IDEAYA Biosciences Advances Solid Tumour Treatment, First Patient Dosed In IDEAYA’s IDE574 Trial, Exploring Novel Epigenetic Therapy For Resistant Cancers

IDEAYA Biosciences, Inc. has announced the enrollment of the first patient in its Phase 1 dose-escalation trial evaluating IDE574, a potential first-in-class oral small molecule targeting cancer survival pathways. The study will assess the safety, efficacy, and pharmacokinetics of the drug as a standalone treatment in patients with solid tumors, including breast, prostate, colorectal, and lung cancers.

IDE574 is a dual inhibitor of the lysine acetyltransferase paralogs KAT6 and KAT7, which play a key role in cancer cell survival. The molecule demonstrates strong potency in cellular assays while maintaining high selectivity, avoiding interference with related proteins, such as KAT5 and KAT8, which are essential for normal cellular function. This targeted mechanism positions IDE574 as a promising candidate for epigenetic cancer therapies.

"Targeting mechanisms of resistance and tumor heterogeneity in cancer are core strategies of our R&D efforts, and we are excited to advance IDE574 in the clinic to evaluate its potential as a monotherapy agent to drive deeper, more durable antitumor responses for patients versus historical clinical data published with KAT6-selective agents," said Michael White, Ph.D., Chief Scientific Officer of IDEAYA Biosciences. "We are thrilled to advance another potential first-in-class agent into the clinic that targets large solid tumor indications of high unmet need, including breast, prostate, CRC, and lung cancer.  We believe the novel chromatin remodeling mechanism of the KAT6/7 dual inhibitor IDE574, has the potential for monotherapy efficacy and to treat breast cancer patient's refractory to hormone-based therapy due to ESR1 mutations, and to evaluate rational combinations with assets in the IDEAYA pipeline," said Yujiro S. Hata, President and Chief Executive Officer, IDEAYA Biosciences.

KAT6 and KAT7 regulate cell identity and lineage programs, processes that are often disrupted during cancer development. The therapy may be particularly relevant in cases where tumors develop resistance to existing treatments. For example, ESR1 mutations, commonly seen in hormone-resistant breast cancer, highlight the need for alternative therapeutic approaches like KAT6/7 inhibition.

Preclinical studies have shown encouraging results, with IDE574 demonstrating strong and sustained anti-tumor activity as a monotherapy. The drug has outperformed single-target KAT6 inhibition in models with specific genetic alterations, such as 8p11 amplifications and ESR1 mutations, supporting its potential as a novel treatment option in precision oncology.