TABLE 5

Kinetic parameters of lenvatinib and M2 metabolized by AO in human liver cytosol

Data represent the mean ± S.D. of triplicate determinations. Kinetic parameters are calculated using the substrate inhibition model.

ParameterLenvatinibM2
Km (μM)161.5 ± 62.51.7 ± 0.2
Vmax (pmol/min/mg)73.0 ± 22.2269.8 ± 10.1
Ki (μM)177.6 ± 96.6239.8 ± 71.6
CLint (Vmax/Km, ml/min/mg)2.2163.9