Merck, SML3017-10MG, Lenvatinib mesylate

Biochem/physiol Actions
Lenvatinib (E7080) is an orally active inhibitor against multiple receptor tyrosine kinases, including VEGFR (Flt-1/KDR/Flt-4 IC50 = 22/4.0/5.2 nM), PDGFR1/2 (IC50 = 39/51 nM), FGFR1 and KIT (IC50 = 46 and 100 nM, respectively) that inhibits angiogenesis in vitro (VEGF/SCF-induced HUVEC tube formation IC50 = 5.1/5.2 nM). Lenvatinib oral administration results in tumor growth arrest (30 mg/kg b.i.d. p.o.) and even regression (100 mg/kg b.i.d. p.o.) in vivo among mice harboring SCF-producing human small cell lung carcinoma H146 cells.
Orally active receptor tyrosine kinase inhibitor against VEGFR (Flt-1/KDR/Flt-4), PDGFR1/2, FGFR1 and KIT with anti- angiogenesis efficacy in vitro and in vivo.