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vepdegestrant + letrozole
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Vepdegestrant + letrozole is an investigational combination therapy being evaluated for the treatment of estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer. Vepdegestrant (ARV-471) is an orally bioavailable PROTAC (Proteolysis Targeting Chimera) protein degrader that specifically targets the estrogen receptor (ER). It works by recruiting an E3 ubiquitin ligase to the ER, triggering its ubiquitination and subsequent degradation by the proteasome, which effectively reduces ER protein levels in both wild-type and mutant (ESR1) forms. Letrozole is a non-steroidal aromatase inhibitor that lowers systemic estrogen levels by blocking the enzyme aromatase, which converts androgens into estrogens. This combination is currently being studied in the neoadjuvant setting, specifically within the I-SPY-2 Endocrine Optimization Platform (EOP), to assess its ability to optimize therapeutic response in patients with early-stage breast cancer.
- Other names
- ARV-471 + letrozolevepdegestrant + letrozole
02
Targets
ESR1 (ERα)CRBN (Cereblon)CYP19A1 (Aromatase)
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