AMG 232

Description: AMG 232 (AMG-232; AMG232) is a novel, potent, selective, orally bioavailable and piperidinone-based inhibitor of MDM2-p53 protein-protein interaction with anticancer activity. It inhibits MDM2-p53 interaction with an IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM. AMG 232 is currently being evaluated in human clinical trials for the treatment of cancer. p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is currently in clinical trials for multiple tumor indications.