Fruquintinib — Drug Monograph

Brand names: Fruzaqla

Drug class: Tyrosine Kinase Inhibitor

Mechanism of Action

Highly selective oral small-molecule tyrosine kinase inhibitor of vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR-1/2/3). By blocking VEGF-mediated signaling, it inhibits tumor angiogenesis and vascular permeability. Its high kinase selectivity is designed to allow continuous target coverage with fewer off-target effects than less-selective multikinase VEGFR inhibitors.

FDA Indications

• Metastatic colorectal cancer 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 (FDA approved 2023)

Common Side Effects

• Hypertension
• Palmar-plantar erythrodysesthesia (hand-foot syndrome)
• Proteinuria
• Fatigue / asthenia
• Diarrhea
• Dysphonia
• Abdominal pain
• Hypothyroidism

Clinical Pearl

Fruquintinib (FRESCO-2) extends survival in heavily pretreated metastatic colorectal cancer regardless of prior regorafenib or trifluridine/tipiracil, giving a later-line antiangiogenic option. As a VEGFR TKI its class hazards dominate: control blood pressure, monitor proteinuria, and hold it around surgery for wound healing.

Related Therapies & Mechanisms

• Encorafenib (Braftovi) — Tyrosine Kinase Inhibitor · CRC
• Regorafenib (Stivarga) — Tyrosine Kinase Inhibitor · CRC
• Tucatinib (Tukysa) — Tyrosine Kinase Inhibitor · CRC
• Afatinib (Gilotrif) — Tyrosine Kinase Inhibitor