Table 1.
Summary of sitaxsentan pharmacokinetic parameters after oral administration of a single 100-mg dose to subjects with normal and impaired renal function
| Parameter | Normal | Mildly impaired | Moderately impaired | Severely impaired | P-value |
|---|---|---|---|---|---|
| Cmax (µg ml−1) | 13.9 ± 3.12 | 11.6 ± 4.01 | 10.3 ± 4.45 | 13.0 ± 6.88 | 0.4834 |
| Tmax (h) (range) | 1.00 (1.0–1.5) | 1.50 (1.0–2.5) | 1.01 (1.0–3.5) | 1.00 (0.5–1.5) | 0.9072 |
| AUC∞ (h µg−1 ml−1) | 21.8 ± 9.59 | 22.5 ± 8.64 | 18.7 ± 6.26 | 20.8 ± 10.2 | 0.3265 |
| T1/2 (h) | 9.0 ± 1.2 | 9.6 ± 1.1 | 8.6 ± 1.1 | 8.8 ± 1.5 | 0.5656 |
| CL/F (ml min−1) | 84.5 ± 34.7 | 82.3 ± 38.2 | 94.9 ± 37.3 | 88.0 ± 30.7 | 0.9310 |
| Vz/F (l) | 64.8 ± 24.0 | 65.4 ± 22.9 | 69.6 ± 28.2 | 68.3 ± 30.1 | 0.9869 |
| FU | |||||
| 1 h | 0.0133 ± 0.0012 | 0.0123 ± 0.0070 | 0.0130 ± 0.0066 | 0.0176 ± 0.0045 | – |
| 1.5 h | 0.0140 ± 0.0013 | 0.0127 ± 0.0067 | 0.0127 ± 0.0066 | 0.0174 ± 0.0026 | – |
| 2 h | 0.0117 ± 0.0058 | 0.0152 ± 0.0023 | 0.0133 ± 0.0068 | 0.0166 ± 0.0039 | – |
Results are presented as mean ± standard deviation except for Tmax for which the median is reported.