Table 1 Selected pharmacokinetic parameters of riociguat and metabolite M1 (BAY 60-4552) by age and gender following a single oral dose of riociguat 2.5 mg
Parameter | Young female (n = 9) | Elderly female (n = 9) | Young male (n = 9) | Elderly male (n = 9) |
|---|---|---|---|---|
Riociguat | ||||
AUC, μg·h/L | 803 (55) | 1145 (36) | 750 (58) | 1036 (48) |
Cmax, μg/L | 113 (22) | 125 (35) | 80.4 (25) | 96.7 (32) |
AUCnorm, g·h/L | 24.8 (57) | 32.6 (45) | 26.5 (55) | 32.8 (50) |
Cmax,norm, g/L | 3.48 (20) | 3.56 (36) | 2.84 (23) | 3.06 (22) |
t½, h | 8.97 (51) | 11.8 (31) | 8.10 (39) | 12.2 (62) |
CLR, L/ha | 0.320 (28) | 0.223 (33) | 0.389 (37) | 0.287 (28) |
M1 | ||||
AUC, μg·h/L | 640 (26) | 651 (38) | 476 (20) | 687 (44) |
Cmax, μg/L | 28.1 (53) | 22.4 (52) | 14.9 (44) | 18.8 (71) |
AUCnorm, g·h/L | 20.5 (26) | 19.2 (30) | 17.4 (28) | 22.5 (35) |
Cmax,norm, g/L | 0.899 (51) | 0.661 (42) | 0.544 (51) | 0.615 (65) |
t½, h | 16.0 (34) | 16.7 (21) | 14.9 (28) | 21.3 (33) |
CLR, L/ha | 0.824 (32) | 0.487 (36) | 0.718 (39) | 0.573 (44) |