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ARV-473
- 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
ARV-473 is an **epimer** of vepdegestrant (ARV-471), which is investigated primarily as a metabolite in clinical studies of vepdegestrant. Both compounds are members of the PROteolysis TArgeting Chimera (PROTAC) class, designed to degrade the **estrogen receptor** (ER) in breast cancer. ARV-473 is formed in vivo after administration of vepdegestrant and displays measurable plasma concentrations and pharmacokinetic properties distinct from its parent drug. Its mechanism involves facilitating the ubiquitination and proteasomal degradation of the estrogen receptor via recruitment of an E3 ubiquitin ligase. ARV-473 is investigated for its pharmacokinetic and safety profile in patients with ER+/HER2- advanced or metastatic breast cancer, often in combination regimens[1][3][4].
- Brand names
- ARV-473ARV473ARV 473
- Other names
- ARV-473ARV473ARV 473
02
Targets
ER (Estrogen receptor)CRBN (Cereblon)
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