BAY1125976

BAY1125976 is an orally bioavailable, highly selective and potent allosteric inhibitor of the serine/threonine protein kinase AKT isoforms 1 and 2 (AKT1/2). It binds to an allosteric site formed by the kinase and PH domains of AKT1/2 in a non–ATP competitive manner. This inhibition disrupts the PI3K/AKT/mTOR signaling pathway, leading to reduced cell proliferation and increased apoptosis in tumor cells with activated AKT signaling. The drug was developed primarily for solid tumors including hormone receptor-positive metastatic breast cancer. Clinical development reached phase I trials but was discontinued after limited efficacy as monotherapy was observed. The originator is Bayer[5][4][3][7][6].

Other names

1402608-02-92-[4-(1-aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamideImidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-