Lenvatinib is a potent inhibitor of VEGF-R2 and VEGF-R3 kinase activities with IC50 values of 4.0 and 5.2 nM, respectively.. It is slightly less potent against the related receptor kinases VEGF-R1, FGF-R1, PGDFR3β and Kit (IC50 values of 22, 46, 39, and 100 nM, respectively). It is orally active, inhibiting H136 cell tumor growth in mice at 30 mg/kg.