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palbociclib + vepdegestrant
- 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
01
Overview
palbociclib + vepdegestrant is an investigational combination therapy for advanced or metastatic estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer. Palbociclib is a small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in cancer cells. Vepdegestrant (ARV-471) is an oral PROteolysis Targeting Chimera (PROTAC) estrogen receptor degrader that induces targeted degradation of the estrogen receptor, thereby inhibiting ER-driven tumor growth. The combination aims to provide superior anti-tumor activity by simultaneously blocking cell proliferation and degrading the primary driver of ER+ breast cancer. It is being co-developed by Arvinas and Pfizer and has shown promising efficacy and safety in Phase 1b clinical trials among heavily pre-treated patients with advanced ER+/HER2- breast cancer[1][3][5].
- Brand names
- Ibrance
- Other names
- palbociclib + ARV-471palbociclib + PF-07850327
02
Targets
ESR1 (ERα)CDK6 (Cyclin-dependent kinase 6)PR (Progesterone receptor)KOR (Kappa opioid receptor)ESR2 (ERβ)GR (Glucocorticoid receptor)CDK4 (Cyclin-dependent kinase 4)AR (Adrenergic receptors)
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