Mouse (3.0 mg/kg) | Rat (3.0 mg/kg) | Monkey (0.08 mg/kg) | Human (1.0 mg)a | |
---|---|---|---|---|
Varenicline | ||||
AUC(0-tlast) (ng · h/ml)b | 963 | 2390 ± 610 | 210 ± 26 | 90.3 ± 6.8 |
Cmax (ng/ml) | 293 | 234 ± 55 | 19.3 ± 3.4 | 4.01 ± 0.71 |
tmax (h) | 1.0 | 1.8 ± 1.3 | 3.0 ± 1.0 | 4.3 ± 2.3 |
t1/2 (h) | 1.4 | 4.0 ± 0.9 | 24 ± 6 | 17 ± 3 |
CL/F (ml/min/kg) | 52 | 21 ± 5 | 6.3 ± 0.8 | 2.5 ± 0.2 |
Total Radioactivity: | ||||
AUC(0-tlast) (ng Eq. · h/ml)b | 1380 | 4340 ± 980 | 331 ± 34 | 114 ± 11 |
Cmax (ng Eq./ml) | 386 | 413 ± 82 | 29.0 ± 6.4 | 4.57 ± 0.47 |
tmax (h) | 1.0 | 2.4 ± 1.4 | 3.0 ± 1.0 | 2.8 ± 1.6 |
t1/2 (h) | 1.8 | 5.1 ± 0.6 | 30 ± 3 | 17 ± 2 |
Varenicline as percentage of total drug-related material | 70 | 55 | 63 | 79 |