Ensem Therapeutics Inc. has disclosed new tetracyclic GTPase KRAS mutant inhibitors, particularly G12V mutant inhibitors, potentially useful for the treatment of cancer.
Ensem Therapeutics Inc. has presented data for ETX-929, a small-molecule, oral pan-KRAS inhibitor with potent ON and OFF dual-state inhibitory activity for both wild-type and mutant KRAS.
A recent Ensem Therapeutics Inc. patent details the discovery of tricyclic derivatives acting as GTPase KRAS (mutant) inhibitors for use in the treatment of cancer.
Ensem Therapeutics Inc. has divulged new bicyclic heteroaryl and heterocyclic compounds acting as Werner syndrome ATP-dependent helicase (WRN; RECQ3; RECQL2) inhibitors potentially useful for the treatment of cancer.
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.
