WALTHAM, Mass.--(BUSINESS WIRE)--Ensem Therapeutics, Inc. (ENSEM), a pioneering drug discovery and development company that leverages its unique Kinetic Ensemble platform to advance innovative small molecule precision medicines for oncology, today announced that Dr. Shengfang Jin, Chief Executive Officer of ENSEM, will present an overview of the company and its pipeline progress at the 43rd Annual J.P. Morgan Healthcare Conference on Thursday, January 16, 2025 at 7:30 a.m. PT/ 10:30 a.m. ET.
About ETX-636
ETX-636 is a novel orally bioavailable allosteric pan-mutant-selective inhibitor and degrader of PI3Kα, which has demonstrated a dual mechanism of action, inhibition of mutant PI3Kα enzymatic activity, as well as proteosome-mediated selective degradation of mutant PI3Kα protein. The dual mechanism of action results in deep and durable pathway inhibition and induces concordant tumor regression in kinase and helical domain PI3Kα -mutant breast cancer xenografts. ETX-636 is in IND-enabling studies, with a first-in-human clinical trial anticipated to begin in the first half of 2025.
About ETX-197/BG-68501
ETX-197/BG-68501 was designed through ENSEM's Kinetic Ensemble platform to induce previously unexplored interactions within the CDK2 ATP binding pocket, leading to increased potency and selectivity compared to other CDK2 inhibitors. ETX-197/BG-68501 shows tight binding (slow off-rate) for CDK2 which results in potent and concordant pharmacodynamic modulation and anti-proliferative activity both in vitro and in vivo. BeiGene is currently conducting a first-in-human Phase 1a/1b clinical study (NCT06257264) to assess the safety tolerability, pharmacokinetics, pharmacodynamics and preliminary anti-tumor activity of ETX-197/BG-68501.
About Ensem Therapeutics
ENSEM is a pioneering drug discovery and development company that leverages its unique Kinetic Ensemble platform to advance innovative small molecule precision medicines for oncology. ENSEM integrates AI deep learning and advanced computational and cutting-edge experimental methodologies to identify non-obvious binding pockets and accelerate structure-based drug design, with a focus on high-value and difficult-to-drug targets.
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Contacts
Robert Gottlieb
RMG Associates, LLC
Info@ensemtx.com
