IDEAYA Biosciences Advances Potential First-In-Class KAT6/7 Inhibitor IDE574 Into Phase 1 Trials

The dual inhibitor targets solid tumors including breast, prostate, colorectal, and lung cancer.

Apr. 6, 2026 at 11:09am

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IDEAYA Biosciences has announced the enrollment of the first patient in a Phase 1 clinical trial evaluating IDE574, a potential first-in-class oral small molecule that inhibits the lysine acetyltransferase (KAT) 6 and 7 enzymes. The company plans to assess the safety, efficacy, and pharmacokinetics of IDE574 as a monotherapy in solid tumor patients, including those with breast, prostate, colorectal, and lung cancer.

Why it matters

Targeting mechanisms of resistance and tumor heterogeneity are key strategies for IDEAYA, and the company believes IDE574's novel chromatin remodeling mechanism could provide monotherapy efficacy and potentially treat breast cancer patients with ESR1 mutations who are refractory to hormone-based therapy. The dual inhibition of KAT6 and KAT7 is also expected to be more effective than selective KAT6 inhibition alone based on preclinical data.

The details

IDE574 is a selective, equipotent dual inhibitor of both KAT6 and KAT7 with single-digit to low-teen nanomolar cellular potency, while sparing other structurally similar KAT paralogs. KAT6 and KAT7 are epigenetic modulators that are corrupted by oncogenic transformation. IDE574 has demonstrated robust and durable monotherapy anti-tumor activity, superior to KAT6 inhibition alone, in preclinical models with 8p11 amplifications and ESR1 mutations, as well as in selected indications dependent on lineage-specific transcription factor activity.

  • The first patient has been enrolled in IDEAYA's Phase 1 dose escalation trial of IDE574.

The players

IDEAYA Biosciences

A precision medicine oncology company committed to developing transformative therapies for cancer, including small-molecule drugs and antibody-drug conjugates.

Michael White, Ph.D.

Chief Scientific Officer of IDEAYA Biosciences.

Yujiro S. Hata

President and Chief Executive Officer of IDEAYA Biosciences.

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What they’re saying

“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.”

— 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.”

— Yujiro S. Hata, President and Chief Executive Officer, IDEAYA Biosciences

What’s next

IDEAYA plans to evaluate the safety, efficacy, and pharmacokinetics of IDE574 as a monotherapy in the Phase 1 dose escalation trial in solid tumor patients, including those with breast, prostate, colorectal, and lung cancer.

The takeaway

IDEAYA's advancement of IDE574, a potential first-in-class dual inhibitor of KAT6 and KAT7, into Phase 1 clinical trials highlights the company's focus on developing novel targeted therapies to address mechanisms of resistance and tumor heterogeneity in solid cancers with high unmet need, such as breast, prostate, colorectal, and lung cancer.