Drug | V_{max}^{a} | K_{m}^{a} | V_{max}/K_{m} | PS_{dif}^{a} | K_{p,uu,V0}^{b} | f_{T,cell,V0}^{b} |
---|---|---|---|---|---|---|

pmol/min/10^{6} Cells | μM | μL/min/10^{6} Cells | μL/min/10^{6} Cells | |||

Pitavastatin | 893 ± 124 | 5.43 ± 1.29 | 164 ± 45 | 3.00 ± 1.41 | 55.8 ± 29.9 | 0.172 ± 0.131 |

Rosuvastatin | 250 ± 80 | 2.86 ± 1.82 | 87.4 ± 62.3 | 1.76 ± 1.15 | 50.7 ± 48.0 | 0.649 ± 0.688 |

Pravastatin | 178 ± 11 | 20.3 ± 1.4 | 8.77 ± 0.81 | 1.16 ± 0.08 | 8.56 ± 0.87 | 0.685 ± 0.428 |

↵

^{a}The initial uptake rate in rat hepatocytes was calculated from the uptake of [^{3}H]pitavastatin, [^{3}H]rosuvastatin, and [^{3}H]pravastatin for 0.5–1.5 minutes. Kinetic parameters are obtained by fitting to the data at seven concentrations (0.1, 0.3, 1, 3, 10, 30, and 100*µ*M for all statins; Supplemental Fig. 2) using eq. 4.↵

^{b}The K_{p,uu,V0}and f_{T,cell,V0}were calculated using eqs. 5 and 6, respectively. C/M ratios at 37°C (Table 2) were used for the calculation of the f_{T,cell,V0}.