idasanutlin

Idasanutlin (RG7388) is a potent, selective, second-generation small molecule MDM2 antagonist developed by Roche. It functions by binding to the p53-binding pocket of MDM2, thereby preventing the degradation of the p53 tumor suppressor protein. This stabilization leads to the reactivation of the p53 pathway, inducing cell cycle arrest and apoptosis in cancer cells that retain wild-type p53. Idasanutlin has been primarily investigated for the treatment of acute myeloid leukemia (AML), where it reached Phase 3 clinical trials (MIRROS study), as well as in polycythemia vera and various solid tumors. Despite its potency, the Phase 3 trial in relapsed/refractory AML did not meet its primary endpoint of improving overall survival, leading to a shift in its development focus.

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idasanutlin