rezatapopt

Rezatapopt is a first-in-class, orally available small molecule designed to selectively bind and stabilize the TP53 Y220C mutant protein, a specific mutation in the p53 tumor suppressor gene. By binding to the crevice created by this mutation, rezatapopt restores the wild-type conformation and function of p53, reactivating its tumor-suppressive activities such as DNA binding and cell cycle regulation. This mechanism aims to disrupt tumor progression in cancers harboring the TP53 Y220C mutation. Rezatapopt is being developed primarily for patients with locally advanced or metastatic solid tumors carrying this mutation—a group that includes at least 30 different cancer types such as ovarian, lung, breast, and endometrial cancers. The drug is currently under investigation in Phase 1/2 clinical trials (notably NCT04585750) and has received Fast Track designation from the US FDA for these indications.

Other names

PMV-586PMV586PMV 586PMV-586-101PMV586-101PMV 586-101