TABLE 1.
Total drug AUCs and Cmaxs achieved in rats compared with human reference profilesc
| Drug, dose (mg) | AUC0–ta (μg · h/ml) |
Cmax (μg/ml) |
||
|---|---|---|---|---|
| Rat | Humanb | Rat | Human | |
| GSK1322322 | ||||
| 1,000 | 28 ± 8.3 (30) | 25 ± 8.3 (34) | 9.0 ± 1.9 (21) | 10.5 ± 5.1 (49) |
| 1,500 | 41 ± 7.4 (18) | 37 ± 11 (29) | 18 ± 2.4 (14) | 20 ± 8.6 (42) |
| LVX, 500 | 37 ± 5.7 (16) | 40 | 3.6 ± 0.7 (20) | 4.3 |
| AZM, 1,000/500 | 6.5 ± 1.0 (15) | 4.9 | 0.7 ± 0.07 (10) | 0.5 |
| LZD, 625 | 135 ± 15.4 (11) | 147 | 21 ± 0.73 (3) | 17 |
a
AUC0–t, the AUC for the dosing interval (i.e., 12 h for GSK1322322 and LZD, 24 h for LVX and AZM).
b
Mean human reference profiles for GSK1322322 were calculated from data from a phase I trial of a single oral dose (10, 11); all other treatments were estimated from published oral PK data (16–18, 26).
c
The data represent means ± standard deviations (coefficient of variation [in percent]).