Fruquintinib is a selective tyrosine kinase inhibitor that targets vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3. By inhibiting these receptors, it blocks the VEGF signaling pathway, which is a key regulator of angiogenesis—the formation of new blood vessels. This anti-angiogenic effect starves tumors of the oxygen and nutrients they need to grow.

Fruquintinib is indicated for the treatment of adult patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, as well as an anti-VEGF therapy. It is also used for a certain type of colon or rectal cancer. It is taken as an oral capsule once daily for 21 days in a row, followed by a 7-day break, which constitutes one treatment cycle. By specifically targeting the tumor's blood supply, fruquintinib offers a distinct approach to managing advanced colorectal cancer.