amg-232

Overview

AMG-232 is an MDM2 antagonist that disrupts the p53-MDM2 interaction, stabilizing wild-type p53. It is nominated as a therapeutic candidate in tumors with MDM2 focal amplification, which enriches p53 for degradation. In TCGA melanoma analysis, MDM2 focal amplifications were enriched in the Triple-WT melanoma subtype alongside BCL2 overexpression.

Evidence in the corpus

• MDM2 focal amplifications enriched in Triple-WT melanoma subtype (14% of 318 TCGA cases; no hot-spot BRAF/RAS/NF1); AMG-232 and nutlin-3 nominated as MDM2-inhibitor strategies for MDM2-amplified, BCL2-high tumors in this subgroup PMID:26091043

Resistance mechanisms

Cancer types (linked)

• MEL

Sources

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