RG7112

RG7112 (RO5045337) is an orally active, small-molecule inhibitor of the MDM2-p53 interaction. It belongs to the nutlin family of compounds. By binding to the p53-binding pocket of MDM2, it prevents the degradation of p53, leading to the stabilization and activation of the p53 pathway. This induces cell cycle arrest and apoptosis in cancer cells expressing wild-type p53. It was developed by Roche for the treatment of various hematologic malignancies, including acute myeloid leukemia (AML) and chronic lymphocytic leukemia (CLL), as well as certain solid tumors like liposarcoma. While it demonstrated proof-of-concept in early trials, its development was eventually discontinued in favor of more potent second-generation MDM2 inhibitors such as idasanutlin.

Other names

MDM2 inhibitor RG7112MDM-2 inhibitor RG7112MDM 2 inhibitor RG7112RO-5045337RO5045337RO 5045337