IDEAYA Biosciences (NASDAQ:IDYA) announced today the first-patient-in for its Phase 1 dose-escalation clinical trial of IDE574, a potential first-in-class oral dual inhibitor of KAT6 and KAT7 targeting a broad range of solid tumors.
The study, which officially commenced on April 6, 2026, is designed to evaluate the safety, pharmacokinetics, and preliminary monotherapy efficacy of IDE574 in patients with advanced solid tumors, including breast, prostate, colorectal, and lung cancers.
The initiation marks a significant milestone for IDEAYA’s precision medicine pipeline as it moves another novel epigenetic therapy into the clinic.
IDE574 distinguishes itself through a highly potent and selective profile.
Preclinical data indicates single-digit to low-teen nanomolar cellular potency and a 350x to 2,000x selectivity advantage over the related KAT5 and KAT8 proteins.
Most notably, the compound has demonstrated superior monotherapy durability in preclinical models when compared to selective KAT6 inhibitors, suggesting that the dual inhibition of both KAT6 and KAT7 may offer a more robust clinical response.
The company is scheduled to present a comprehensive preclinical profile of IDE574 at the American Association for Cancer Research (AACR) Annual Meeting 2026, which is currently underway.
The presentation is expected to detail the mechanistic rationale for dual KAT6/7 inhibition and provide further evidence of the molecule's potential to overcome resistance mechanisms common in traditional hormone-driven cancers.