Lenvatinib – Targeted Therapy
Lenvatinib is a potent oral multi-kinase inhibitor with significant anti-angiogenic and anti-tumor properties. The drug belongs to the class of targeted therapies and acts on a broad spectrum of receptors involved in pathological tumor growth, including vascular endothelial growth factor receptors (VEGFR1–3) and fibroblast growth factor receptors (FGFR1–4).
The mechanism of action of lenvatinib involves the simultaneous blockade of several signaling pathways. In addition to inhibiting VEGFR, the drug suppresses the activity of PDGFRα, KIT, and RET receptors. This leads to substantial inhibition of angiogenesis (the formation of new tumor blood vessels), suppression of malignant cell proliferation, and alteration of the tumor microenvironment, which together cause tumor regression and inhibit metastasis.
The drug reaches peak plasma concentrations rapidly after oral administration. The uniqueness of lenvatinib lies in its ability to bind to FGFR receptors, which helps overcome resistance to other angiogenesis inhibitors and ensures high efficacy across various types of solid tumors.
Indications
Lenvatinib is used in oncological practice for the treatment of progressive forms of cancer:
- Thyroid Cancer: therapy for progressive, locally advanced, or metastatic differentiated thyroid cancer that is refractory to radioactive iodine.
- Hepatocellular Carcinoma (HCC): first-line therapy for unresectable liver cancer.
- Renal Cell Carcinoma (RCC): in combination with everolimus or pembrolizumab for advanced kidney cancer following prior therapy.
- Endometrial Carcinoma: in combination with pembrolizumab for patients with disease progression following systemic therapy.
Dosage and administration
The dosage of lenvatinib is tailored individually based on the indication and the patient's body weight.
- Differentiated Thyroid Cancer: the recommended dose is 24 mg once daily.
- Hepatocellular Carcinoma: dose depends on body weight: 12 mg (for weight ≥60 kg) or 8 mg (for weight <60 kg) once daily.
- Administration Rules: capsules are taken at the same time every day, with or without food. They should be swallowed whole or dissolved in water/apple juice without being crushed or chewed.
- Dose Adjustment: if toxicity develops (e.g., severe hypertension or proteinuria), the dose may be reduced to 20, 14, 10, or 8 mg.
- Monitoring: regular monitoring of blood pressure, thyroid function, and urinary protein levels is mandatory during treatment.