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vandetanib + fulvestrant
- Development stage
- Phase 2
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral (vandetanib), Intramuscular (fulvestrant)
01
Overview
vandetanib + fulvestrant is a combination therapy using two pharmaceutical agents: vandetanib, a multi-targeted small molecule tyrosine kinase inhibitor, and fulvestrant, an estrogen receptor antagonist. Vandetanib selectively inhibits the activity of several receptor tyrosine kinases, including VEGF receptor, EGFR, and RET, thereby blocking cell signaling pathways involved in tumor growth, angiogenesis, and progression. Fulvestrant blocks estrogen receptor (ER), reducing estrogen-driven cellular proliferation. Together, the combination targets both estrogen signaling and tyrosine kinase-mediated oncogenic signaling, achieving enhanced anti-tumor activity in cancers such as non-small cell lung cancer (NSCLC) and advanced hormone-resistant breast cancer, including models resistant to aromatase inhibitors. The rationale for the combination is based on observed cross-talk between ER and EGFR pathways, and dual inhibition achieves greater cell growth suppression and increased tumor cell apoptosis than either agent alone[1][2][3].
- Brand names
- Caprelsa (vandetanib)Faslodex (fulvestrant)
- Other names
- vandetanib + fulvestrant
02
Targets
PTK6 (Protein-tyrosine kinase 6)EGFR (Epidermal growth factor receptor)EPH (EPH receptor family)ESR1 (ERα)ESR2 (ERβ)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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