fruquintinib + raltitrexed

Fruquintinib + raltitrexed is an investigational combination therapy for metastatic colorectal cancer (mCRC), particularly in patients who have failed standard first- and second-line treatments. Fruquintinib is a highly selective small molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, thereby inhibiting tumor angiogenesis. Raltitrexed is a thymidylate synthase inhibitor that disrupts DNA synthesis in rapidly dividing cells by blocking the formation of thymidine monophosphate, an essential precursor for DNA replication. The combination aims to leverage complementary mechanisms—targeted anti-angiogenic activity from fruquintinib and cytotoxic antimetabolite action from raltitrexed—to improve tumor response rates and progression-free survival in heavily pretreated mCRC patients[1][2][3][7].