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IDEAYA Biosciences Announces First-Patient-In for Phase 1 Trial of IDE574, a Potential First-In Class Dual Inhibitor of KAT6/7 to Target Multiple Solid Tumor Indications, including Breast, Prostate, CRC, and Lung Cancer
Potential first-in-class and selective equipotent dual inhibitor of KAT6/7 with single-digit to low teens nano-molar cellular potency in target engagement
About this update from Ideaya Biosciences, Inc.
[{"type":"text","content":"Potential first-in-class and selective equipotent dual inhibitor of KAT6/7 with single-digit to low teens nano-molar cellular potency in target engagement assays against KAT6 and KAT7, and ~350-to-2,000-fold selectivity over the KAT5 and KAT8 paralogsKAT6/7 dual inhibitor demonstrates greater monotherapy efficacy and durability than KAT6 selective inhibitors in preclinical CDX and PDX modelsMultiple combination opportunities with IDE574 and IDEAYA's proprietary pipelinePotential first-in-class and best-in-class preclinical profile will be presented at AACR 2026SOUTH SAN FRANCISCO, Calif., April 6, 2026 /PRNewswire/ -- IDEAYA Biosciences, Inc. (NASDAQ: IDYA), a leading precision medicine oncology company, today announced that the first patient has been enrolled in its Phase 1 dose escalation trial evaluating IDE574, a potential first-in-class oral small molecule equipotent dual inhibitor of the lysine acetyltransferase (KAT) 6 and 7 paralogs, both of which have been shown to support cancer cell survival. The company is planning to evaluate safety, efficacy and pharmacokinetics of IDE574 as a monotherapy in the Phase 1 dose escalation trial in solid tumor patients, including breast, prostate, colorectal, and lung cancer. \n \n \n \n \n \n \n \n\"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.IDE574 is a selective, equipotent dual inhibitor of both KAT6 and KAT7 with single-digit to low-teen nanomo...