Table 2. In Vivo Pharmacokinetic Parameters of VU2957 (7).
| parameter | mousea | rata (SD) | doga (beagle) | NHPa (cyno) |
|---|---|---|---|---|
| dose (mg/kg) iv/po | 1/3 | 0.2/3 | 0.5/3 | 0.2/3 |
| CLp (mL/min/kg) | 78.3 | 37.7 | 31.6 | 17.1 |
| Vss (L/kg) | 9.93 | 3.0 | 4.3 | 3.2 |
| elimination t1/2 (h) | 2.98 | 1.05 | 2.95 | 3.98 |
| Cmax (μM) po | 1.10 | 1.44 | 0.49 | 0.26 |
| Tmax (h) po | 0.42 | 2.0 | 1.0 | 6.0 |
| AUCo-inf (μM·h) po | 1.55 | 9.66 | 1.82 | 2.81 |
| F (%) po | 79 | 100 | 37.5 | 31.6 |
| total brain/total plasma (Kp) | 0.78 | 1.51 | ND | 1.24 |
| unbound brain/unbound plasma (Kp,uu) | 0.16 | 0.09 | ND | 0.07 |
a
Values represent means from two to three animals; ND = not determined.