vepdegestrant

Vepdegestrant is an oral, heterobifunctional **PROteolysis TArgeting Chimera (PROTAC)** estrogen receptor degrader developed by **Arvinas** and **Pfizer** for **ER-positive, HER2-negative advanced or metastatic breast cancer**, particularly tumors harboring **ESR1 mutations**. The molecule is designed to bind the estrogen receptor and recruit an E3 ubiquitin ligase complex, leading to ubiquitination and subsequent proteasomal degradation of ER, thereby suppressing ER-driven tumor signaling. It was initially developed as ARV-471 under a global Arvinas/Pfizer collaboration announced in 2021, later advanced through the Phase 3 VERITAC-2 program, and received U.S. FDA approval in 2026 as **Veppanu** for adults with ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer after progression following at least one line of endocrine therapy.

Brand names

Veppanu

Other names

ARV-471 (PROTAC)Arv 471Arv471Arv-471