Table 6. Mouse Plasma Pharmacokinetic Parameters after a Single Oral Dosea.
| parameter | 1b | 35 | 11 | 13 | 7 | 9 |
|---|---|---|---|---|---|---|
| dose (mg/kg) | 10 | 20 | 20 | 20 | 20 | 20 |
| mouse PPB (% bound) | 99.7 | 95.3 | 99.2 | 97.2c | 99.2c | 97.4 |
| Tmax (h) | 1.5 | 1 | 1 | 1 | 1 | 1 |
| apparent T1/2 (h) | 2.5 | 2.3 | 2.1 | 2.1 | 1.9 | 1.5 |
| Cmax (μM) | 3.1 (0.01) | 29 (1.4) | 8.6 (0.07) | 4.5 (0.13)c | 7.0 (0.06)c | 5.0 (0.13) |
| AUC0-inf (μM·h) | 22.6 (0.07) | 169 (7.9) | 51 (0.41) | 16.7 (0.47)c | 19.7 (0.16)c | 22.7 (0.59) |
a
Values in parentheses have been corrected for plasma protein binding and represent unbound values.
b
Average from two studies as previously reported.12
c
Protein binding in mouse plasma is an approximation based on rat and human plasma protein binding data. Calculated unbound parameters (in italics) are therefore approximations only.