Insights Into Vepdegestrant (ARV-471): The First-in-Class Estrogen Receptor Proteolysis-Targeting Chimera Approaching Food and Drug Administration Approval for Breast Cancer - PubMed
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- #breast cancer
- #estrogen receptor degrader
- #PROTAC
- Vepdegestrant (ARV-471) is a first-in-class estrogen receptor proteolysis-targeting chimera (PROTAC) for breast cancer treatment.
- It is an orally bioavailable PROTAC-based estrogen receptor (ER) degrader, developed for ER-positive, HER2-negative breast cancer, especially those with ESR1 mutations.
- A New Drug Application (NDA) for vepdegestrant was submitted to the FDA on June 6, 2025, marking a significant milestone in PROTAC technology.
- The review covers the design, synthesis, degradation mechanism, preclinical pharmacology, and clinical development of vepdegestrant.
- The article discusses the future prospects of oral PROTAC-based ER degraders in breast cancer therapy.