Table 3.
Pharmacokinetic parameters of riociguat and metabolite M1 after a single oral dose of riociguat 2.5 mg with and without coadministration of aspirin 500 mg (n = 15)
| Parameter | Riociguat | Riociguat plus aspirin |
|---|---|---|
| Riociguat | ||
| AUC, μg h/L | 566 (70.8) | 545 (80.1) |
| Cmax, μg/L | 82.6 (21.5) | 70.4 (31.9) |
| tmax, hours | 1.00 (0.500–3.00) | 1.00 (0.500–3.00) |
| t1/2, hours | 6.80 (59.8) | 6.39 (73.2) |
| Metabolite M1 | ||
| AUC, μg h/L | 504 (22.6) | 526 (28.9) |
| Cmax, μg/L | 17.3 (53.9) | 17.9 (53.2) |
| tmax, hours | 4.00 (3.00–24.0) | 6.00 (3.00–24.0) |
| t1/2, hours | 14.7 (30.2) | 14.7 (34.1) |
Note
Values are geometric means (percent coefficient of variation), except for tmax, which is given as median (range). AUC: area under the plasma concentration–time curve from time 0 to infinity; Cmax: maximum concentration in plasma; tmax: time to Cmax; t1/2: terminal elimination half-life.