Dose | Sample Site | Parameter | WT | Slco1a/1b−/− | Fold Difference (KO/WT) |
---|---|---|---|---|---|
15 mg/kg orally (male) | Systemic blood | cmax (μg/ml) | 0.4 | 1.2 | 3.0 |
tmax (min) | 5 | 5 | |||
AUC0–∞ (min·μg/ml) | 11.3 | 80.1 | 7.1 | ||
AUCoral/AUCi.v.* Dosei.v./Doseoral | 0.011 | 0.058 | 5.2 | ||
Half-life (min) | 89 | 74 | |||
Portal blood | AUC0–∞ (min·μg/ml) | 174 | 296 | 1.7 | |
15 mg/kg orally (female) | Systemic blood | AUC0–∞ (min·μg/ml) | 7.3 | 103.3 | 14.2 |
Half-life (min) | 67.4 | 42.7 | 0.6 | ||
5 mg/kg i.v. (male) | Systemic blood | AUC0–∞ (min·μg/ml) | 246 | 423 | 1.7 |
Clearance (ml/min/kg) | 20.3 | 11.8 | 0.58 | ||
Half-life (min) | 26.2 | 49.9 |