IDEAYA Biosciences, Inc.

Potential best-in-class profile, including ~1,400-fold selective binding to MTA-PRMT5 versus SAM-PRMT5 complexes, and single-digit nanomolar potency in MTAP-deleted cell lines IDE892 is being evaluated as a monotherapy agent in MTAP-deleted solid tumors, including NSCLC and PDAC, and targeting combination FPI with IDE397 (MAT2A) in mid-2026 Targeting nomination of a first-in-class CDKN2A development candidate in H2 2026 and IND in H1 2027; prevalence of CDKN2A-deficiency has been reported at over 80% in PDAC IDEAYA will deprioritize combination activities with Trodelvy as part of a strategic prioritization of its proprietary MTAP-deleted and CDKN2A pipeline March 9, 2026 -- IDEAYA Biosciences, Inc. (NASDAQ: IDYA), a leading precision medicine oncology company, today announced that the first patient has been enrolled in its Phase 1 clinical trial evaluating IDE892, an investigational MTA-cooperative PRMT5 inhibitor being developed for patients with MTAP-deleted solid tumors, including non-small cell lung cancer and pancreatic cancer. The trial will assess safety, tolerability, pharmacokinetics, and pharmacodynamics of IDE892 as a monotherapy agent and in combination with IDE397, IDEAYA's MAT2A inhibitor, in mid-2026. Dual inhibition of IDE892 and IDE397 has demonstrated durable and well-tolerated tumor regressions in preclinical MTAP-deleted tumor models, including in NSCLC. "We are excited to have enrolled the first patient in our Phase 1 clinical trial evaluating IDE892 in patients with MTAP-deleted solid tumors, including non-small cell lung cancer and pancreatic cancer. We designed IDE892 with potential best-in-class properties, including specific biophysical and pharmacokinetic properties that we believe will maximize its therapeutic window and clinical efficacy, both as a monotherapy agent and as a combination partner with our MAT2A inhibitor, IDE397. Next, we look forward to advancing our first-in-class CDKN2A-defiency program to progress our broader corporate strategy of enabling wholly owned rational combinations targeting MTAP-deletion," said Yujiro S. Hata, President and Chief Executive Officer, IDEAYA Biosciences. IDE892 was designed to be a potential best-in-class PRMT5 inhibitor, with ~1,400-fold selective binding to MTA-PRMT5 versus SAM-PRMT5 complexes and observed single-digit nano-molar potency in endogenous MTAP-deleted cell lines, and greater than 50-fold potency differential in MTAP-deleted versus MTAP wild type HCT116 isogenic cell lines. In addition, IDE892 inhibited the arginine dimethylation of a key PRMT5 substrate involved in mRNA splicing, spliceosome protein SmB (SmB-SDMA), with pico-molar potency in MTAP-deleted cell lines with greater than 100-fold potency differential versus an MTAP wild type cell line. IDE892 has demonstrated monotherapy regressions in MTAP-deleted preclinical models, and durable complete responses in combination with IDE397. Loss of MTAP leads to the accumulation of methylthioadenosine (MTA) and increased dependence on PRMT5 and MAT2A, two key enzymes involved in methylation and RNA splicing. In MTAP-deleted tumors, this biology establishes a robust synthetic lethal vulnerability that underpins the mechanistic rationale for combining IDE892 and IDE397. In preclinical studies, dual inhibition of PRMT5 and MAT2A with the combination of IDE892 and IDE397 resulted in potent anti-tumor activity in MTAP-deleted tumor models, including complete and durable responses at well-tolerated doses below those required for monotherapy activity. IDEAYA has also advanced its CDKN2A-deficiency program and is on track to select a potential first-in-class development candidate in H2 2026 with a target IND in H1 2027. IDEAYA has demonstrated robust monotherapy efficacy with its CDKN2A lead in multiple preclinical models, including in a KRAS mutation pancreatic model. IDEAYA plans to evaluate its CDKN2A-deficiency program preclinically as a monotherapy agent, and in combination with assets in its MTAP-deletion portfolio and potentially other RAS and KRAS targeted assets. CDKN2A-defiency is common in cancer, with a prevalence of over 80% in pancreatic cancer (M. Schutte, et al., Cancer Research, 1997; IDEAYA analysis, TCGA) and is typically co-deleted in MTAP-deletion solid tumors and a common co-alteration with KRAS mutations, particularly in pancreatic cancer, creating rational combination opportunities with MTAP-deletion and KRAS targeted therapies, respectively. As part of IDEAYA's strategic prioritization of its proprietary MTAP-deleted pipeline, including IDE397 and IDE892, and the advancement of its CDKN2A-deficiency program, the company has deprioritized its clinical combination activities with Trodelvy and will be concluding enrollment in the ongoing Phase 1/2 trials with Gilead. Based on preliminary data from these trials supporting the mechanistic rationale for the combination in MTAP-deleted cancers, IDEAYA may evaluate additional combinations between IDE397 and other TOP1 payload ADCs in this setting, including IDE034, its B7H3/PTK7 bispecific TOP1 ADC. MTAP deletion is estimated to occur in 15–20% of non-small cell lung cancer, up to 40% of pancreatic cancer, and approximately 15% of all solid tumors, and is commonly co-deleted with CDKN2A due to the proximity of the two genes on chromosome 9p21. There are no approved therapies for patients with MTAP deletion, highlighting the significant unmet need and important new opportunities for precision therapies. IDEAYA is 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, or ADCs, for molecularly defined solid tumor indications. 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. The content above comes from the network. if any infringement, please contact us to modify.

The crown jewel of a transaction with Servier is no doubt Day One Biopharmaceuticals\' Ojemda (tovorafenib), a type 2 RAF inhibitor approved in 2024 to treat patients 6 months and older with relapsed or refractory pediatric low-grade glioma. \n As nonprofit-governed Servier continues to make gains with its IDH-mutant glioma med Voranigo, the drugmaker is wading deeper into the rare oncology arena with a new M&A play. Servier on Friday unveiled a definitive agreement to acquire Day One Biopharmaceuticals—a commercial-stage company developing targeted therapies for pediatric cancers and other diseases—for $21.50 per share in cash. The total value of the deal, which is expected to close in the second quarter, comes to roughly $2.5 billion, the companies said in a March 6 release. The crown jewel of the transaction is no doubt Day One’s Ojemda (tovorafenib), a type 2 RAF inhibitor approved by the FDA in April 2024 to treat patients ages 6 months and older with relapsed or refractory pediatric low-grade glioma (pLGG), a more advanced stage of the common childhood brain tumor. That drug will likely mesh well with Servier’s Voranigo, also approved in 2024 under a different glioma niche in patients 12 years and older with a susceptible IDH1 or IDH2 mutation. Servier acquired that drug by way of transaction, too, picking Voranigo up in its 2021 purchase of Agios Pharmaceuticals for $2 billion. Over on the R&D side of things, Servier will also be able to tap into Day One’s early- to late-stage pipeline, which includes additional programs for tovorafenib in pediatric low-grade gliomas, plus assets running through development in indications like adenoid cystic carcinoma and adult and pediatric solid tumors.  Servier says it plans to fund the deal through a mix of existing cash and investments. The company’s share price offer reflects a premium of roughly 68% over Day One’s closing price March 5, according to the companies’ press announcement. “In less than a decade, we have built a durable oncology platform in the United States,” David Lee, CEO of Servier’s U.S. arm, told Fierce in an emailed statement Friday. “That didn’t happen through short-term thinking—it came from sustained investment in science, infrastructure and people.”He reiterated Servier’s ambition to “lead in rare cancers,” noting that for these patients, “progress often depends on a small number of people and organizations choosing to commit when others will not.” Lee continued, “When the science is promising and the need is urgent, we believe it is our responsibility to build the capabilities that can turn discovery into real outcomes for patients.”Servier has long leaned on its patient-centric ethos—credited to its unique governance model under the nonprofit Fondation Internationale de Recherche Servier—as one of the company’s key strengths and distinguishing features. Lee remarked similarly on the company’s governance model allowing Servier “to do things that other companies can’t” and “invest in diseases that other people would not be able to make a business case for” during an interview with Fierce Pharma at the J.P. Morgan Healthcare Conference in 2025. At the time, Lee noted that the landscape for brain cancer treatment remained “pretty open,” adding that, in terms of potential external opportunities for Servier, “anything mutation-driven is still good for us … but we’re open to any [glioblastomas], gliomas or astrocytomas.”Taking a look at the population Ojemda addresses, the FDA has specifically cleared the RAF inhibitor in relapsed or refractory pLGG patients with a BRAF fusion or rearrangement, or BRAF V600 mutation. PLGG is the most common type of childhood brain tumor, with BRAF alterations making up about 1,100 of 1,500 new diagnoses each year. Outside the U.S., Ojemda also won a positive recommendation for approval in the same indication in Europe late last month, a region where Ipsen holds licensing rights to the Day One drug. Servier is making its latest oncology play as the drugmaker seeks to achieve 10 billion euros ($11.5 billion) in annual sales by 2030. After a successful showing in its 2024-25 financial year, which ended in September with 16.2% growth to 6.9 billion euros ($8.2 billion), the group’s president, Olivier Laureau, said in January that Servier was “one important step closer” to meeting that target. Servier didn’t mince words about Voranigo’s contribution to its earnings haul last year, noting that its overall oncology business grew 55% in the 2024-25 fiscal period, with the unit’s contribution toward Servier’s overall revenue rising to 32% from 24% in the previous period.  Servier has been busy on the oncology dealmaking front, last year licensing a phase 1 asset from Black Diamond Therapeutics for RAF/RAS-mutant solid tumors, acquiring a phase 1/2 leukemia candidate from BioNova Pharmaceuticals and obtaining ex-U.S. rights to Ideaya Biosciences’ potential first-in-class PKC inhibitor darovasertib under development in uveal melanoma—not to mention an oncology drug discovery pact with artificial intelligence biotech Insilico Medicine made in January. As of late, the company has also been working to bolster its offerings in neurology. 

IDE034 is a B7H3/PTK7 bispecific TOP1 ADC designed to target tumor cells expressing both B7H3 and PTK7 preferentially, and is being evaluated as monotherapy and in combination with IDEAYA’s PARG inhibitor IDE161. IDEAYA has dosed the first patient in its Phase 1 trial of IDE034, initially evaluating safety, tolerability, and PK. First dosing triggers a $5 million milestone payment to Biocytogen under the companies’ option and license agreement. BEIJING--(BUSINESS WIRE)-- #Antibody --Biocytogen Pharmaceuticals (Beijing) Co., Ltd. (Biocytogen, SSE: 688796; HKEX: 02315), a global biotechnology company that drives the research and development of novel antibody-based drugs with innovative technologies, today announced that its partner IDEAYA Biosciences, Inc. (“IDEAYA”; Nasdaq: IDYA) has dosed the first patient in IDEAYA’s Phase 1 dose-escalation/expansion clinical trial of IDE034, an investigational B7H3/PTK7 bispecific TOP1 ADC. Pursuant to the companies’ option and license agreement, first patient dosing triggers a $5 million milestone payment to Biocytogen. According to IDEAYA, the Phase 1 study is designed to characterize IDE034’s safety profile, tolerability, and PK as a monotherapy, and IDEAYA also intends to evaluate combination regimens with DNA damage response (DDR) -targeting agents such as its oral PARG inhibitor IDE161 as the program advances. IDE034 is a potential first-in-class bispecific B7H3/PTK7 TOP1 ADC, independently developed by Biocytogen and licensed to IDEAYA in July 2024. IDEAYA has stated that IDE034 is designed to preferentially internalize in tumor cells co-expressing B7H3 and PTK7, supporting selectivity and tolerability, and estimates 30–40% co-expression across several major solid tumors with limited dual expression in normal tissues. “Reaching first dosing in the IDE034 Phase 1 trial marks an important step in translating this bispecific TOP1 ADC concept into clinical evaluation,” said Dr. Yuelei Shen, President and CEO of Biocytogen. “We appreciate IDEAYA’s strong execution in advancing IDE034 into the clinic and look forward to the readout of initial safety and PK data from the ongoing Phase 1 study.” About Biocytogen Biocytogen (SSE: 688796; HKEX: 02315) is a global biotechnology company that drives the research and development of novel antibody-based drugs with innovative technologies. Founded on gene editing technology, Biocytogen has established a dual-engine platform combining a fully human antibody library with an extensive target-humanized mouse model portfolio, enabling a systematic approach to accelerating global drug discovery and development. Biocytogen has independently developed its proprietary RenMice ® (RenMab ® / RenLite ® / RenNano ® /RenTCR™/ RenTCR mimic™) platforms for fully human monoclonal/bispecific/multispecific antibody discovery, bispecific antibody-drug conjugate discovery, hu-VHH discovery, and TCR mimic antibody discovery, and has established a sub-brand, RenSuper™ Biologics, to explore global partnerships for an off-the-shelf library of >1,000,000 fully human antibody sequences against over 1000 targets for worldwide collaboration. As of June 30, 2025, approximately 280 therapeutic antibody and multiple clinical asset co-development/out-licensing/transfer agreements and over 50 target-nominated RenMice ® licensing projects have been established around the globe, including several partnerships with multinational pharmaceutical companies (MNCs). Biocytogen pioneered the generation of drug target knock-in humanized models for preclinical research, and currently provides a few thousand off-the-shelf animal and cell models under the company's sub-brand, BioMice™, along with preclinical pharmacology and gene-editing services for clients worldwide. Headquartered in Beijing, Biocytogen has branches in China (Haimen, Jiangsu, Shanghai), the USA (Boston, San Francisco, San Diego), and Germany (Heidelberg). For more information, please visit . Contacts Biocytogen Contacts Antibody assets and platforms: BD-Licensing@biocytogen.com Media: pr@biocytogen.com.cn