Ensem Therapeutics Inc. has disclosed phosphatidylinositol 3-kinase α (PI3Kα) inhibitors, particularly PI3Kα mutant inhibitors, reported to be useful for the treatment of cancer.
Work at Ensem Therapeutics Inc. has led to the discovery of anilino-pyrazole derivatives acting as cannabinoid CB2 receptor agonists. As such, they are reported to be useful for the treatment of anxiety disorders, autoimmune disease, depression, neurodegeneration, neuroinflammation, osteoarthritis, chronic pain and substance abuse and dependence, among others.
Ensem Therapeutics Inc. has gained IND clearance from the FDA for ETX-636, a novel allosteric pan-mutant-selective PI3Kα inhibitor and degrader. A first-in-human trial will begin this quarter. The phase I/II study will evaluate ETX-636 administered alone and in combination with fulvestrant in participants with advanced solid tumors, including breast cancer, harboring a PI3Kα mutation.
In tumoral cells, the modulation of the G1/S phases of cell cycle is destabilized by amplification and high expression of cyclin E (CCNE) or by mutation or loss of retinoblastoma 1 (RB1) gene. Cancer cells meeting these characteristics have been sown to be highly sensitive to cyclin-dependent kinase 2 (CDK2) depletion.
Ensem Therapeutics Inc. has disclosed quinazoline derivatives acting as GTPase KRAS (G12D mutant) inhibitors reported to be useful for the treatment of cancer.
Beigene Ltd. and Ensem Therapeutics Inc. have announced an agreement for Beigene to acquire an exclusive global license to an IND application-ready oral cyclin-dependent kinase 2 (CDK2) inhibitor.
Two-year-old Ensem Therapeutics Inc. landed a deal potentially worth $1.33 billion, if all milestones are met, with Beigene Ltd. to advance its lead IND-ready oral cyclin-dependent kinase 2 (CDK2) inhibitor. Beigene, which has a presence in Basel, Switzerland, Beijing, and Cambridge, Mass., plans to fold the inhibitor into its breast cancer efforts, which includes its internally discovered phase I CDK4 inhibitor. Rights to the Ensem product are exclusive and global.
