Table 2.
Summary of the plasma roxadustat pharmacokinetic parameters
| Parameter | Subjects with moderate hepatic impairment [N = 8] | Subjects with normal hepatic impairment [N = 8] |
|---|---|---|
| Pharmacokinetic parameters of total (bound and unbound) roxadustat concentration | ||
| AUC∞, ng·h/ml | 63,693 (30,947) | 49,807 (15,111) |
| C max, ng/ml | 6975 (1514) | 8498 (2203) |
| t max, ha | 2.0 (0.5–3.0) | 1.5 (1.0–2.0) |
| t ½, ha | 14.7 (10.0–30.1) | 12.6 (10.2–16.8) |
| Aelast, mg | 2.4 (1.8) | 1.6 (0.6) |
| CLR, l/h | 0.05 (0.04) | 0.03 (0.01) |
| Pharmacokinetic parameters of unbound roxadustat concentration | ||
| AUC∞,u, ng·h/ml | 708.2 (314.8) | 396.9 (94.8) |
| AUClast,u, ng·h/ml | 2.4 (1.8) | 396.0 (94.9) |
| C max,u, ng/ml | 78.4 (17.0) | 67.7 (13.4) |
| CLR,u, l/h | 4.1 (3.0) | 4.0 (1.6) |
| f u, % | 1.1 (0.16) | 0.81 (0.07) |
Data are expressed as mean (SD) unless otherwise specified
Ae last cumulative amount of drug excreted from the time of administration to the last measurable concentration, AUC last area under the concentration–time curve from the time of administration to the last measurable concentration, AUC ∞ area under the concentration–time curve from the time of drug administration to infinity, C max maximum concentration, CL R renal clearance, SD standard deviation, t ½ terminal half-life, F u fraction of unbound drug, t max time to maximum concentration, u unbound
aMedian (range)