Ensem Therapeutics Reaches Milestone with CDK2 Inhibitor for Solid Tumors in Trials

Ensem Therapeutics, Inc., based in Waltham, Massachusetts, recently announced a significant milestone in its collaboration with BeiGene. BeiGene has administered the first doses of BG-68501, a cyclin-dependent kinase 2 (CDK2) inhibitor, to five patients in its initial Phase 1 clinical trial aimed at treating solid tumors. This marks the first clinical application of BG-68501, previously known as ETX-197, which was discovered using Ensem’s Kinetic Ensemble® platform—a collection of AI, machine learning, computational, and experimental tools designed to identify hidden pockets in target proteins for drug discovery.

Shengfang Jin, CEO and Co-Founder of Ensem Therapeutics, emphasized the importance of this development, noting that hyperactivity of CDK2 is a significant factor in many cancers but has been tough to target in drug discovery. Jin expressed optimism about the collaboration with BeiGene, a company renowned for its innovative clinical developments. Through this partnership, Ensem aims to test its novel approach to targeting cryptic sites, which are not apparent in static protein structures.

The ongoing Phase 1 clinical trial by BeiGene is focused on evaluating BG-68501 in patients with advanced or metastatic solid tumors that may be dependent on CDK2. These tumors include HR+/HER2- breast cancer, platinum-refractory or resistant serous ovarian cancer, fallopian tube cancer, primary peritoneal cancer, small cell lung cancer, among others, under the trial registration number NCT06257264.

Dr. Jin highlighted that the complete nonclinical development of ETX-197, from concept to Investigational New Drug (IND) submission within two years, underscores the efficacy and speed of Ensem’s platform. This rapid development cycle validates Ensem’s ability to execute projects swiftly and effectively. The company is currently progressing with multiple early-stage programs targeting cancer drivers and plans to nominate two development candidates in 2024.

Ensem Therapeutics specializes in drug discovery and development, leveraging its proprietary Kinetic Ensemble® platform. This platform combines computational techniques, AI deep learning, and advanced experimental methods to discover non-obvious binding sites and expedite the structure-based design of drugs. The company's focus is on developing precision medicines for oncology, particularly targeting high-value and difficult-to-drug molecules.