TABLE 1

Pharmacokinetic parameters after i.v. and PO administrations of 5 mg/kg pravastatin to FVB WT, Oatp1a/1b KO, hOATP1B1, hOATP1B3, and hOATP1B1/1B3 mice

Values are reported as the mean ± S.D. (n = 4 mice).

Mouse Linei.v. AdministrationPO Administration
CLAUC0-2hrAUC0-2hrCmax
ml/min/kgµM*hµM*hµM
Study 1
 FVB WT150 ± 22a1.32 ± 0.20a0.045 ± 0.01a0.07 ± 0.04a
 Oatp1a/1b KO36 ± 2.85.46 ± 0.400.81 ± 0.330.68 ± 0.35
 hOATP1B145 ± 9.14.50 ± 0.810.39 ± 0.06a0.39 ± 0.14
 hOATP1B356 ± 7.4a3.55 ± 0.48a0.17 ± 0.06a0.16 ± 0.05a
Study 2
 FVB WT132 ± 8.9a1.49 ± 0.11aNCNC
 Oatp1a/1b KO39 ± 3.65.07 ± 0.480.86 ± 0.220.74 ± 0.18
 hOATP1B1/1B383 ± 13a2.39 ± 0.36a0.23 ± 0.04a0.22 ± 0.07a
  • AUC0-2hr, Area under the blood concentrations-time curve from time 0 to 2 hours; CL, Blood clearance; NC, not calculated.

  • a Significantly different from Oatp1a/1b KO mice (P < 0.05).