Table 3.
Primary and secondary pharmacokinetic (PK) efficacy endpoints at steady-state (Days 7–8)
| Variable | Patients (N = 11) | Healthy subjects (N = 10) | Patients : healthy subjects ratio | 90% CI |
|---|---|---|---|---|
| AUC0–24 h (µg h/l)* | 387·91 ± 134·13 | 225·35 ± 59·63 | 1·71 | 1·40; 2·07 |
| AUC0–12 h (µg h/l) | 360·16 ± 134·04 | 194·00 ± 57·42 | 1·84 | 1·49; 2·26 |
| AUC18–24 h (µg h/l) | 3·03 ± 2·71 | 6·37 ± 4·21 | 0·48 | 0·26; 0·88 |
| AUC0–8 (µg h/l) | 388·90 ± 134·07 | 228·53 ± 60·45 | 1·69 | 1·39; 2·05 |
| Cmax(µg/l) | 55·15 ± 26·87 | 27·29 ± 10·90 | 1·99 | 1·53; 2·59 |
| tmax(h) | 5·00 (3·00; 6·50) | 4·50 (3·50; 9·00) | N/A | –1·0; 1·0 |
| Cl/f (l/h) | 9·64 ± 3·61 | 16·45 ± 6·11 | 0·59 | 0·45; 0·76 |
| t1/2,z (h)† | 2·28 ± 0·43 | 3·23 ± 0·75 | 0·71 | 0·60; 0·83 |
Values are the geometric mean ± SD, except for tmax[median (minimum; maximum)].
*
Primary end-point;
†
Terminal half-life; N/A, not applicable.