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 |
CNC, could not calculate; ND, not detected.