Table 2. Pharmacokinetic Parameters of 6 Following Administration to Rat, Dog, and Monkey.
| route | parameter | rat | dog | monkey |
|---|---|---|---|---|
| iva | dose (mg/kg) | 1.0 | 1.1 | 0.93 |
| Cl (mL/min/kg) (%LBF) | 27 ± 5 (35) | 9.8 ± 1.8 (18) | 6.4 ± 0.5 (15) | |
| Vdss (L/kg) | 1.8 ± 0.3 | 1.1 ± 0.2 | 1.8 ± 0.1 | |
| t1/2 (h) | 2.2 ± 0.8 | 1.7 ± 0.02 | 4.2 ± 0.6 | |
| pob | dose (mg/kg) | 2.1 | 2.0 | 1.9 |
| Tmax (h) | 0.83 ± 0.29 | 0.75 ± 0.43 | 1.5 ± 0.0 | |
| Cmax (μg/mL) | 320 ± 79 | 910 ± 130 | 770 ± 99 | |
| AUC (μg·h/mL) | 1.1 ± 0.2 | 2.5 ± 0.49 | 4.4 ± 0.5 | |
| bioavailability (%) | 84 ± 8 | 78 ± 3 | 88 ± 13 |
a
The vehicle for iv studies was 20% Cavitron, 5% DMSO in PBS.
b
The vehicle for po studies was 6% Cavitron, 5% DMSO in PBS.