On April 19, 2023 IDEAYA Biosciences, Inc. (NASDAQ: IDYA), a precision medicine oncology company committed to the discovery and development of targeted therapeutics, reported achievement of First-Patient-In in the Phase 1 clinical trial evaluating IDE161 (NCT 05787587) and release of a poster presentation profiling IDE161 at AACR (Free AACR Whitepaper) 2023 (Press release, Ideaya Biosciences, APR 19, 2023, View Source [SID1234630329]). 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).

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"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.

IDEAYA’s 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.

IDEAYA is planning to present a poster with preclinical data profiling IDE161 at the 2023 Annual Meeting of the American Association for Cancer Research (AACR) (Free AACR Whitepaper) on Wednesday, April 19, 2023:

Abstract 6093: "IDE161, a potential first-in-class clinical candidate PARG inhibitor, selectively targets Homologous-Recombination-Deficient and PARP inhibitor resistant breast and ovarian tumors" (Abed, M. et al.)
Date/Time: Wednesday April 19, 2023 at 9:00 am – 12:30 pm ET
Session / Location: Molecular/Cellular Biology and Genetics, Targeting DNA Damage Response and Novel Pathways; Poster Section 13, Poster Board 1
The IDE161 abstract is available online at View Source in connection with the 2023 Annual Meeting of AACR (Free AACR Whitepaper), and the poster will be available online at View Source following the presentation.

An updated corporate presentation, reflecting updates from AACR (Free AACR Whitepaper) 2023 for IDE161 (PARG), as well as for IDE397 (MAT2A), co-published with Amgen, and Werner Helicase, co-published with GSK, will also be available on the IDEAYA website at its Investor Relations page: View Source

IDEAYA owns or controls all commercial rights in IDE161, subject to certain economic obligations under its exclusive, worldwide license with Cancer Research UK and University of Manchester.