Drug | Lot | Kp,uu,truea | Kp,uu,V0a | Kp,uu,ssa | RV0/trueb | Rss/trueb |
---|---|---|---|---|---|---|
Pitavastatin | Hu8075 | 90.7 | 198 | 106 | 2.18 | 1.17 |
TFF | 8.35 | 18.3 | 9.75 | 2.18 | 1.17 | |
Rosuvastatin | Hu8075 | 72.4 | 199 | 71.9 | 2.74 | 0.994 |
TFF | 1.26 | 3.45 | 1.25 | 2.74 | 0.994 | |
Pravastatin | Hu8075 | 17.9 | 54.5 | 15.2 | 3.05 | 0.850 |
TFF | Not calculatedc |
↵a Theoretical values of Kp,uu,true, Kp,uu,V0, and Kp,uu,ss were calculated by Supplemental Equations 6, 8, and 11, respectively. The fi,ion, fo,ion, fi,uion, fo,uion, λ (Table 1), Vmax/Km (Table 5), and PSdif,inf,uion in each lot of human hepatocytes determined by fo,ion, fo,uion, λ, and PSdif (Table 5), according to eq. 7, were used for the calculation.
↵b RV0/true = Kp,uu,V0/ Kp,uu,true and Rss/true = Kp,uu,ss/ Kp,uu,true were calculated by eqs. 11 and 12.
↵c Not calculated for Lot TFF because kinetic parameters (Km, Vmax, and PSdif) of pravastatin were not determined (Table 5).