Drug intelligence / Profile preview

nutlin-3

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
01

Overview

Nutlin‑3 is a small molecule experimental drug that acts as a potent and selective antagonist of the MDM2 protein. By inhibiting the interaction between MDM2 and the tumor suppressor protein p53 (encoded by TP53), Nutlin‑3 stabilizes and activates p53. This leads to cell cycle arrest and apoptosis in cancer cells with wild-type p53. Nutlin‑3 is being investigated primarily for its antitumor activity in cancers retaining functional p53—such as certain pediatric tumors and hematological malignancies—and has shown synergistic effects when combined with other chemotherapeutic agents like cisplatin or bortezomib. It is currently considered an experimental agent and has been evaluated in early-phase clinical trials for diseases such as retinoblastoma[1][6][8].

Other names
(±)-nutlin-32-piperazinone, 4-(((4r,5s)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-(4-methoxy-2-(1-methylethoxy)phenyl)-1h-imidazol-1-yl)carbonyl)-, rel-(±)-4-[4,5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-piperazin-2-one
02

Targets

MDM2 (Mouse double minute 2 homolog)

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