Lenvatinib mesylate

Lenvatinib is an inhibitor of the receptor tyrosine kinases VEGF receptor 2 (VEGFR2) and VEGFR3 (IC₅₀s = 4 and 5.2 nM, respectively).^1,2 It also inhibits the related kinases VEGFR1, FGFR1, PDGFRα, PDGFRβ and KIT (IC₅₀s = 22, 46, 51, 39, and 100 nM, respectively).¹ Lenvatinib (30 mg/kg, twice per day) reduces tumor growth in an H146 small cell lung cancer mouse xenograft model and induces tumor regression when administered at a dose of 100 mg/kg twice per day. Formulations containing lenvatinib have been used in the treatment of differentiated thyroid cancer, renal cell carcinoma, and hepatocellular carcinoma.

1.Matsui, J., Yamamaoto, Y., Funahashi, Y., et al.E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibitionInt. J. Cancer122(3)664-671(2008) 2.Matsui, J., Funahashi, Y., Uenaka, T., et al.Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R) 2 and VEGF-R3 kinaseClin. Cancer Res.14(17)5459-5465(2008)