Table 2.
Plasma PK variables of OZ439 and its metabolites in healthy fasted subjects after administration of a single dose of 400, 800 or 1600 mg of OZ439 (oral dispersion). Values represent the geometric mean (CV%) for all parameters with the exception of tmax which is the median (range)
| Dose of OZ439 | n | Cmax (ng ml−1) | tmax (h) | AUC(0,t) (ng ml−1 h) | AUC(0,∞)* (ng ml−1 h) | t1/2* (h) |
|---|---|---|---|---|---|---|
| OZ439 | ||||||
| 400 mg | 5 | 566 (53.9) | 3.00 (2.00–4.00) | 5430 (72.0) | 5540 (71.3) | 31.2 (33.5) |
| 800 mg | 6 | 917 (35.6) | 3.00 (3.00–6.00) | 9630 (56.9) | 9790 (56.7) | 25.2 (25.8) |
| 1600 mg | 6 | 1340 (44.5) | 5.00 (2.00–6.00) | 17500 (70.1) | 18400 (68.0) | 30.7 (41.9) |
| OZ579 | ||||||
| 400 mg | 5 | 147 (31.6) | 4.00 (2.00–4.00) | 2120 (32.6) | 2210 (33.4) | 26.5 (21.0) |
| 800 mg | 6 | 165 (48.1) | 3.50 (3.00–6.00) | 2360 (35.5) | 2520 (35.2) | 28.8 (19.9) |
| 1600 mg | 6 | 193 (28.6) | 4.00 (3.00–4.00) | 3570 (15.5) | 4070 (17.4) | 38.0 (34.1) |
| OZ580 | ||||||
| 400 mg | 5 | 171 (38.2) | 6.00 (4.00–8.00) | 3680 (34.1) | 3790 (39.6) | 15.7 (28.5) |
| 800 mg | 6 | 153 (62.6) | 5.00 (4.00–8.00) | 3430 (45.6) | 3490 (45.3) | 15.6 (34.9) |
| 1600 mg | 6 | 145 (56.1) | 5.00 (4.00–8.00) | 4080 (24.8) | 4490 (22.7) | 30.3 (44.3) |
| AA3 | ||||||
| 400 mg | 5 | 63.0 (46.5) | 6.00 (4.00–8.00) | 1360 (37.4) | 1650 (14.8) | 14.2 (12.9) |
| 800 mg | 6 | 58.4 (68.2) | 4.00 (3.00–6.00) | 1290 (53.7) | 1530 (45.8) | 18.8 (25.2) |
| 1600 mg | 6 | 52.4 (57.0) | 5.00 (4.00–8.00) | 1610 (26.8) | 1830 (28.1) | 33.1 (51.6) |
*
The number of subjects may differ for the variables AUC(0,∞) and t1/2.