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Table 2 Summary of plasma pharmacokinetic variables of KH176

From: KH176 under development for rare mitochondrial disease: a first in man randomized controlled clinical trial in healthy male volunteers

A. For the SAD study
  SAD study
 Dose    10 mg (N = 4) 30 mg (N = 4) 100 mg (N = 4) 100 mg (N = 4) 300 mg (N = 4) 800 mg (N = 4) 2000 mg (N = 4)
 Food status    fasted fasted fasted fed fasted fasted fasted
 Cmax (ng/mL) Geomean 12.9 56.2 167 165 766 2170 5990
   CV% geomean 21.3 21.0 27.2 7.40 53.9 27.9 20.9
 tmax (h) Geomean 1.25 1.25 1.00 2.50 0.992 1.50 0.750
   CV% geomean (0.500–1.50) (0.500–1.50) (0.500–2.00) (2.00–3.00) (0.500–3.00) (1.00–1.50) (0.500–3.00)
 AUClast (h*ng/mL) Geomean 75.0 389 1310 1650 6320 21,000 61,200
   CV% geomean 14.8 8.16 16.7 1.67 20.2 27.5 9.07
 AUC0-inf (h*ng/mL) Geomean   474 1540 1970 7500 25,800 79,100
   CV% geomean   8.39 13.1 1.04 19.1 33.9 8.82
 t1/2 (h) Geomean NA 10.3 9.10 9.09 9.64 9.80 11.5
   CV% geomean   14.6 15.2 3.83 4.29 19.1 4.73
B. For the MAD study  
  MAD study
 Dose    100 mg b.i.d (n = 4) 200 mg b.i.d (n = 4) 400 mg b.i.d (n = 4)
 Day    1 7 1 7 1 7
 Cmax (ng/mL) Geomean 184 353 313 748 1330 2100
   CV% geomean 57.0 19.1 20.0 29.3 27.3 27.2
 tmax* (h) Geomean 1.25 1.00 1.75 2.00 1.00 1.50
   CV% geomean (0.500–8.00) (0.500–1.50) (1.50–2.00) (1.50–2.00) (0.500–1.50) (0.500–3.00)
 AUCtau (h*ng/mL) Geomean 1090 2760 2250 5960 6890 14,900
   CV% geomean 49.3 22.6 26.1 26.8 19.2 28.2
 Racc   Geomean   2.52   2.65   2.17
   CV% geomean   31.2   2.5   14.4
  1. Geomean geometric mean, h hour, NA not assessable, R accumulation ratio, *median (range)