Table 2.
Summary of PK parameters
| PK parametera | Participants with renal and hepatic impairment (N = 11) | Healthy controls (N = 11) |
|---|---|---|
| AUC∞ (h⋅ng/mL) | 4736 (23.12) | 2249 (19.51) |
| AUClast (h⋅ng/mL) | 4720 (23.16) | 2237 (19.53) |
| AUC0–24 (h⋅ng/mL) | 3483 (23.07) | 2032 (19.09) |
| Cmax (ng/mL) | 279.1 (29.07) | 261.3 (33.52) |
| C24 (ng/mL) | 71.11 (35.09) | 17.60 (46.00) |
| tmax (h) | 3.00 (1.50–10.00) | 1.50 (0.50–4.00) |
| t½λz (h) | 14.66 (20.94) | 9.818 (40.94) |
| λz (/h) | 0.04729 (20.94) | 0.07060 (40.94) |
| CL/F (L/h) | 1.056 (23.12) | 2.224 (19.51) |
| CLNR/F (L/h) | 0.8487 (42.97) | 0.9716 (14.72) |
| Vz/F (L) | 22.32 (36.53) | 31.50 (37.10) |
| CLR (L/h) | 0.1080 (154.0) | 1.224 (32.34) |
| Ae (0–72) (mg) | 0.5007 (147.5) | 2.740 (15.45) |
| Fe (0–72) (%) | 10.01 (147.5) | 54.80 (15.45) |
λz terminal elimination rate constant, Ae amount of unchanged drug excreted into urine, AUC area under plasma concentration-time curve, AUC0–24 AUC from time zero to 24 h, AUC∞ AUC from zero to infinity, AUClast AUC from time zero to time of last measurable concentration, C24 concentration at 24 h post-dose, CL/F apparent total body clearance of drug from plasma after extravascular administration, CLNR/F apparent total nonrenal body clearance of drug from plasma after extravascular administration, CLR renal clearance of drug from plasma, Cmax maximum plasma drug concentration, CV% percentage coefficient of variation, fe percentage of dose excreted unchanged in urine, PK pharmacokinetic, t½λz half-life associated with terminal slope of a semi-logarithmic concentration-time curve, tmax time to reach the maximum observed plasma concentration, Vz/F apparent volume of distribution during the terminal phase after extravascular administration
aData are summarised as geometric mean (CV%) except tmax is presented as median (min–max)