IDEAYA Biosciences Submits IND for First-in-Class KAT6/7 Dual Inhibitor IDE574 Targeting Breast and Lung Cancers
核心洞察
IDEAYA Biosciences has submitted an IND application to the FDA for IDE574 (搜索), a potential first-in-class KAT6 (搜索)/7 dual inhibitor with high selectivity over related KAT5 (搜索)/8 enzymes.
The company plans to initiate a Phase 1 dose escalation trial of monotherapy IDE574 (搜索) in the first quarter of 2026 for patients with hormone receptor-positive breast cancer (搜索) and lung adenocarcinoma (搜索).
Preclinical studies demonstrate that IDE574 (搜索) disrupts tumor lineage identity and delivers robust anti-tumor activity in patient-derived lung and breast cancer (搜索) xenograft models.
IDEAYA Biosciences has submitted an investigational new drug (IND) application to the U.S. Food and Drug Administration for IDE574 (搜索), a potential first-in-class KAT6 (搜索)/7 dual inhibitor designed to target breast and lung cancers. The South San Francisco-based precision medicine oncology company announced the regulatory filing on December 10, 2025, with plans to begin a Phase 1 dose escalation trial of monotherapy IDE574 in the first quarter of 2026.
Novel Mechanism Targets Epigenetic Modulators
IDE574 (搜索) represents an equipotent, highly selective small molecule dual inhibitor of lysine acetyltransferase (KAT) 6 and 7, both of which have been shown to support cancer cell survival. The compound demonstrates high selectivity over related KAT5 (搜索)/8 enzymes, distinguishing it from other structurally similar KAT family members.
"IDE574 (搜索) is a promising potential first-in-class molecule that potently inhibits two tumor-promoting epigenetic modulators, KAT6 (搜索) and KAT7 (搜索), while sparing other structurally similar KAT family members," said Michael White, Ph.D., Chief Scientific Officer of IDEAYA Biosciences.
Preclinical Evidence Supports Clinical Development
Preclinical studies have demonstrated that KAT6 (搜索) and KAT7 (搜索) collaboratively control lineage-specific tumorigenic transcription factor activity essential for tumor cell proliferation and survival. According to White, dual KAT6/7 inhibition by IDE574 (搜索) disrupts tumor lineage identity and delivers robust anti-tumor activity in patient-derived lung and breast cancer (搜索) xenograft models dependent upon lineage-specific transcription factor activity.
IND-enabling studies support the potential clinical evaluation of IDE574 (搜索) monotherapy in patients with hormone receptor-positive breast cancer (搜索) and lung adenocarcinoma (搜索), as well as additional opportunities associated with lineage addiction.
Clinical Development Timeline
The company is targeting to begin the Phase 1 dose escalation trial in the first quarter of 2026. IDEAYA also plans to share data from its preclinical work with IDE574 (搜索) at a medical conference in the first half of 2026, presenting details on the pharmacologic profile and evidence of anti-tumor activity in solid tumor models.
Company Background
IDEAYA Biosciences positions itself as a precision medicine oncology company committed to the discovery, development, and commercialization of transformative cancer therapies. The company's approach integrates expertise in small-molecule drug discovery, structural biology and bioinformatics with internal capabilities in identifying and validating translational biomarkers to develop tailored, potentially first-in-class targeted therapies aligned to genetic drivers of disease.
The company has built a pipeline of product candidates focused on synthetic lethality and antibody-drug conjugates for molecularly defined solid tumor indications, with a mission to bring forth precision oncology therapies that are more selective, more effective, and deeply personalized to improve clinical outcomes for cancer patients.