Table 1.
Pharmacokinetic parameters of selisistat in R6/2 mice (mean ± SD, n = 3)
| Dose (mg/kg) | 5 mg/kg | 10 mg/kg |
20 mg/kg | |
|---|---|---|---|---|
| Plasma | Brain | Plasma | Plasma | |
| Cmax (μm) | 6.9 ± 6.9 | 21.5 ± 3.3 | 10.5 ± 3.6 | 29.3 ± 6.4 |
| tmax (h) | 0.3 ± 0.1 | 1.0 ± 0.0 | 0.8 ± 0.4 | 0.5 ± 0.0 |
| AUC0–τ(last) (μm h) | 9.9 ± 4.5 | 71.1 ± 9.1 | 35.4 ± 10.4 | 77.5 ± 9.7 |
| t1/2,z (h) | 2.7 ± 2.3 | 2.8 ± 0.4 | 1.4 ± 0.5 | 0.9 ± 0.2 |
| Css,avg (μm) | 0.4 ± 0.2 | 3.0 ± 0.4 | 1.5 ± 0.4 | 3.2 ± 0.4 |
Maximal plasma concentrations (Cmax) achieved at time tmax. AUC0–τ is the area under the time versus plasma concentration curve at steady state and the Css,avg indicates the average plasma concentration, i.e. the AUC0–τ divided by the dosing interval, τ (24 h). t1/2,z is the terminal plasma half-life. Brain versus plasma was determined for 10 mg/kg only.