Table 2. Pharmacokinetic Parameters of INCB003284.
rats | dogs | monkeys | chimpanzees | ||
---|---|---|---|---|---|
iv (two animals in each species) | dose (mg/kg) | 5 | 5 | 5 | 1 |
CL (L/h/kg) | 3.4 ± 0.3 | 0.57 ± 0.02 | 0.82 ± 0.04 | 0.35 ± 0.01 | |
Vss | 10.5 ± 0.5 | 1.6 ± 0.1 | 0.7 ± 0.2 | 0.94 ± 0.03 | |
T1/2 (h) | 2.8 ± 0.2 | 3.5 ± 0.1 | 2.2 ± 0.3 | 3.8 ± 0.2 | |
po (two animals in each species) | dose (mg/kg) | 10 | 30 | 30 | 4 |
Cmax (nM) | 573 ± 120 | 7813 ± 560 | 2633 ± 320 | 1122 ± 750 | |
Tmax (h) | 4.0 ± 0.6 | 1.5 ± 0.5 | 1.5 ± 0.3 | 2.0 ± 0 | |
AUC (nM·h) | 3657 ± 560 | 33,283 ± 1215 | 9078 ± 980 | 4942 ± 3388 | |
T1/2 (h) | 2.9 ± 0.3 | 3.3 ± 0.7 | 5.1 ± 0.5 | 5.3 ± 1.0 | |
F % | 20 | 31 | 13 | 23 |