IDEAYA Biosciences is making significant strides in its precision medicine oncology pipeline with the nomination of new development candidates and a clinical study collaboration with Gilead Sciences. These advancements underscore IDEAYA's commitment to developing targeted therapeutics for cancers with specific molecular profiles.
IDE251: A Novel KAT6/KAT7 Inhibitor
IDEAYA Biosciences recently nominated IDE251 as a new development candidate. This molecule is a potential first-in-class dual inhibitor targeting KAT6 and KAT7, which are implicated in certain types of cancer, including breast and non-small cell lung cancer (NSCLC). Preclinical studies have demonstrated robust and durable anti-tumor activity in tumor models with 8p11 amplifications, a genetic anomaly present in approximately 15% of breast cancer patients and 17.5% of squamous NSCLC cases. The company is preparing for an Investigational New Drug (IND) submission to the U.S. Food and Drug Administration (FDA) in 2025, contingent upon successful completion of ongoing preclinical and IND-enabling studies.
According to Yujiro S. Hata, President and CEO of IDEAYA Biosciences, the nomination of IDE251 is a significant milestone, marking the third development candidate this quarter and the eighth in the company's precision medicine oncology pipeline. Michael White, Ph.D., Chief Scientific Officer at IDEAYA, emphasized the molecule's potential to deliver superior anti-tumor activity compared to KAT6 inhibition alone in preclinical models.
Collaboration with Gilead on IDE397 and Trodelvy
IDEAYA has entered into an additional clinical study collaboration and supply agreement with Gilead Sciences to evaluate the efficacy and safety of IDE397, its investigational, potential first-in-class, small molecule MAT2A inhibitor, in combination with Gilead's Trodelvy® (sacituzumab govitecan-hziy), a Trop-2 directed antibody-drug conjugate (ADC), in methylthioadenosine phosphorylase (MTAP)-deletion non-small cell lung cancer (NSCLC).
The prevalence of MTAP-deletion is estimated to be approximately 15% in NSCLC. Darrin Beaupre, M.D., Ph.D., Chief Medical Officer, IDEAYA Biosciences, stated, "We are pleased to broaden the ongoing evaluation of the potential first-in-class clinical combination of IDE397 and Trodelvy to now include patients with MTAP-deletion NSCLC in our ongoing Phase 1 trial currently evaluating the combination in MTAP-deletion urothelial cancer."
IDE892: A Potential Best-in-Class MTA-cooperative PRMT5 Inhibitor
IDEAYA Biosciences announced the development candidate nomination of IDE892, a potential best-in-class MTA-cooperative PMRT5 inhibitor. IDE892 was discovered through IDEAYA's iterative physics-based ligand design and optimization platform and has demonstrated exceptionally selective antiproliferative activity in MTAP-deleted tumor cell models and durable complete responses in combination with MAT2A inhibitor IDE397 in challenging MTAP-deletion preclinical models. IND-enabling studies for IDE892 are ongoing to support an Investigational New Drug (IND) filing to the U.S. Food and Drug Administration (FDA) in mid-2025, subject to satisfactory completion of ongoing preclinical and IND-enabling studies.
"We continue to expand our precision medicine oncology pipeline and are excited to nominate our 7th development candidate in IDE892, a potential best-in-class MTA-cooperative PMRT5 inhibitor. IDE892 advances our strategic objective to enable a wholly owned combination between the PRMT5 and MAT2A mechanisms, to deliver potentially greater efficacy in MTAP-deletion solids tumors through this rational combination approach," said Yujiro S. Hata, President and Chief Executive Officer of IDEAYA Biosciences.
