What is the use of lenvatinib mesylate?

Lenvatinib mesylate (E7080; 4-[3-chloro-4-(N′-cyclopropylureido) phenoxy] 7-methoxyquinoline-6-carboxamide mesylate) is an oral molecule that inhibits multiple tyrosine kinase receptors such as VEGF-R-1–3, FGF-R-1–4, RET, c-KIT and PDGF-R-β. 

Uses

Lenvatinib mesylate, a first-line anticancer agent for the treatment of unresectable hepatocellular carcinoma, is a BCS class II drug with low aqueous solubility. 

Lenvatinib is under investigation both as monotherapy and in combination with cytotoxic agents for multiple types of solid tumor, including thyroid carcinoma and hepatocellular carcinoma (Phase III trials) and melanoma, renal carcinoma, nonsmall cell lung carcinoma, glioblastoma multiforme and ovarian and endometrial carcinoma (Phases I and II trials). Inhibition of xenograft tumor growth by lenvatinib was observed at doses as low as 1.0 and 10.0 mg/kg, suggesting greater efficacy of this agent compared with other VEGF-R-2 inhibitors. 

Lenvatinib inhibits angiogenesis predominantly through effects on VEGF-R-2 inhibition but also through inhibition of KIT and FGF-R-1. Inhibition of VEGF-R-3 mediated lymphangiogenesis also contributed to its ability to suppress lymph node and lung metastases in a mammary tumor model.

Lenvatinib mesylate is an oral multi-targeted tyrosine kinase inhibitor that selectively inhibits the activity of several key receptors including vascular endothelial growth factor receptors (VEGFRs), fibroblast growth factor receptors (FGFRs), platelet-derived growth factor receptor α (PDGFRα), and rearranged during transfection (RET) proto-oncogene; clinically, it is approved for the treatment of various solid tumors, such as locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer, unresectable hepatocellular carcinoma, advanced renal cell carcinoma when combined with everolimus, and endometrial carcinoma when combined with pembrolizumab for patients who have disease progression following prior systemic therapy and are not candidates for curative surgery or radiation.

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