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IDEAYA Biosciences Announces IDE251: A First-in-Class Dual KAT6/7 Inhibitor for 8p11-Amplified Cancers

NextEdge Admin

17 Dec 2024

2 min 36 sec

IDEAYA Biosciences, a precision medicine oncology company, has announced the nomination of IDE251 as its third development candidate this quarter and the eighth in its pipeline. IDE251 is a potential first-in-class, small-molecule dual inhibitor targeting KAT6 and KAT7, epigenetic modulators involved in cell identity and lineage programs disrupted by oncogenic transformation.

IDE251 selectively inhibits KAT6 and KAT7 while sparing other structurally similar KAT family members. Preclinical studies demonstrate that dual inhibition of KAT6/7 delivers robust and durable anti-tumor activity, outperforming KAT6 inhibition alone. The therapy shows particular promise in cancers with 8p11 amplification, which is found in approximately 15% of breast cancer cases and up to 17.5% of squamous non-small cell lung cancers (NSCLC). IDEAYA also sees potential in biomarker-defined settings where cancers rely on lineage-specific transcription factors.

Currently, IND-enabling studies are underway to support clinical evaluation of IDE251 as a monotherapy in 8p11-amplified breast and lung cancers, with additional opportunities in lineage addiction-driven cancers. IDEAYA targets submission of an Investigational New Drug (IND) application to the U.S. FDA in 2025, contingent on successful preclinical outcomes.

Yujiro S. Hata, IDEAYA’s President and CEO, emphasized IDE251’s potential to address significant unmet needs in breast and lung cancers, while Chief Scientific Officer Michael White, Ph.D., highlighted its differentiated preclinical profile and selective targeting mechanism.

IDEAYA Biosciences integrates biomarker-driven patient selection with precision drug discovery, focusing on synthetic lethality and epigenetic modulation to develop therapies for molecularly defined oncology populations. The advancement of IDE251 reflects IDEAYA's commitment to delivering targeted therapies that offer improved outcomes for patients with specific molecular alterations.