Indications
Lenvatinib Mesylate (Lenvakin) is a kinase inhibitor, and it is indicated for four cancers. The first is differentiated thyroid cancer (DTC). Here it is used for patients whose disease is locally recurrent or metastatic, is progressive, and is refractory to radioactive iodine. For renal cell carcinoma (RCC), Lenvatinib Mesylate is given in combination with Everolimus. It is indicated for patients with advanced RCC who have already had one prior anti-angiogenic therapy. In hepatocellular carcinoma (HCC), the medicine is indicated as first-line treatment for patients whose disease is unresectable. The last indication is endometrial carcinoma. Lenvatinib Mesylate is used in combination with Pembrolizumab for patients with advanced endometrial carcinoma that is not microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR). These patients must have disease progression following prior systemic therapy and must not be candidates for curative surgery or radiation.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Lenvatinib is a kinase inhibitor. It blocks the kinase activity of the vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR) and VEGFR3 (FLT4). It also blocks other kinases that are linked to pathogenic angiogenesis, tumor growth and cancer progression, besides their normal work in the cell. These include the fibroblast growth factor (FGF) receptors FGFR1, 2, 3 and 4, platelet-derived growth factor receptor alpha (PDGFR ), KIT and RET. In hepatocellular carcinoma cell lines that depend on activated FGFR signaling, Lenvatinib also showed antiproliferative activity, along with inhibition of FGF-receptor substrate 2 (FRS2 ) phosphorylation.
Absorption: The time to peak plasma concentration (Tmax) was typically 1 to 4 hours after the dose. A high-fat meal (approximately 900 calories, of which approximately 55% came from fat, 15% from protein and 30% from carbohydrates) did not change the extent of absorption. It did slow the rate of absorption, and the median Tmax moved from 2 hours to 4 hours.
Distribution: In vitro, Lenvatinib binding to human plasma proteins ranged from 98% to 99% at concentrations of 0.3 to 30 μg/mL. The blood-to-plasma concentration ratio ranged from 0.59 to 0.61 at concentrations of 0.1 to 10 μg/mL in vitro.
Metabolism: In humans, the main metabolic pathways for Lenvatinib were enzymatic (CYP3A and aldehyde oxidase) and non-enzymatic processes.
Excretion: Ten days after a single dose of radiolabeled Lenvatinib, approximately 64% of the radiolabel had left in the feces and approximately 25% in the urine.
Elimination: The terminal elimination half-life of Lenvatinib was approximately 28 hours.
Pregnancy & Breastfeeding
Use in Pregnancy: Going by how Lenvatinib works, it can harm the embryo and fetus when given to a pregnant woman. Pregnant women should be told about the possible risk to the baby. Women who could become pregnant should be advised to use effective contraception while taking Lenvatinib and for at least 30 days after the last dose.
Use in Lactation: It isn't known whether Lenvatinib passes into human milk. Because breastfed infants could have serious adverse reactions, women should be advised to stop breastfeeding during treatment with Lenvatinib and for at least 1 week after the last dose.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.