Vepdegestrant (ARV-471)

Uses

ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. It is developed for the research of breast cancer.

Biological Activity

ARV-471 is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. It leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. ARV-471 robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of ~2 nM.

in vivo