Lenvatinib is an oral, small-molecule, multi-targeted tyrosine kinase inhibitor (TKI) that selectively inhibits the kinase activities of vascular endothelial growth factor receptors (VEGFR1-3), fibroblast growth factor receptors (FGFR1-4), platelet-derived growth factor receptor alpha (PDGFRα), RET, and KIT. It is a cornerstone therapy for advanced thyroid cancer and hepatocellular carcinoma (HCC) in the Indian context, often used after failure of sorafenib in HCC.
Adult: DTC & HCC: 12 mg (for body weight ≥60 kg) or 8 mg (for body weight <60 kg) orally once daily. RCC (with pembrolizumab): 20 mg orally once daily. RCC (with everolimus): 18 mg orally once daily. The 4mg strength is used for dose titration and adjustment.
Note: Take at the same time each day, with or without food. Swallow capsule whole with a glass of water. Do not open or crush the capsule. If a dose is missed, it can be taken if less than 12 hours have passed; if more than 12 hours, skip the dose and take the next dose at the usual time. Do not take two doses to make up for a missed dose.
Lenvatinib is a multi-kinase inhibitor that potently blocks the intracellular kinase domains of multiple pro-angiogenic and oncogenic pathway receptors. Its primary antitumor activity is attributed to inhibition of VEGFR1-3 and FGFR1-4, leading to reduced tumor angiogenesis. Additional inhibition of PDGFRα, RET, and KIT contributes to direct antitumor effects and stromal modulation.
Pregnancy: Category D. Based on animal studies and mechanism, can cause fetal harm. Contraindicated. Women of childbearing potential must use effective contraception during and for at least 30 days after the final dose.
Driving: May cause fatigue, dizziness, and weakness. Patients should be cautioned about operating machinery or driving until they know how lenvatinib affects them.
| Strong CYP3A4 Inducers (e.g., Rifampicin, Phenytoin, Carbamazepine, St. John's Wort) | Decrease lenvatinib plasma concentrations, potentially reducing efficacy. | Major |
| Strong CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir) | Increase lenvatinib plasma concentrations, potentially increasing toxicity. | Major |
| Midazolam (CYP3A4 substrate) | Lenvatinib may increase midazolam exposure. | Moderate |
| Warfarin | Increased risk of bleeding due to potential pharmacodynamic interaction. Monitor INR closely. | Moderate |
| Antihypertensive Agents | Lenvatinib-induced hypertension may necessitate dose escalation of antihypertensives. | Moderate |
| Other QT-prolonging drugs (e.g., certain antiarrhythmics, antipsychotics, antibiotics) | Additive risk of QTc prolongation. | Moderate |