Table 2.
Pharmacokinetic parameters in single-dose cohorts
Parameter | 25 mg, n = 5 | 50 mg, n = 5 | 100 mg, n = 5 | 200 mg, n = 5 | 400 mg, n = 5 |
---|---|---|---|---|---|
AUC0-t (ng · h/ml) | 142 ± 65 | 242 ± 80 | 1062 ± 601 | 1793 ± 408 | 3770 ± 1502 |
AUC0-∞ (ng · h/ml) | 146 ± 67 | 249 ± 81 | 1069 ± 603 | 1798 ± 407 | 3778 ± 1505 |
Cmax (ng/ml) | 55.5 ± 23.8 | 86.3 ± 42.9 | 397 ± 241 | 707 ± 211 | 1504 ± 492 |
Tmax (h) | 0.5 (0.5–1.0) | 0.5 (0.5–1.0) | 0.5 (0.3–1.0) | 0.5 (0.5–1.5) | 1.0 (0.5–1.1) |
t1/2 (h) | 2.4 ± 0.7 | 2.6 ± 1.1 | 6.1 ± 2.1 | 5.4 ± 1.4 | 6.3 ± 2.3 |
MRT (h) | 2.7 ± 0.3 | 3.0 ± 0.4 | 3.2 ± 0.3 | 2.9 ± 0.2 | 2.9 ± 0.5 |
Data are presented as mean ± sd, except for Tmax, which is presented as median (range). MRT, Mean residence time.