Dose (mg/kg) | 1 | 1.3 ± 1.0 | 0.50 ± 0.10 | 0.50 ± 0.10 | 1.7 ± 0.3 | 0.78 ± 0.13 | 1.1 ± 0.2 |
| 4 | 1.3 ± 1.0 | 0.50 ± 0.10 | 0.50 ± 0.10 | 1.7 ± 0.3 | 0.79 ± 0.13 | 1.1 ± 0.2 |
Cmax,obs (ng/ml) | 1 | 1230 ± 265 | 88.9 ± 45.9 | 1860 ± 295 | 35.7 ± 31.0 | 407 ± 224 | 205 ± 120 |
| 4 | 1790 ± 104 | 343 ± 127 | 1700 ± 1570 | 342 ± 180 | 216 ± 167 | 155 ± 164 |
Tmax,obs (h) | 1 | 2.3 ± 1.3 | 0.63 ± 0.25 | 0.033 | 0.63 ± 0.25 | 0.5 | 1.1 ± 1.3 |
| 4 | 1.2 ± 0.8 | 0.5 | 0.033 | 0.75 ± 0.29 | 1.3 ± 0.6 | 1.3 ± 1.2 |
t1/2 (h) | 1 | 4.2 ± 0.8 | 2.4 ± 1.7 | 1.3 ± 0.3 | 9.0 ± 7.3 | 1.3 ± 0.4 | 4.3 ± 4.3 |
| 4 | 6.8 ± 1.2 | 1.7 ± 0.4 | 2.0 ± 0.8 | 3.2 ± 1.2 | 1.9 ± 0.2 | 2.2 ± 0.7 |
AUC0–24 (ng × h/ml) | 1 | 10800 ± 857 | 92.5 ± 50.3 | 337 ± 55 | 54.7 ± 50.6 | 525 ± 264 | 408 ± 366 |
| 4 | 17900 ± 1220 | 760 ± 313 | 871 ± 359 | 685 ± 193 | 550 ± 391 | 390 ± 403 |
Foral | | | 0.274 | | | | |
Inhibitor dose (mg/kg) | | 9.2 ± 1.1b | 22.2 ± 4.5c | 22.2 ± 4.4c | 22.2 ± 4.4c | 9.7 ± 1.6d | 11.1 ± 2.2e |
Inhibitor AUC0–24 (μg × h/ml) | 4 | 12.8 ± 2.8b | 272 ± 167c | 458 ± 314c | 379 ± 45c | 230 ± 77d | 24.3 ± 10.0e |
Inhibitor Cmax (μg/ml) | 4 | 0.864 ± 0.177b | 44.1 ± 27.3c | 42.8 ± 26.2c | 43.5 ± 16.0c | 14.4 ± 4.5d | 2.06 ± 0.73e |
Inhibitor Cavg,obs,0–24 h (μg/ml) | 4 | 0.533b | 11.3c | 19.1c | 15.8c | 9.58d | 1.01e |