On March 14, 2024 858 Therapeutics reported an upcoming poster presentation at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2024, taking place April 5-10 in San Diego, California (Press release, 858 Therapeutics, MAR 14, 2024, View Source [SID1234641186]). The presentation will describe the preclinical characterization of ETX-19477, including potent antitumor activity in multiple animal models.

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Presentation Details for AACR (Free AACR Whitepaper) 2024
Abstract Number: 2083
Title: Discovery of ETX-19477, a novel and selective PARG inhibitor with high potency against tumors with underlying replication stress
Session Title: Novel Targets and Pathways
Session Date and Time: April 8, 2024, 9:00 AM – 12:30 PM (PDT)

About ETX-19477

The company’s lead asset, ETX-19477, is a novel and potent small molecule inhibitor of PARG, a glycohydrolase that plays a pivotal role in the regulation of DNA repair mechanisms and cooperates with PARP to carry out the single-strand break repair cycle. Pharmacological inhibition of PARG results in hyperPARylation, which leads to the death of cancer cells undergoing replication stress. In multiple animal models, ETX-19477 shows potent tumor growth inhibition, and its efficacy is associated with specific biomarker-defined tumors. A Phase I clinical trial is expected to start in the first half of 2024 in patients with advanced solid tumors at multiple sites in the U.S.