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fruquintinib
- Development stage
- Approved
- Lead developer
- HUTCHMED
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Fruquintinib is a highly selective oral small-molecule tyrosine kinase inhibitor that targets vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3. By inhibiting these receptors, fruquintinib blocks the VEGF signaling pathway essential for tumor angiogenesis—the process by which tumors develop new blood vessels to support their growth. This mechanism results in the inhibition of endothelial cell proliferation and tubule formation, thereby slowing or stopping tumor progression. Fruquintinib is primarily indicated for adults with metastatic colorectal cancer who have previously received standard chemotherapy regimens (fluoropyrimidine-, oxaliplatin-, irinotecan-based therapies), anti-VEGF therapy, and if appropriate based on RAS status, anti-EGFR therapy. The drug was developed independently in China as a next-generation VEGFR inhibitor with improved selectivity and reduced off-target toxicity compared to earlier agents.
- Brand names
- FruzaqlaElunate
- Other names
- 6-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-3-benzofurancarboxamide
02
Targets
VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR2 (Vascular endothelial growth factor receptor 2)
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