Table 7. Pharmacokinetic Properties of Compound 36a (BAY-069)a.
| BAY-069 (36a) | |||
|---|---|---|---|
| metabolic stability | CLblood[L/h/kg] | Fmax [%] | |
| human liver microsomes | 0.11 | 92 | |
| rat hepatocytes | 1.8 | 56 | |
| Caco-2 permeability | PappA–B[nm/s] | PappB–A [nm/s] | efflux ratio |
| 252 | 122 | 0.48 | |
| species | CLblood[L/h/kg] | Vss[L/kg] | t1/2 [h] iv | AUCnorm[kg·h/L] iv | AUCnorm[kg h/L] po | F [%] po |
|---|---|---|---|---|---|---|
| rat | 0.64 | 0.25 | 1.6 | 2.9 | 2.5 | 89 |
Doses applied to rats were 0.3 mg/kg i.v. and 0.6 mg/kg for p.o. administration.