Fruquintinib (Elunate)

Mechanism of action

From the NCI Drug Dictionary: An orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities. Upon oral administration, fruquintinib inhibits VEGF-induced phosphorylation of VEGFRs 1, 2, and 3 which may result in the inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and tumor cell death.

Diseases for which it is established

• Colorectal cancer

History of changes in FDA indication

• 2023-11-08: Approved for adult patients with metastatic colorectal cancer (mCRC) who received prior fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if RAS wild-type and medically appropriate, an anti-EGFR therapy. (Based on FRESCO & FRESCO-2)

History of changes in NMPA indication

• 2018-09: Approved for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine, oxaliplatin and irinotecan, including those who have previously received anti-VEGF therapy and/or anti-epidermal growth factor receptor (EGFR) therapy (RAS wild type). (Based on FRESCO)

Also known as

• Code name: HMPL-013
• Brand names: Elunate, Fruzaqla