Species | Gender | Dose | Route | CLp | t1/2 | Vdss | AUC | Cmax | Tmax | CLrenal | F |
---|---|---|---|---|---|---|---|---|---|---|---|
ml · min−1 · kg−1 | h | l/kg | ng · h/ml | ng/ml | h | l/h | % | ||||
Human | M and F | 150 mg | p.o. | 8.04a | 5.6 | 3.80a | 3070 | 717 | 1.5 | 1.75 | 62.5a |
M (n = 7) | 150 mg | p.o. | 8.25a | 5.4 | 3.79a | 3070 | 672 | 1.7 | 1.86 | 61.5 | |
F (n = 3) | 150 mg | p.o. | 7.56a | 5.9 | 3.83a | 3070 | 820 | 1.1 | 1.50 | 64.7 | |
Dog | M and F | 10 mg/kg | i.v. | 8.92 | 1.8 | 1.42 | 18,100 | ||||
10 mg/kg | p.o. (fasted) | 1.3 | 1.39 | 12,200 | 3330 | 1.8 | |||||
10 mg/kg | p.o. (fed) | 1.6 | 2.64 | 8940 | 1980 | 4.5 |
p.o., oral; i.v., intravenous; CLp, plasma clearance; Vdss, steady-state distribution volume; AUC, area under the plasma concentration time curve; Cmax, maximal plasma concentration; CLrenal, renal clearance of unchanged parent compound.
↵a The calculations are based on the estimated oral bioavailability, assuming average human body weight of 70 kg.