lenvatinib mesilate: clinical use

Prescribing considerations

• Control hypertension before starting and actively manage gastrointestinal toxicity to reduce dehydration and renal injury.
• Assess cardiovascular and arterial thrombotic history, bleeding risk, major-vessel tumour involvement, fistula risk and previous surgery or radiotherapy.
• Consider hepatic and renal function, performance status, age, wound healing, dental health and concomitant anticancer treatment.

Contraindications and cautions

• Hypersensitivity to lenvatinib or an excipient.
• Breastfeeding.

Monitoring

• Blood pressure before and during treatment.
• Urinary protein and renal function.
• Liver function, with vigilance for hepatic encephalopathy in hepatocellular carcinoma.
• Thyroid function and thyroid-stimulating hormone where suppression is required.
• Electrolytes, particularly calcium, potassium and magnesium; ECG where clinically indicated.
• Evidence of cardiac dysfunction, bleeding, arterial thrombosis, fistula, perforation, dehydration, wound-healing problems, jaw osteonecrosis and tumour lysis syndrome.

Clinical pharmacology

Inhibits VEGFR1–3, FGFR1–4, PDGFRα, KIT and RET. It is rapidly absorbed, highly protein bound and extensively metabolised through CYP3A4 and non-CYP pathways; mean terminal half-life is approximately 28 hours.

Formulation and product differences

• Hard capsules can be swallowed whole or dispersed intact to prepare an oral suspension.
• Suspension for feeding-tube administration must be prepared with water. Caregivers should not open, break or crush capsules.

Capsule

Route: Oral

Strengths: 4 mg, 10 mg