IDEAYA Biosciences initiated Part 2 monotherapy expansion for IDE892, a PRMT5 inhibitor with 1,400-fold selective MTA cooperative binding, in MTAP-deleted pancreatic and lung cancers after achieving projected efficacious exposures.
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IDEAYA starts IDE892 expansion in 2 cancer types with 1,400-fold selectivity
IDEAYA Biosciences has initiated Part 2 monotherapy expansion for its PRMT5 inhibitor IDE892 in MTAP-deleted pancreatic and lung cancers after clearing multiple dose cohorts and achieving projected efficacious target exposures, the company said Monday.
"The drug's 1,400-fold selective MTA-PRMT5 cooperative binding versus SAM-PRMT5 cooperative binding, lack of brain penetrance, and favorable drug-like properties are intended to maximize its therapeutic window as both a monotherapy agent and in combination," Yujiro S. Hata, president and chief executive officer at IDEAYA, said.
IDE892 showed a CYP3A4 IC50 greater than 45 micromolar with no time-dependent inhibition of any of the seven major cytochrome P450 enzymes, based on full kinetic CYP inactivation assays. The maximum tolerated dose has not yet been reached in the ongoing dose escalation, which continues in parallel with the expansion phase.
MTAP deletion occurs in about 15 percent of all solid tumors, including up to 40 percent of pancreatic ductal adenocarcinoma and roughly 15 percent of non-small cell lung cancer. No approved therapies exist for MTAP-deleted cancers, representing a significant unmet need that IDEAYA is targeting with what it calls the industry's deepest MTAP-deletion pipeline.
The company is also advancing combination studies of IDE892 with its MAT2A inhibitor IDE397 in MTAP-deleted NSCLC and PDAC, and has entered a clinical collaboration with Roche to evaluate IDE892 with Roche's pan-RAS inhibitor RG6505 in MTAP-deleted PDAC, with first-patient-in targeted for the second half of 2026. A third program targeting CDKN2A, the most common co-alteration of MTAP deletion, is in preclinical toxicology studies with an IND application targeted for the first half of 2027.
The expansion initiation marks a key milestone for IDEAYA's synthetic lethality strategy. Investors will watch for initial efficacy data from the monotherapy expansion cohorts and the company's planned MTAP/CDKN2A, KRAS, and Pancreatic Cancer R&D Day in the fourth quarter of 2026.
This article is for informational purposes only and does not constitute investment advice.
[1] IDEAYA Biosciences Announces IDE892, a Potential Best-in-Class MTA-Cooperative PRMT5 Inhibitor, Initiates Part 2 Monotherapy Expansion in the Phase 1/2 Study in MTAP-Deleted Pancreatic and Lung Cancers[2] IDEAYA initiates expansion phase for cancer drug IDE892 By Investing.com - Investing.com Canada
