Table 2. Pharmacokinetic parameters following single dose administration to uninfected BALB/c (benznidazole) or Swiss outbred (nifurtimox, fexinidazole, fexinidazole sulfone) mice.
| Drug | Cmax (μM) | Tmax (h) | AUC∞ (μM.h) |
|---|---|---|---|
| Benznidazole | |||
| 10 mg kg−1 | 27.0 | 0.5 | 51.1 |
| 30 mg kg−1 | 80.4 | 1.0 | 252 |
| 100 mg kg−1 | 153 | 1.0 | 726 |
| Nifurtimox | |||
| 100 mg kg−1 | 52.5 | 1.0 | 179 |
| Fexinidazole | |||
| 100 mg kg−1 | 0.30 (FX) | 0.5 (FX) | 0.94 (FX) |
| 63.3 (FXSX) | 0.5 (FXSX) | 304 (FXSX) | |
| 103 (FXS) | 2.2 (FXS) | 1300 (FXS) | |
| Fexinidazole sulfone | |||
| 100 mg kg−1 | 217 | 2.0 | 2010 |
Data for fexinidazole sulfone were taken from ref. 27. FX = fexinidazole; FXSX = fexinidazole sulfoxide; FXS = fexinidazole sulfone. Note that data for nifurtimox were generated in male mice and gender-related differences in PK properties cannot be ruled out.