TABLE 2.
The pharmacokinetic parameters of berzosertib in FVB wild-type and Mdr1a/b−/− Bcrp1−/− mice after administration of a single oral dose of 20 mg/kg
| Parameter | Units | Wild-Type | Mdr1a/b−/− Bcrp1−/− | ||
|---|---|---|---|---|---|
| Plasma | Brain | Plasma | Brain | ||
| t 1/2 | h | 4.1 | 5.73 | 6.22 | 7.93 |
| Tmax | h | 1 | 2 | 1 | 8 |
| C max | ng/ml | 403.8 | 200.5 | 373.7 | 2375.8 |
| AUC0-∞ | h*ng/ml | 3252 ± 245 | 2294 ± 140 | 4017 ± 211 | 55,909 ± 3359 |
| CL/F | l/h/kg | 6.14 | — | 4.98 | — |
| Vd/F | l/kg | 36.4 | — | 44.7 | — |
| Oral bioavailability | 0.67 | 0.74 | |||
CL/F, apparent clearance; Tmax, time at the maximum drug concentration; Vd/F, apparent volume of distribution.