Drug | Lot | C/M Ratioc | Kp,uu,ssd | fT,cell,ssd | |
---|---|---|---|---|---|
37°C | On ice | ||||
Diazepam | Hu8075a | 216 ± 20 | 181 ± 38 | 1.19 ± 0.51 | 0.00553 ± 0.00115 |
TFFb | 124 ± 53 | 303 ± 22 | 0.409 ± 0.247 | 0.00330 ± 0.00024 | |
Pitavastatin | Hu8075a | 471 ± 88 | 35.2 ± 2.6 | 13.4 ± 2.7 | 0.0284 ± 0.0021 |
TFFb | 150 ± 2.6 | 21.8 ± 3.2 | 6.92 ± 1.02 | 0.0460 ± 0.0068 | |
Rosuvastatin | Hu8075a | 52.2 ± 8.6 | 4.51 ± 0.41 | 11.6 ± 2.2 | 0.222 ± 0.020 |
TFFb | 27.2 ± 2.5 | 4.28 ± 0.53 | 6.36 ± 1.06 | 0.234 ± 0.029 | |
Pravastatin | Hu8075a | 3.73 ± 0.73 | 1.84 ± 0.12 | 2.03 ± 0.54 | 0.545 ± 0.035 |
TFFb | 2.65 ± 1.29 | 2.07 ± 0.64 | 1.28 ± 0.89 | 0.484 ± 0.151 |
↵a Isolated cryopreserved human hepatocytes (Lot Hu8075) were incubated with diazepam (0.2 µM), pitavastatin (0.1 µM), rosuvastatin (0.1 µM), and pravastatin (0.2 µM).
↵b Pooled cryopreserved human hepatocytes from 20 mixed-sex donors (Lot TFF) were incubated with diazepam (1 µM), pitavastatin (0.5 µM), rosuvastatin (0.5 µM), and pravastatin (1 µM).
↵c C/M ratios at 37°C and on ice were calculated using the uptake data at 30 minutes and 60 minutes, respectively (Fig. 2).
↵d The Kp,uu,ss and fT,cell,ss were calculated from C/M ratios using eqs. 2 and 3, respectively.