Fruquintinib is a quinazoline derivative substituted with [2-methyl-3-(methylcarbamoyl)-1-benzofuran-6-yl]oxy at position 4, methoxy at position 6, and methoxy at position 7. It is a highly potent and selective inhibitor of VEGFR1, VEGFR2, and VEGFR3 (IC50 = 33, 0.35, and 35 nM), used in the treatment of metastatic colorectal cancer. It functions as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an antineoplastic agent, and a vascular endothelial growth factor receptor antagonist. It belongs to the classes of quinazolines, aromatic ethers, 1-benzofurans, and secondary carboxamides.
