Drug information of lenvatinib
Mechanism of effect
Receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4
Also inhibits other RTKs 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; the platelet-derived growth factor receptor alpha (PDGFR-alpha), KIT, and RET
Endometrial carcinoma, advanced
Hepatocellular carcinoma, unresectable
Renal cell carcinoma, advanced
Thyroid cancer, differentiated
Peak plasma time: 1-4 hr after PO administration
Administration with food does not affect the extent of absorption but can delay the mean peak plasma time from 2 hr to 4 hr
Protein bound: 98-99%
Metabolized by the CYP3A enzymes and aldehyde oxidase
Half-life: 28 hr
Excretion (10 days after single dose): 64% feces; 25% urine
Drug indicationsadvanced renal cell carcinoma , hepatocellular carcinoma , Thyroid Cancer , Endometrial Carcinoma
Endometrial carcinoma, advanced: Oral: 20 mg once daily (in combination with pembrolizumab), continue until disease progression or unacceptable toxicity .
Hepatocellular carcinoma, unresectable: Oral: 12 mg once daily (patients ≥60 kg [actual body weight]) or 8 mg once daily (patients <60 kg [actual body weight]) continue until disease progression or unacceptable toxicity.
Renal cell carcinoma, advanced: Oral: 18 mg once daily (in combination with everolimus), continue until disease progression or unacceptable toxicity .
Thyroid cancer, differentiated: Oral: 24 mg once daily until disease progression or unacceptable toxicity .
Missed doses: Do not take a missed dose within 12 hours of the next dose (if within 12 hours, skip the missed dose and return to regular administration time).
Dosage adjustment for surgery: Temporarily withhold lenvatinib treatment for at least 1 week prior to elective surgery; do not reinitiate therapy for ≥2 weeks following major surgery and until adequate wound healing.
Drug contraindicationsHypersensitivity to this drug
Hypersensitivity to lenvatinib or any component of the formulation
Side effectsDiarrhea , Proteinuria , hemorrhage , liver failure , ECG prolonged QT , renal failure , cardiac failure , tiredness , swelling of the face, mouth, hands, or feet , Fistulas
Hypertension , peripheral edema ,Fatigue , headache , voice disorder , mouth pain , dizziness , insomnia ,Palmar-plantar erythrodysesthesia , skin rash , alopecia ,Increased thyroid stimulating hormone level , weight loss , hypothyroidism , increased gamma-glutamyl transferase , hyponatremia ,Diarrhea , decreased appetite , nausea , stomatitis , vomiting , abdominal pain ,constipation , dysgeusia , xerostomia , dyspepsia ,Proteinuria , urinary tract infection , Hemorrhage ,Increased serum aspartate aminotransferase ,Arthralgia , myalgia ,Renal insufficiency ,Cough ,epistaxis ,Fever ,Hypotension , prolonged QT interval on ECG , cardiac failure , ventricular dysfunction , arterial thromboembolism , cardiac abnormality , pulmonary embolism , reduced ejection fraction ,Hyperkeratosis ,Dehydration , hypocalcemia , hypokalemia , hypercalcemia , hypercholesterolemia , hypoalbuminemia , hypoglycemia , hypomagnesemia ,Infection of mouth , increased serum lipase , increased serum amylase , gastrointestinal fistula , gastrointestinal perforation ,Thrombocytopenia , lymphocytopenia , neutropenia , anemia ,Hepatic encephalopathy , hyperbilirubinemia , increased serum alanine aminotransferase , increased serum alkaline phosphatase , hepatic failure ,Increased serum creatinine ,Pulmonary edema , pneumonia ,Aortic dissection, cholecystitis, hepatitis, nephrotic syndrome, pancreatitis, pneumothorax, reversible posterior leukoencephalopathy syndrome, tumor hemorrhage, wound healing impairment
InteractionsDolasetron , Dofetilide , Amiodarone , Olanzapine , Ondansetron , Propafenone , Pimozide , Thioridazine , lofexidine , ozogamicin , Solriamfetol , Piperaquine , Sodium Stibogluconate , encorafenib , midostaurin , Entrectinib , gilteritinib , Dasatinib , vemurafenib , sparfloxacin , Ribociclib , Inotuzumab , probucol , Halofantrine , Amisulpride , Pentamidine , Quetiapine , dronedarone , Droperidol , Osimertinib , Chloroquine , Hydroxychloroquine , Clarithromycin , Clozapine , Flecainide , escitalopram , Clofazimine , Fingolimod , Levofloxacin , Methadone , Moxifloxacin , Nilotinib , Haloperidol , Gemifloxacin , Domperidone , Doxepin , Risperidone , Citalopram , Flupentixol , ELBASVIR/GRAZOPREVIR , Bepridil , bedaquiline , Gemtuzumab , Remdesivir
(Levofloxacin-Containing Products (Systemic
QT-prolonging Agents (Indeterminate Risk – Avoid
QT-prolonging Class IA Antiarrhythmics (Highest Risk
QT-prolonging Class III Antiarrhythmics (Highest Risk
QT-prolonging Kinase Inhibitors (Highest RiskQT-prolonging Miscellaneous Agents (Highest Risk
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk
QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk
-Hypertension reported in clinical trials
-Cardiac dysfunction, defined as decreased left or right ventricular function, cardiac failure, or pulmonary edema, was reported;-
-Arterial thromboembolic events reported; discontinue drug following a thromboembolic event
-Serious hepatic adverse reactions reported
-Proteinuria reported in clinical trials
-Serious including fatal renal failure or impairment can occur with therapy
-Diarrhea may occur; initiate prompt medical management for diarrhea; monitor for dehydration; interrupt therapy for Grade 3 or 4 diarrhea
-Gastrointestinal (GI) perforation or fistula reported; discontinue if patient develops a GI perforation or life-threatening fistula
-QT prolongation reported
-Reversible posterior leukoencephalopathy syndrome (RPLS) reported rarely
-Hemorrhagic events occurred
-Impairs exogenous thyroid suppression
-Impaired wound healing been reported in patients who received therapy
- May result in reduced fertility in females of reproductive potential and damage to male reproductive tissues, leading to reduced fertility of unknown duration
Points of recommendation
-control blood pressure before treatment; monitor blood pressure after 1 week, then q2weeks for the first 2 months, and then at least monthly thereafter
- monitor for clinical symptoms or signs of cardiac decompensation
- monitor for proteinuria before initiation of, and periodically throughout, treatment;
-monitor ECG in patients with congenital long QT syndrome, CHF, bradyarrhythmias, or those who are taking drugs known to prolong the QT interval
-monitor blood calcium levels at least monthly and replace calcium as necessary during treatment
-monitor TSH levels monthly and adjust thyroid replacement medication as needed
- Advise females of reproductive potential to use effective contraception during treatment and for at least 30 days after last dose
Based on the mechanism of action and findings from animal reproduction studies, lenvatinib may cause fetal harm if administered in pregnancy.
Advise pregnant women of the potential risk to a fetus