| Bioactivity | Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal drug. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC50s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei[1]. | ||||||||||||
| Invitro | Fexinidazole (HOE 239) has two principal metabolites, sulfoxide and sulfone. They have shown trypanocidal activity in vitro with IC50s of 0.7-3.3 μM (0.2-0.9 μg/ml) range against all parasite strains tested[1]. | ||||||||||||
| In Vivo | Fexinidazole (HOE 239; 20-50 mg/kg/day of IP or 25-100 mg/kg/day of PO; four consecutive days) has antitrypanosomal activities[1]. Animal Model: | ||||||||||||
| Name | Fexinidazole | ||||||||||||
| CAS | 59729-37-2 | ||||||||||||
| Formula | C12H13N3O3S | ||||||||||||
| Molar Mass | 279.31 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Kaiser M, et al. Antitrypanosomal activity of fexinidazole, a new oral nitroimidazole drug candidate for treatment of sleeping sickness. Antimicrob Agents Chemother. 2011 Dec;55(12):5602-8. |