IDEAYA Biosciences reached a key clinical milestone on Monday, dosing the first patient in its Phase 1 trial for IDE892, a potential best-in-class PRMT5 inhibitor designed to target MTAP-deleted solid tumors.
The South San Francisco-based precision medicine firm (NASDAQ:IDYA) announced that the multicenter trial is now underway to evaluate the safety, tolerability, and pharmacokinetics of IDE892.
The compound is an MTAP-selective PRMT5 inhibitor that exhibits ~1,400-fold selective binding to the MTA-PRMT5 complex over the SAM-PRMT5 complex, showing single-digit nanomolar potency in MTAP-deleted cell lines.
The study is designed to evaluate IDE892 both as a monotherapy and in combination with IDEAYA’s MAT2A inhibitor, IDE397.
The company expects to achieve first-patient-in (FPI) for the combination arm in mid-2026, focusing on indications like non-small cell lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC).
In a strategic shift, IDEAYA confirmed it will deprioritize its combination activities with Gilead’s Trodelvy (sacituzumab govitecan-hziy).
The company will conclude enrollment in existing Trodelvy combination trials as it prioritizes its wholly-owned MTAP-deletion and CDKN2A pipeline. I