Vepdegestrant — Investigational Agent
Selective Estrogen Receptor Degrader · Phase 3 · Arvinas / Pfizer
Mechanism of Action
Vepdegestrant is a first-in-class oral PROTAC (proteolysis-targeting chimera) that harnesses the ubiquitin-proteasome system to degrade the estrogen receptor. One end binds ER while the other recruits an E3 ubiquitin ligase, driving ER ubiquitination and catalytic degradation more completely than conventional SERDs. It degrades both wild-type and ESR1-mutant ER, removing the receptor rather than merely antagonizing it.
Investigational Indications
- ER+/HER2- advanced or metastatic breast cancer, particularly ESR1-mutant disease