IDEAYA Announces First Patient Dosed in Phase 1 Clinical Trial for IDE161 as Potential First-in-Class PARG Inhibitor Targeting HRD Solid Tumors

IDEAYA Biosciences, a precision medicine oncology company committed to the discovery and development of targeted therapeutics, announced achievement of First-Patient-In in the Phase 1 clinical trial evaluating IDE161 and release of a poster presentation profiling IDE161 at AACR 2023. IDE161 is a potent, selective, small-molecule inhibitor of PARG, a novel and mechanistically-differentiated target in the same clinically validated pathway as poly (ADP-ribose) polymerase (PARP).

“We are excited to clinically investigate IDE161 as a potential first-in-class synthetic lethality treatment for cancer patients with homologous recombination deficiencies (HRD). We believe IDE161 may be impactful for ER+ / Her2- breast cancer patients with HRD, as well as for patients having ovarian cancer and other solid tumors with HRD, for whom current treatment options are limited,” said Dr. Darrin M. Beaupre, M.D., Ph.D., Chief Medical Officer, IDEAYA Biosciences. “Based on its preclinical tolerability profile, IDE161 may also be suitable for evaluation with several distinct classes of combination agents, providing multiple paths to demonstrate patient benefit in these populations,” continued Dr. Beaupre.

Dr. Timothy Yap, M.D., Ph.D., Associate Professor of Investigational Cancer Therapeutics at The University of Texas MD Anderson Cancer Center in Houston, the site which dosed the first patient, is a leading principal investigator for the Phase 1 clinical trial evaluating IDE161.

The IDEAYA Phase 1 clinical trial will evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic properties and preliminary efficacy of IDE161 as monotherapy in patients having tumors with homologous recombination deficiency (HRD). The clinical protocol includes dose escalation in solid tumors with HRD. Subject to selection of an expansion dose, the company is planning expansion in cohorts for patients having HRD tumors in breast cancer, ovarian cancer, and a basket of other solid tumors. The breast cancer cohort will focus on estrogen receptor positive (ER+), human epidermal growth factor receptor 2 negative (Her2-) tumors with HRD, which represent approximately 10% to 14% of breast cancer patients.