PMV Pharmaceuticals, Inc. announced that the first patient has been dosed in the registrational, tumor-agnostic PYNNACLE Phase 2 trial of rezatapopt (PC14586) in patients with advanced solid tumors harboring a TP53 Y220C mutation and KRAS wild-type (WT). Rezatapopt is a first-in-class precision oncology small molecule investigational therapy that selectively targets mutated p53 Y220C proteins in solid tumors. About Rezatapopt: Rezatapopt (PC14585) is a first-in- class, small molecule, p53 reactivator designed to selectively bind to the pocket in the p53 Y220C mutant protein, restoring the wild-type, or normal, p53 protein structure and tumor-suppressing function.

The U.S. Food and Drug Administration (FDA) granted Fast Track designation to Rezatapopt for the treatment of patients with locally advanced or metastatic solid tumors with a p53 Y220C mutation. The ongoing Phase 1/2 PYNNACLE clinical trial is evaluating rezatapopt in patients with advanced solid tumors Harboring a TP53 Y220 C mutation. The primary objective of the Phase 1 portion of the trial was to determine the maximum tolerated dose and recommended Phase 2 dose (RP2D) of rezatapopt when administered orally to patients.

Safety, tolerability, pharmacokinetics and effects on biomarkers will also be assessed. The Phase 2 portion is a registrational, expansion basket clinical trial comprising five cohorts (ovarian, lung, breast, and endometrial cancers, and other solid tumors) with the primary objective of evaluating the efficacy of rezatapopt at the RP2D in patients with TP53 Y220C and KRAS wild-type advanced solid tumors.