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Table 1 The effects of ketoconazole and clarithromycin on riociguat pharmacokinetics (geometric means and coefficients of variation)

From: Pharmacokinetic interaction of ketoconazole, clarithromycin, and midazolam with riociguat

  Riociguat/ketoconazole study Riociguat/clarithromycin study
Parameter Riociguat 0.5 mg (n=16) Riociguat 0.5 mg + ketoconazole (n=16) Riociguat 1 mg (n=14) Riociguat 1 mg + clarithromycin (n=14)
  GM %CV GM %CV GM %CV GM %CV
AUC (µg·h/L) 81.9 78.6 204.9 44.9 171.1 97.0 240.0 88.9
Cmax (µg/L) 9.4 29.9 13.7 19.3 20.8 37.7 21.6 33.9
t1/2 (h) 7.3 78.5 9.2 57.1 6.4 77.1 7.9 54.6
CL/f (L/h) 6.1 78.6 2.4 44.9 5.8 97.0 4.2 88.9
  1. AUC, area under plasma concentration–time curve; CL/f, total riociguat clearance from plasma; Cmax, maximum riociguat plasma concentration; CV, coefficient of variation; GM, geometric mean; t1/2, elimination half-life.