Drug intelligence / Profile preview

p53 hotspot mutation inhibitor

Development stage
Preclinical
Lead developer
PMV Pharmaceuticals
Modality
Small Molecules
Administration
Intratumoral Injection, Intra-arterial Infusion, Perfusion, Intravenous
01

Overview

PMV Pharmaceuticals is developing undisclosed small molecule inhibitors designed to target and reactivate various p53 hotspot mutations in solid tumors. The p53 protein is a critical tumor suppressor that is mutated in approximately half of all human cancers, often resulting in protein instability and loss of function. This preclinical program utilizes a discovery platform to identify small molecules that bind to specific mutant p53 proteins and restore their wild-type conformation and transcriptional activity, thereby inducing apoptosis in cancer cells. This approach is intended to be tumor-agnostic, targeting the specific genetic mutation rather than the tissue of origin. This program is distinct from the company's lead candidate, rezatapopt (PC14586), which specifically targets the Y220C mutation.

Other names
p53 hotspot mutation programp-53 hotspot mutation programp 53 hotspot mutation program
02

Targets

TP53 Y220C (Tumor suppressor protein p53 Y220C mutant)

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