Table 2.
Parameter | Healthy subjects | Severe renal impairment vs healthy subjectsa | Moderate hepatic impairment vs healthy subjectsa | Absence vs presence of foodb,c | Co-administration with strong CYP3A4 and P-gp inhibitor vs withouta |
---|---|---|---|---|---|
Absolute bioavailability (%) | 80–100a,b | Not given | Not given | 66 vs ≥80 % | Not given |
Area under the concentration–time curve (ng/mL/h) | Approximately 1,000–1,500a | 64 % higher | 127 % higher | 39 % higher | Approximately 150 % higher |
Maximum concentration (ng/mL) | 141a–173b | 35 % higher | 27 % higher | 76 % higher | 53–72 % higher |
Time to maximum concentration (h) | 2–4 | Similar to control | Similar to control | Not given | Similar to control |
Apparent half-life (h) | 5–9 (young), 11–13 (elderly) | Similar to control | Similar to control | Not given | Similar to control |
Severe renal impairment corresponded to a creatinine clearance of <30 mL/min; moderate hepatic impairment corresponded to Child–Pugh B
CYP cytochrome P450, P-gp P-glycoprotein
a10 mg oral dose
b20 mg oral dose
cTaking 15 and 20 mg doses with food corrects pharmacokinetic parameters