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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

From: Effects of age and gender on the pharmacokinetics of the soluble guanylate cyclase stimulator riociguat

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)
  1. aArithmetic mean (percentage coefficient of variation). All other parameters are expressed as geometric means (percentage coefficient of variation).
  2. AUC, area under the plasma concentration–time curve from time 0 to infinity; AUCnorm, AUC divided by dose per kilogram of body weight; Cmax, maximum concentration in plasma; Cmax,norm, Cmax divided by dose per kilogram of body weight; t½, terminal elimination half-life; CLR, renal clearance.