Table 1.
Summary of mean pharmacokinetic parameters of basmisanil following single oral dosing across species.
| Species (n/sex) | Dose (mg/kg)a | Cmaxb (ng/mL) | Tmax (h) (range) | AUC0-lastb (ng*h/mL) | F (%) |
|---|---|---|---|---|---|
| Wistar rat (n = 2 male) | 9 | 400 | 0.5 | 1100 | 41 |
| C57/Bl6 mouse (n = 2 male) | 4 | 520 | 0.3 | 455 | 25 |
| Beagle dog (n = 3 male)c | 4 | 788 ± 275 | 1.5 (0.8–5) | 10,600 ± 2040 | 61 |
| Cynomolgus macaque (n = 3 male) | 10 | 3650 ± 110 | 1.5 (1.5–3) | 27,500 ± 8800 | 48 |
| Human (n = 6 male), SAD study BP25129 | 45 mg | 767 ± 15.4 | 3.5 (2.0–4) | 6040 ± 38.7 | ~ 75 |
| 160 mg | 1860 ± 14.3 | 4.0 (2.5–6) | 20,300 ± 38.3 | ||
| 330 mg | 2120 ± 24.0 | 4.0 (2.5–8) | 30,500 ± 20.8 |
AUC area under the concentration–time curve, Cmax maximum plasma concentration, SAD single ascending dose, F bioavailability (%), Tmax median time to reach maximum concentration.
aDose is expressed as mg/kg, except for humans where dose is expressed as mg.
bFor dog and cynomolgus macaque: ± standard deviation; for human: ± percent coefficient of variation.
cBasmisanil administered as capsule in dog, as microsuspension in rat, mouse and cynomolgus macaque, and as tablet formulation in human.