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. 2014 Aug;58(8):4362–4370. doi: 10.1128/AAC.02754-13

TABLE 2.

Pharmacokinetic parameters for fexinidazole, fexinidazole sulfoxide, and fexinidazole sulfone after single oral administration of fexinidazole sulfoxide or fexinidazole sulfone to uninfected mice

Drug administered and dose (mg/kg) Parameter Fexinidazole Fexinidazole sulfoxide Fexinidazole sulfone
Fexinidazole sulfoxide
    10 Cmax (μg/ml) 0.012 3.56 6.88
Tmax (h) 0.5 0.5 2.0
AUCinf (μg·h/ml) CNCa 7.68 43.4
Half-life (h) CNC 0.8 1.9
    25 Cmax (μg/ml) 0.053 13.1 14.8
Tmax (h) 0.5 0.5 2.0
AUCinf (μg·h/ml) 0.070 27.1 117
Half-life (h) 0.80 0.7 2.1
    50 Cmax (μg/ml) 0.130 21.6 35.4
Tmax (h) 0.5 0.5 2.0
AUCinf (μg·h/ml) 0.180 54.4 308
Half-life (h) 1.8 1.3 2.0
    100 Cmax (μg/ml) 0.330 32.9 58.4
Tmax (h) 0.25 0.5 4.0
AUCinf (μg·h/ml) 0.480 160 806
Half-life (h) 2.6 1.5 2.2
Fexinidazole sulfone
    10 Cmax (μg/ml) ND ND 8.48
Tmax (h) 1.0
AUCinf (μg·h/ml) 46.6
Half-life (h) 2.0
    25 Cmax (μg/ml) ND ND 21.0
Tmax (h) 1.0
AUCinf (μg·h/ml) 124
Half-life (h) 3.2
    50 Cmax (μg/ml) ND ND 33.5
Tmax (h) 2.0
AUCinf (μg·h/ml) 304
Half-life (h) 2.3
    100 Cmax (μg/ml) ND ND 67.6
Tmax (h) 2.0
AUCinf (μg·h/ml) 624
Half-life (h) 2.2
a

CNC, could not calculate; ND, not detected.