Lenvatinib

Lenvatinib is a kinase inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvatinib inhibits other kinases that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; platelet derived growth factor receptor alpha (PDGFRA), KIT, and RET.

• LENVIMA is a kinase inhibitor that is indicated: Differentiated Thyroid Cancer (DTC) For the treatment of adult patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer (DTC). ( 1.1 ) Renal Cell Carcinoma (RCC) In combination with pembrolizumab, for the first line treatment of adult patients with advanced renal cell carcinoma (RCC).

• None. None.contraindicated

Single Agent Therapy: DTC: The recommended dosage is 24 mg orally once daily. ( 2.3 ) HCC: The recommended dosage is based on actual body weight: 12 mg orally once daily for patients greater than or equal to 60 kg or 8 mg orally once daily for patients less than 60 kg. ( 2.5 ) Combination Therapy: EC: The recommended dosage is 20 mg orally once daily in combination with pembrolizumab 200 mg administered as an intravenous infusion over 30 minutes every 3 weeks. ( 2.6 ) RCC: The recommended dosage is: 20 mg orally once daily with pembrolizumab 200 mg administered as an intravenous infusion over 30 minutes every 3 weeks. ( 2.4 ) 18 mg orally once daily with everolimus 5 mg orally once daily. ( 2.4 ) Modify the recommended daily dose for certain patients with renal or hepatic impairment. ( 2.8 , 2.9 ) 2.1 Patient Selection For the pMMR/not MSI-H advanced endometrial carcinoma indication, select patients for treatment with LENVIMA in combination with pembrolizumab based on MMR or MSI status in tumor specimens [see Clinical Studies ( 14.4 )]. Information on FDA-approved tests for patient selection is available at: http://www.fda.gov/CompanionDiagnostics . 2. 2 Important Dosage Information Reduce the dose for certain patients with renal or hepatic impairment [see Dosage and Administration ( 2.8 , 2.9 )] . Take LENVIMA once daily, with or without food, at the same time each day [see Clinical Pharmacology ( 12.3 )] . If a dose is missed and cannot be taken within 12 hours, skip that dose and take the next dose at the usual time of administration. 2.

Hypertension : Control blood pressure prior to treatment and monitor during treatment. Withhold for Grade 3 hypertension despite optimal antihypertensive therapy. Discontinue for Grade 4 hypertension. ( 2.7 , 5.1 ) Cardiac Dysfunction : Monitor for clinical symptoms or signs of cardiac dysfunction. Withhold or discontinue for Grade 3 cardiac dysfunction. Discontinue for Grade 4 cardiac dysfunction. ( 2.7 , 5.2 ) Arterial Thromboembolic Events : Discontinue following an arterial thromboembolic event. ( 2.7 , 5.3 ) Hepatotoxicity : Monitor liver function prior to treatment and periodically during treatment. Withhold or discontinue for Grade 3 or 4 hepatotoxicity. Discontinue for hepatic failure. ( 2.7 , 5.4 ) Renal Failure or Impairment : Withhold or discontinue for Grade 3 or 4 renal failure or impairment. ( 2.7 , 5.5 ) Proteinuria : Monitor for proteinuria prior to treatment and periodically during treatment. Withhold for 2 or more grams of proteinuria per 24 hours. Discontinue for nephrotic syndrome. ( 2.7 , 5.6 ) Diarrhea : May be severe and recurrent. Promptly initiate management for severe diarrhea. Withhold or discontinue based on severity. ( 2.7 , 5.7 ) Fistula Formation and Gastrointestinal Perforation : Discontinue in patients who develop Grade 3 or 4 fistula or any Grade gastrointestinal perforation. ( 2.7 , 5.8 ) QT Interval Prolongation : Monitor and correct electrolyte abnormalities. Withhold for QT interval greater than 500 ms or for 60 ms or greater increase in baseline QT interval.

The following adverse reactions are discussed elsewhere in the labeling: Hypertension [see Warnings and Precautions ( 5.1 )] Cardiac Dysfunction [see Warnings and Precautions ( 5.2 )] Arterial Thromboembolic Events [see Warnings and Precautions ( 5.3 )] Hepatotoxicity [see Warnings and Precautions ( 5.4 )] Renal Failure and Impairment [see Warnings and Precautions ( 5.5 )] Proteinuria [see Warnings and Precautions ( 5.6 )] Diarrhea [see Warnings and Precautions ( 5.7 )] Fistula Formation and Gastrointestinal Perforation [see Warnings and Precautions ( 5.8 )] QT Interval Prolongation [see Warnings and Precautions ( 5.9 )] Hypocalcemia [see Warnings and Precautions ( 5.10 )] Reversible Posterior Leukoencephalopathy Syndrome [see Warnings and Precautions ( 5.11 )] Hemorrhagic Events [see Warnings and Precautions ( 5.12 )] Impairment of Thyroid Stimulating Hormone Suppression/Thyroid Dysfunction [see Warnings and Precautions ( 5.13 )] Impaired Wound Healing [see Warnings and Precautions ( 5.14 )] Osteonecrosis of the Jaw (ONJ) [see Warnings and Precautions ( 5.15 )] In DTC, the most common adverse reactions (incidence ≥30%) for LENVIMA are hypertension, fatigue, diarrhea, arthralgia/myalgia, decreased appetite, decreased weight, nausea, stomatitis, headache, vomiting, proteinuria, palmar-plantar erythrodysesthesia syndrome, abdominal pain, and dysphonia.

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, LENVIMA can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . In animal reproduction studies, oral administration of lenvatinib during organogenesis at doses below the recommended human doses resulted in embryotoxicity, fetotoxicity, and teratogenicity in rats and rabbits ( see Data ) . There are no available human data informing the drug-associated risk. Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryofetal development study, daily oral administration of lenvatinib mesylate at doses ≥0.3 mg/kg [approximately 0.14 times the recommended clinical dose of 24 mg based on body surface area (BSA)] to pregnant rats during organogenesis resulted in dose-related decreases in mean fetal body weight, delayed fetal ossifications, and dose-related increases in fetal external (parietal edema and tail abnormalities), visceral, and skeletal anomalies. Greater than 80% post-implantation loss was observed at 1.0 mg/kg/day (approximately 0.5 times the recommended clinical dose of 24 mg based on BSA).

Metabolism

12. 3 Pharmacokinetics In patients with solid tumors administered single and multiple doses of LENVIMA once daily, the maximum lenvatinib plasma concentration (C max ) and the area under the concentration-time curve (AUC) increased proportionally over the dose range of 3.2 mg (0.1 times the recommended clinical dose of 24 mg) to 32 mg (1.33 times the recommended clinical dose of 24 mg) with a median accumulation index of 0.96 (20 mg) to 1.54 (6.4 mg).

Due to the high plasma protein binding, lenvatinib is not expected to be dialyzable [see Clinical Pharmacology ( 12.3 )] . Death due to multiorgan dysfunction occurred in a patient who received a single dose of LENVIMA 120 mg orally.

• Feb 13, 2015NDANDA206947Eisai Inc

1. 1Diarrhoea4,00513%
2. 2Hypertension3,57111%
3. 3Fatigue3,21410%
4. 4Decreased Appetite3,0519.6%
5. 5Nausea2,4017.6%
6. 6Malignant Neoplasm Progression2,3057.3%
7. 7Blood Pressure Increased2,0716.5%
8. 8Vomiting1,9356.1%
9. 9Asthenia1,5715.0%
10. 10Dehydration1,4854.7%
11. 11Weight Decreased1,4034.4%
12. 12Malaise1,2864.1%
13. 13Pyrexia1,2253.9%
14. 14Headache1,1543.6%
15. 15Hypothyroidism1,0523.3%

The 10 most recently updated of 652 ClinicalTrials.gov registrations naming Lenvatinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Evaluate Investigational Agents With or Without Pembrolizumab (MK-3475) in Participants With Advanced Esophageal Cancer Previously Exposed to Programmed Cell Death 1 Protein (PD-1)/ Programmed Cell Death Ligand 1 (PD-L1) Treatment (MK-3475-06B)
  Recruiting · Phase 1 · Phase 2 · Interventional · 230 enrolled · Merck Sharp & Dohme LLC
  NCT05319730updated 2026-06-12
• A Real-world Study of Immunotherapy Combination Regimens for Treating Liver Cancer in Cold Regions
  Active not recruiting · Observational · 1,000 enrolled · Harbin Medical University
  NCT07645209updated 2026-06-12
• Long-term Safety and Efficacy Extension Study for Participants With Advanced Tumors Who Are Currently on Treatment or in Follow-up in a Pembrolizumab (MK-3475) Study (MK-3475-587/KEYNOTE-587)
  Recruiting · Phase 3 · Interventional · 3,500 enrolled · Merck Sharp & Dohme LLC
  NCT03486873updated 2026-06-12
• Extension Study for Participants in Studies That Include Belzutifan (MK-6482-043/LITESPARK-043)
  Recruiting · Phase 3 · Interventional · 450 enrolled · Merck Sharp & Dohme LLC
  NCT07405164updated 2026-06-12
• Adding Biotherapy or Placebo to Standard Treatment for Advanced Kidney Cancer
  Recruiting · Phase 3 · Interventional · 718 enrolled · SWOG Cancer Research Network
  NCT07383441updated 2026-06-11
• The Application of Locoregional Therapy Combined With Systemic Therapy in the Perioperative Period of Huge Hepatocellular Carcinoma: A Retrospective Cohort Study
  Completed · Observational · 715 enrolled · Tongji Hospital
  NCT07639294updated 2026-06-10
• Construction and Clinical Validation of a Predictive Model for Postoperative Adjuvant Therapy in Hepatocellular Carcinoma Based on Whole-Slide Digital Pathological Images and Deep Learning
  Recruiting · Observational · 11,000 enrolled · Second Affiliated Hospital, School of Medicine, Zhejiang University
  NCT07417800updated 2026-06-10
• Study of Pembrolizumab Plus Chemotherapy With Lenvatinib for Malignant Pleural Mesothelioma
  Active not recruiting · Phase 2 · Interventional · 25 enrolled · Hyogo Medical University
  NCT06318286updated 2026-06-10
• A Study of BL-B01D1 Monotherapy, BL-B01D1 in Combination With Lenvatinib, BL-B01D1 in Combination With PD-1 Monoclonal Antibody, and BL-B01D1 in Combination With PD-1 Monoclonal Antibody and Bevacizumab in Patients With Advanced Hepatocellular Carcinoma
  Recruiting · Phase 2 · Interventional · 74 enrolled · Sichuan Baili Pharmaceutical Co., Ltd.
  NCT06986785updated 2026-06-10
• Hepatic Arterial Infusion Chemotherapy Plus Envafolimab and Lenvatinib for First-Line Unresectable Advanced Biliary Tract Cancer
  Recruiting · Phase 1 · Phase 2 · Interventional · 20 enrolled · West China Hospital
  NCT07636798updated 2026-06-09

Frequently asked questions

How does Lenvatinib work?

Lenvatinib is a kinase inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvatinib inhibits other kinases that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; platelet derived growth factor receptor alpha (PDGFRA), KIT, and RET.

What is Lenvatinib used for?

According to FDA labeling, Lenvatinib carries indications including: LENVIMA is a kinase inhibitor that is indicated: Differentiated Thyroid Cancer (DTC) For the treatment of adult patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer (DTC). ( 1.1 ) Renal Cell Carcinoma (RCC) In combination with pembrolizumab, for the first line treatment of adult patients with advanced renal cell carcinoma (RCC).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Lenvatinib?

Lenvatinib is classified as Other protein kinase inhibitors, Kinase Inhibitor, Receptor Tyrosine Kinase Inhibitors, Decreased Endothelial Proliferation.

What are the brand names for Lenvatinib?

Lenvatinib is marketed under brand names including Lenvima.

What are the contraindications for Lenvatinib?

Lenvatinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.