Ensem Therapeutics Announces Achievement of Milestone Following Entry of Small Molecule CDK2 Inhibitor into Clinical Trials for Solid Tumors

ETX-197/BG-68501 is the first clinical-stage compound discovered with ENSEM’s Kinetic Ensemble^® Platform

WALTHAM, Mass.--(BUSINESS WIRE)--Ensem Therapeutics, Inc. today announced that its partner BeiGene has dosed the first five patients in its first-in-human Phase 1 trial to evaluate BG-68501, a small molecule cyclin-dependent kinase 2 (CDK2) inhibitor for the treatment of solid tumors. The achievement triggers a milestone payment from BeiGene, which licensed the compound (formerly ETX-197) from ENSEM in November 2023. BG-68501 is the first clinical stage compound to emerge from ENSEM’s Kinetic Ensemble^® platform, a suite of novel AI/ML, computational and experimental technologies to uncover cryptic pockets in target proteins for drug discovery.

“CDK2 hyperactivity plays a well-recognized role in many cancers but has been an extremely challenging target for drug discovery,” said Shengfang Jin, CEO and Co-Founder of ENSEM. “Through our partner BeiGene, which has a proven track record of innovative clinical development, we have an initial opportunity to test our novel approach to targeting cryptic sites, which are not obvious in static protein structures.”

The Phase 1 clinical trial, conducted by BeiGene, is evaluating BG-68501 in advanced or metastatic solid tumors potentially associated with CDK2 dependency, including HR+/HER2- breast cancer, platinum refractory or resistant serous ovarian, fallopian tube, primary peritoneal cancer, small cell lung cancer, and others (NCT06257264).

“The complete nonclinical development of ETX-197 by ENSEM, from conceptualization to IND submission in two years, has validated ENSEM’s platform and demonstrated expeditious project execution,” noted Dr. Jin. ENSEM is currently advancing multiple early-stage programs targeting oncogenic drivers, anticipating nomination of two development candidates in 2024.

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 computational, AI deep learning, 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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