr. Dorman brings over 20 years of global commercialization experience in oncology with prominent biopharmaceutical companies such as Gilead Sciences and Bristol Myers Squibb, where he led multiple commercial launches for products including Trodelvy and Opdivo. Financial Results As of December 31, 2024, IDEAYA had cash, cash equivalents and marketable securities of approximately $1.1 billion, compared to $632.6 million as of December 31, 2023. The increase was primarily driven from $379.9 million in net proceeds from the sale of common stock shares through at-the-market financings during the year, $283.8 million from an underwritten public offering of common stock and pre-funded warrants to purchase common stock completed in July 2024, partially offset by net cash used in operations. IDEAYA believes that these funds will be sufficient to fund its planned operations into at least 2028. Subsequent to the reporting period for the year ended December 31, 2024, the Company generated net proceeds of approximately $25.1 million from the sale of shares of its common stock through at-the-market (ATM) offerings in January 2025. Collaboration revenue for the three months ended December 31, 2024 totaled $7.0 million compared to $3.9 million for the three months ended December 31, 2023. Collaboration revenue was recognized for a $7.0 million milestone payment from GSK that was earned for the IND clearance of IDE275 (GSK959) in October 2024. Research and development (R&D) expenses for the three months ended December 31, 2024, totaled $140.2 million compared to $38.8 million for the three months ended December 31, 2023. The increase was primarily due to a $75.0 million upfront payment under the license agreement for IDE849 with Hengrui Pharma, higher clinical trial expenses to support the portfolio growth and personnel-related expenses. General and administrative (G&A) expenses for the three months ended December 31, 2024 totaled $11.0 million compared to $7.1 million for the three months ended December 31, 2023. The increase was primarily due to higher personnel-related expenses, higher consulting and legal fees. The net loss for the three months ended December 31, 2024, was $130.3 million compared to the net loss of $34.0 million for the three months ended December 31, 2023. Total stock compensation expense for the three months ended December 31, 2024, was $9.5 million compared to $4.8 million for the same period in 2023. The net loss for the year ended December 31, 2024 was $274.5 million compared to $113.0 million for the same period in 2023. Total stock compensation expense for the year ended December 31, 2024, was $34.7 million compared to $18.5 million for the same period in 2023. About IDEAYA Biosciences IDEAYA is a precision medicine oncology company committed to the discovery and development of targeted therapeutics for patient populations selected using molecular diagnostics. IDEAYA's approach integrates capabilities in identifying and validating translational biomarkers with drug discovery to select patient populations most likely to benefit from its targeted therapies. IDEAYA is applying its research and drug discovery capabilities to synthetic lethality – which represents an emerging class of precision medicine targets. IDEAYA's updated corporate presentation is available on its website, at its Investor Relations page: . Forward-Looking Statements This press release contains forward-looking statements, including, but not limited to, statements related to (i) the timing and content of clinical program updates, regulatory updates and clinical trial data readouts; (ii) the potential therapeutic benefits of IDEAYA therapeutics; (iii) the translation of preliminary clinical trial results into future clinical trial results and/or regulatory approval; (iv) timing of development and regulatory milestones; (v) the timing and potential of registration-enabling trial and readouts for darovasertib in 1L HLA-A2 negative MUM; (vi) the timing of the initiation of Phase 3 trial for darovasertib; (vii) the timing and potential for accelerated FDA approval of darovasertib in MUM; (viii) the timing of expansion in IDE397 and Trodelvy combination trial in MTAP-deletion UC and indication in NSCLC; (ix) the timing of combination trial of IDE397 and IDE892 in patients with MTAP-deletion NSCLC; (x) the potential of a Phase 2 expansion monotherapy dose for IDE161; (xi) the timing of initiating IDE161 and DLL3 TOP1i ADC combination trial; (xii) the timing of IDE161 expansion with KEYTRUDA and combinations with TOP1i ADCs in solid tumors; (xiii) timing of INDs for IDE892, IDE034, IDE251, and IDE849; (xiv) timing of data presentation for IDE275 at medical conference; and (xv) the extent to which IDEAYA's existing cash, cash equivalents, and marketable securities will fund its planned operations. Such forward-looking statements involve substantial risks and uncertainties that could cause IDEAYA's preclinical and clinical development programs, future results, performance or achievements to differ significantly from those expressed or implied by the forward-looking statements. Such risks and uncertainties include, among others, the uncertainties inherent in the drug development process, including IDEAYA's programs' early stage of development, the process of designing and conducting preclinical and clinical trials, the regulatory approval processes, the timing of regulatory filings, the challenges associated with manufacturing drug products, IDEAYA's ability to successfully establish, protect and defend its intellectual property, and other matters that could affect the sufficiency of existing cash to fund operations. IDEAYA undertakes no obligation to update or revise any forward-looking statements. For a further description of the risks and uncertainties that could cause actual results to differ from those expressed in these forward-looking statements, as well as risks relating to the business of IDEAYA in general, see IDEAYA's Annual Report on Form 10-K dated February 20, 2024 and any current and periodic reports filed with the U.S. Securities and Exchange Commission. Investor and Media Contact IDEAYA Biosciences Andres Ruiz Briseno SVP, Head of Finance and Investor Relations [email protected] SOURCE IDEAYA Biosciences, Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED