Generic
Lenvatinib Mesylate
8 brands available in the market
At a glance
Lenvatinib Mesylate is an oral receptor tyrosine kinase inhibitor used in the treatment of thyroid cancer, renal cell carcinoma (RCC), hepatocellular carcinoma (HCC), and endometrial carcinoma.
Description
Lenvatinib is a kinase inhibitor that inhibits the kinase activities of VEGF receptors VEGFR1, VEGFR2, and VEGFR3. It also inhibits other kinases such as FGF receptors FGFR1-4, PDGFR-α, KIT, and RET, which are implicated in pathogenic angiogenesis, tumor growth, and cancer progression. Lenvatinib exhibits antiproliferative activity in hepatocellular carcinoma cell lines dependent on activated FGFR signaling.
Indications
- Differentiated thyroid cancer (DTC) - locally recurrent or metastatic, radioactive iodine-refractory
- Renal cell carcinoma (RCC) - in combination with Everolimus, following prior anti-angiogenic therapy
- Hepatocellular carcinoma (HCC) - first-line treatment for unresectable HCC
- Endometrial carcinoma - in combination with Pembrolizumab (non-MSI-H or dMMR)
Therapeutic class
Cytotoxic Chemotherapy
Pharmacological class
Multi-target Tyrosine Kinase Inhibitor
Pharmacology
Lenvatinib inhibits the kinase activities of VEGFR1-3, FGFR1-4, PDGFR-α, KIT, and RET, blocking angiogenesis, tumor growth, and cancer progression.
Mechanism of action
Inhibits VEGF, FGF, and other RTK signaling to block tumor angiogenesis and cell proliferation.
Dosage
Differentiated Thyroid Cancer (DTC): 24 mg PO once daily
Renal Cell Carcinoma (RCC): 18 mg PO once daily + Everolimus 5 mg
Hepatocellular Carcinoma (HCC): ≥60 kg: 12 mg; <60 kg: 8 mg PO once daily
Endometrial Carcinoma: 20 mg PO once daily + Pembrolizumab 200 mg IV every 3 weeks
Severe Renal/Hepatic Impairment: DTC: 14 mg; RCC/Endometrial: 10 mg once daily
Administration
- Swallow capsules whole or dissolve in liquid (1 tablespoon water/apple juice for 10 minutes, stir for 3 minutes)
- Take at the same time each day, with or without food
- If a dose is missed and cannot be taken within 12 hours, skip that dose
Missed dose
If a dose is missed and cannot be taken within 12 hours, skip that dose and take the next dose at the usual time.
Side effects
Common Side Effects:
- Hypertension
- Diarrhea
- Fatigue
- Joint and muscle pain
- Nausea and vomiting
- Decreased appetite
- Weight loss
- Skin rash and peeling
- Mouth sores
- Cough, hoarseness
- Proteinuria
- Hypocalcemia
- QT interval prolongation
Precautions & warnings
- Control blood pressure; monitor after 1 week, then every 2 weeks for first 2 months, then monthly
- Monitor liver function every 2 weeks for first 2 months, then monthly
- Monitor for proteinuria
- Manage diarrhea with fluids; inform your doctor
- Risk of severe hemorrhage (tumor invasion/infiltration)
- Withhold for at least 6 days prior to surgery
- Can cause fetal harm during pregnancy
Contraindications
- Hypersensitivity to Lenvatinib or any components of the formulation
Drug interactions
- Avoid coadministration with drugs that prolong the QT interval
- Decreased exposure with CYP3A4/Pgp substrates
Food interactions
Safety with alcohol is not known; consult your doctor.
Use in pregnancy
Use in Pregnancy: Lenvatinib may be unsafe during pregnancy; animal studies have shown harmful effects on the fetus. Use effective contraception for at least 30 days after the last dose.
Use in lactation
Use in Lactation: Lenvatinib is probably unsafe during breastfeeding; may pass into breast milk. Do not breastfeed for at least 1 week after the last dose.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Safe for elderly; no special dose adjustment needed.
Renal / hepatic impairment
Renal Impairment: Severe (CrCl <30 mL/min): DTC 14 mg; RCC/Endometrial 10 mg once daily.
Hepatic Impairment: Severe (Child-Pugh C): DTC 14 mg; RCC/Endometrial 10 mg once daily.
Overdose effects
Overdose treatment: observation and supportive measures; death due to multiorgan dysfunction occurred with 120 mg single dose. Dialysis is not expected to be effective.
Storage conditions
Store below 30°C in a dry place, protected from light; keep out of reach of children.
Chemical structure
Lenvatinib Mesylate