Ensem Therapeutics Inc. announced that 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. 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).