Fruquintinib (1 brand name, 1 dosage form, 1 route)
Available dosage forms: CAPSULE.
Routes of administration: ORAL.
Brand Names
- FRUZAQLA
Indications and Usage
FRUZAQLA is indicated for the treatment of adult patients with metastatic colorectal cancer (mCRC) who have been previously treated with fluoropyrimidine‑, oxaliplatin‑, and irinotecan‑based chemotherapy, an anti‑VEGF therapy, and, if RAS wild‑type and medically appropriate, an anti-EGFR therapy.
Contraindications
None.
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: Hypertension [see Warnings and Precautions (5.1)]. Hemorrhagic Events [see Warnings and Precautions (5.2)]. Infections [see Warnings and Precautions (5.3)]. Gastrointestinal Perforation [see Warnings and Precautions (5.4)]. Hepatotoxicity [see Warnings and Precautions (5.5)]. Proteinuria [see Warnings and Precautions (5.6)]. Palmar-Plantar Erythrodysesthesia (PPE) [see Warnings and Precautions (5.7)]. Posterior Reversible Encephalopathy Syndrome (PRES) [see Warnings and Precautions (5.8)].
Mechanism of Action
Fruquintinib is a small molecule kinase inhibitor of vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3 with IC50 values of 33, 35, and 0.5 nM, respectively. In vitro studies showed fruquintinib inhibited VEGF-mediated endothelial cell proliferation and tubular formation. In vitro and in vivo studies showed fruquintinib inhibited VEGF-induced VEGFR-2 phosphorylation. In vivo studies showed fruquintinib inhibited tumor growth in a tumor xenograft mouse model of colon cancer.