Table 1 Summary of mean pharmacokinetic parameters of basmisanil following single oral dosing across species.

From: Basmisanil, a highly selective GABAA-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man

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

  1. AUC area under the concentration–time curve, Cmax maximum plasma concentration, SAD single ascending dose, F bioavailability (%), Tmax median time to reach maximum concentration.
  2. aDose is expressed as mg/kg, except for humans where dose is expressed as mg.
  3. bFor dog and cynomolgus macaque: ± standard deviation; for human: ± percent coefficient of variation.
  4. cBasmisanil administered as capsule in dog, as microsuspension in rat, mouse and cynomolgus macaque, and as tablet formulation in human.
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