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ARV-471 + everolimus

Development stage: Unknown
Lead developer: Arvinas
Modality: PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration: Oral

Overview

ARV-471 (vepdegestrant) is an investigational, orally bioavailable PROTAC (proteolysis-targeting chimera) small molecule designed to selectively degrade the estrogen receptor (ER) in ER-positive breast cancer. It works by binding both the estrogen receptor and the E3 ligase cereblon, leading to ubiquitination and proteasomal degradation of ER. Everolimus is an mTOR inhibitor already approved for use in various cancers, including breast cancer. The combination of ARV-471 and everolimus is being studied for its potential synergistic effect in treating advanced or metastatic ER-positive, HER2-negative breast cancer. This combination aims to improve outcomes by targeting both hormone signaling and cell growth pathways[1][3][4][5].

Other names: vepdegestrant + everolimus

Targets

Mechanistic target of rapamycin complex 1CRL4-CRBN (Cereblon-based E3 ubiquitin ligase complex)ESR1 (ERα)

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