fruquintinib: clinical use

Prescribing considerations

• Initiation should be supervised by a clinician experienced in anticancer therapy.
• Control pre-existing hypertension before treatment.
• Review recent thromboembolism, stroke or transient ischaemic attack, aneurysm risk, infection, bleeding risk, hepatic disease, proteinuria, wounds and planned surgery.
• Use particular caution with serious bleeding, uncontrolled hypertension, impaired wound healing or arterial thrombotic risk.
• Severe hepatic impairment has not been studied and use is not recommended.
• Safety and efficacy have not been established in people under 18.

Contraindications and cautions

• Hypersensitivity to fruquintinib or any capsule excipient.

Monitoring

• Blood pressure before and throughout treatment.
• Liver function before treatment and periodically thereafter.
• Urinary protein regularly.
• Blood count and coagulation parameters, particularly when bleeding risk is increased.
• Clinical features of infection, bleeding, gastrointestinal perforation, palmar-plantar erythrodysaesthesia and posterior reversible encephalopathy syndrome.

Clinical pharmacology

Fruquintinib selectively inhibits VEGFR-1, VEGFR-2 and VEGFR-3. Oral absorption peaks at approximately two hours; protein binding is about 95% and mean elimination half-life is approximately 42 hours. Metabolism involves CYP3A and CYP2C enzymes plus non-CYP pathways.

Formulation and product differences

• The product is a hard gelatin capsule intended to be swallowed whole.
• The capsule contains tartrazine and sunset yellow, which may cause allergic reactions.
• Store in the original tightly closed bottle to protect from moisture.

Capsule

Route: Oral

Strengths: 1 mg, 5 mg