Lenvima

Locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer (DTC); First-line treatment of unresectable hepatocellular carcinoma (HCC); Advanced renal cell carcinoma (with pembrolizumab, first-line); Advanced endometrial carcinoma (with pembrolizumab, not MSI-H or dMMR, after prior systemic therapy)

DTC: 24 mg orally once daily
HCC: 12 mg (≥60 kg) or 8 mg (<60 kg) orally once daily
RCC (with pembrolizumab): 20 mg orally once daily
Endometrial (with pembrolizumab): 20 mg orally once daily
Take with or without food at the same time each day

Capsules: 4 mg, 10 mg

Refer to the complete prescribing information for contraindications. Lenvima prescribing should account for patient-specific factors including hypersensitivity to the active ingredient or any excipients.

• Hypertension: Reported in up to 73%. Control BP prior to treatment; monitor after 1 week, then every 2 weeks for 2 months, then monthly.
• Cardiac Dysfunction: Decreased ejection fraction and cardiac failure reported. Monitor for clinical symptoms.
• Arterial Thromboembolic Events: Discontinue following an arterial thrombotic event.
• Hepatotoxicity: Liver failure and death reported, particularly in HCC patients. Monitor LFTs before and during treatment.
• Proteinuria: Monitor with urine dipstick. Suspend for ≥2 g/24h proteinuria.
• Renal Failure/Impairment: Reported in 7% of DTC patients.
• GI Perforation/Fistula: Discontinue if occurs.
• QT Prolongation: Monitor and correct electrolytes.
• Hemorrhage: Serious and fatal hemorrhagic events reported.

Hypertension (73%), diarrhea (67%), fatigue (59%), decreased appetite (54%), decreased weight (51%), nausea (47%), stomatitis (41%), vomiting (36%), proteinuria (34%), PPE (32%), abdominal pain (31%), dysphonia (31%)

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

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

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

Lenvatinib is a receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFRα, KIT, and RET. It inhibits tumor angiogenesis through VEGFR and FGFR inhibition, suppresses tumor cell proliferation through RET and KIT inhibition, and modulates the tumor immune microenvironment.

Tmax: 1-4 hours. Half-life: approximately 28 hours. Protein binding: 98-99%. Metabolized by CYP3A and aldehyde oxidase. Excreted in feces (64%) and urine (25%).

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

• SELECT — Lenvatinib vs. placebo in radioactive iodine-refractory differentiated thyroid cancer. Phase III, n=392.
  🔬 NCT01321554 ↗ 📄 Primary Publication ↗
• REFLECT — Lenvatinib vs. sorafenib in 1L unresectable HCC. Phase III, n=954.
  🔬 NCT01761266 ↗ 📄 Primary Publication ↗

Lenvima has FDA-approved indications across the following cancer types covered on PipelineEvidence: