TABLE 1

Km,u, Vmax, Pdif,u, and CLint values generated for each compound in buffer and plasma incubations

CompoundIncubationKm,uVmaxPdif,uCLintKm,u Reported in the Literature
μMpmol/min per 106 cellsμl/min per 106 cellsμl/min per 106 cellsμM
PravastatinBuffer16.5 ± 4.43208 ± 14.32.59 ± 0.12812.6 ± 3.5016.5a, 29.1b, 30.5c
Plasma9.66 ± 3.2797.9 ± 8.843.94 ± 0.18010.1 ± 3.55
Fold difference1.712.120.6571.25
RosuvastatinBuffer4.00 ± 0.962323 ± 20.213.7 ± 0.62080.8 ± 20.16.05c, 9.17a
Plasma0.995 ± 0.148339 ± 15.655.4 ± 6.60341 ± 53.0
Fold difference4.020.9530.2654.22
AtorvastatinBuffer3.61 ± 1.961650 ± 20376.5 ± 1.99458 ± 2544.03c
Plasma0.115 ± 0.116272 ± 65.5741 ± 37.12370 ± 2450
Fold difference31.46.070.1035.16
PitavastatinBuffer8.71 ± 2.12600 ± 47.0132 ± 0.48168.9 ± 17.66.30c, 26.0d
Plasma0.0812 ± 0.015739.9 ± 2.45475 ± 1.53491 ± 99.7
Fold difference10715.00.2787.13
  • a Nezasa et al. (2003).

  • b Yamazaki et al. (1993).

  • c Yabe et al. (2011).

  • d Shimada et al. (2003).