TABLE 1

The summary of kinetic parameters and expression-adjusted clearance of atorvastatin, racemic fluvastatin, pitavastatin, pravastatin, and rosuvastatin transport in BCRP, MRP2, MRP3, MRP4, MRP8, and P-gp vesicles.

The 95% confidence intervals (95% CI) for the derived parameters are presented in parentheses.

StatinTransporterVmax (95% CI)Km (95% CI)CLin vitroCLadj
pmol/min/mgμMμl/min/mgnl/min/pmol of transporter
AtorvastatinBCRP135 (92.3–258)82.4 (34.05–249)1.630.8
MRP377.0 (57.7–114)31.5 (12.3–84.2)2.468.7
P-gp32.9 (27.3–40.0)10.7 (4.34–23.1)3.1133
FluvastatinBCRP408 (313–580)25.8 (9.81–68.4)15.8298
MRP2105 (45.2–infinity)54.0 (1.92–infinity)1.949.9
MRP3170 (77.1–infinity)48.9 (2.12–infinity)3.597.6
MRP454.7 (23.4–4053)31.8 (0–infinity)1.776.4
MRP874.5 (41.6–580)73.0 (10.5–1524)1.0n/a
P-gp169 (51.6–infinity)282 (21.3–infinity)0.625.8
PitavastatinBCRP115 (98.1–137)15.8 (6.53–32.4)7.3138
MRP317.2 (10.7–29.0)8.97 (0–73.3)1.954.1
P-gp31.8 (18.3–97.4)36.6 (3.64–316)0.937.4
PravastatinMRP3n/dn/d0.25.6
RosuvastatinBCRP86.5 (71.4–106)4.24 (2.02–8.44)20.4385
MRP412.3 (5.13–infinity)39.3 (0.28–infinity)0.313.9
P-gp19.1 (11.3–51.8)46.2 (5.7–344)0.417.8