Fruzaqla

Treatment of adult patients with previously treated, unresectable, metastatic colorectal cancer (mCRC) who have received prior fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if RAS wild-type and medically appropriate, an anti-EGFR therapy.

Recommended dose: 5 mg orally once daily for 3 weeks on / 1 week off (28-day cycle). Take at approximately the same time each day. Swallow capsules whole.
Dose reduction: First reduction to 4 mg once daily; second reduction to 3 mg once daily. Discontinue if unable to tolerate 3 mg daily.

Capsules: 1 mg, 5 mg

None established in prescribing information.

• Hypertension: New or worsening hypertension occurred in 56% of patients. Monitor blood pressure before initiation and regularly during treatment.
• Hepatotoxicity: Fatal hepatic failure reported. Monitor liver function tests periodically.
• Hemorrhage: Severe hemorrhagic events, including fatal cases. Withhold for Grade ≥3 hemorrhage.
• Thrombotic Events: Arterial and venous thromboembolism including MI and stroke reported.
• Gastrointestinal Perforation/Fistula: Reported. Permanently discontinue if confirmed.
• Wound Healing Complications: Withhold fruquintinib ≥2 weeks before elective surgery.
• Posterior Reversible Encephalopathy Syndrome (PRES): Reported. Confirm diagnosis with MRI; discontinue if confirmed.
• Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential to use effective contraception.

Hypertension (56%), Fatigue (28%), Palmar-plantar erythrodysesthesia (26%), Diarrhea (24%), Nausea (19%), Stomatitis (17%), Dysphonia (16%), Weight decreased (15%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Strong CYP3A4 inhibitors: Increase fruquintinib exposure; avoid concomitant use.
Strong CYP3A4 inducers: Decrease exposure; avoid concomitant use.
P-gp inhibitors: May increase fruquintinib exposure.

Can cause fetal harm. Advise females of reproductive potential to use effective contraception. Consult the full prescribing information for pregnancy risk details.

Advise women not to breastfeed during treatment and for a period after the last dose. Refer to prescribing information for duration guidance.

Safety and effectiveness in pediatric patients have not been established unless otherwise noted in the full prescribing information.

Dose modifications for organ impairment are specified in the complete prescribing information.

Fruquintinib is a highly selective, potent inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3. By blocking VEGFR-mediated signaling, it inhibits tumor angiogenesis and growth. Fruquintinib has minimal off-target activity compared to other VEGFR inhibitors.

Tmax: ~2 hours. Bioavailability: ~78%. Protein binding: ~89%. Metabolized primarily by CYP3A4. Half-life: ~40–50 hours. Elimination: primarily fecal. Steady state: by Day 15.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• FRESCO-2 — Fruquintinib vs placebo in previously treated metastatic colorectal cancer. Global Phase III, n=691.
  🔬 NCT04322539 ↗📄 Primary Publication ↗
• FRESCO — Fruquintinib vs placebo in Chinese patients with metastatic colorectal cancer. Phase III, n=416.
  🔬 NCT02314819 ↗📄 Primary Publication ↗

Fruzaqla has FDA-approved indications across the following cancer types covered on CancerDrugEvidence: