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Ref Type Journal Article
PMID (24967612)
Authors Rew Y, Sun D
Title Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer.
Journal Vol Issue Date Pages Journal Short Title
Journal of medicinal chemistry 57 15 2014 Aug 14 6332-41 J Med Chem
URL
Abstract Text We recently reported the discovery of AMG 232 (1), a potent and selective piperidinone inhibitor of the MDM2-p53 protein-protein interaction. Compound 1 is currently being evaluated in human clinical trials for the treatment of cancer. This article provides an overview of its discovery from the de novo design of the piperidinone series to the structure-activity studies leading to the identification of 1. In addition, this article also describes the preclinical pharmacology and pharmacokinetics of 1, along with its drug metabolism and safety assessment.

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Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
MDM2 amp TP53 wild-type osteosarcoma sensitive KRT-232 Preclinical Actionable In a preclinical study, KRT-232 (AMG 232) inhibited tumor growth in osteosarcoma cell line xenograft models with wild-type TP53 and MDM2 amplification (PMID: 25567130, PMID: 24967612). 24967612 25567130