Table 4.
Rat | Dog | Monkey | Human predicted | ||
---|---|---|---|---|---|
IV 1 mg/kg |
Clearance (mL/min/kg) | 24.3 ± 1.7 | 5.7 ± 1.7 | 15.2 ± 5.9 | 5.6 |
AUClast (nM·h) | 1484 ± 121 | 6640 ± 2257 | 2632 ± 926 | ||
Half-life (hour) | 2.0 ± 0.3 | 5.2 ± 1.4 | 4.0 ± 0.5 | 13 | |
MRT (hour) | 1 ± 0.2 | 6.6 ± 2.0 | 3.8 ± 0.7 | ||
Vss (L/kg) | 1.8 ± 0.5 | 2.2 ± 0.8 | 3.7 ± 1.3 | 5.2 | |
| |||||
PO suspension 5 mg/kg | AUClast (nM·h) | 3995 ± 964 | 4546 ± 2157 | 2031 ± 1038 | |
C max (nM) | 674 ± 227 | 487 ± 155 | 219 ± 94 | ||
T max (hour) | 3.3 ± 1.2 | 1.7 ± 0.6 | 2.0 ± 0 | ||
F (%) | 54% | 13% | 16% | 28% |
MRT-mean residence time; AUClast-area under the plasma concentration-time curve from zero time until the last quantifiable concentration.