Fexinidazole is an antiprotozoal agent. It has activity against Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis, Entamoeba histolytica, Trypanosoma brucei, and Leishmania donovani. The biologically relevant active metabolites in vivo are the sulfoxide and sulfone. Fexinidazole was discovered by the German pharmaceutical company Hoechst AG, but its development as a pharmaceutical was halted in the 1980s. Fexinidazole is now being studied through a collaboration between Sanofi and the Drugs for Neglected Diseases Initiative (DNDi) for the treatment of Chagas disease and human African trypanosomiasis (sleeping sickness). Fexinidazole is the first drug candidate for the treatment of advanced-stage sleeping sickness in thirty years.
3D model (JSmol)
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|Molar mass||279.31 g·mol−1|
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
A clinical trial in the Democratic Republic of the Congo and the Central African Republic concluded that fexinidazole had a 91.2 success rate at treating sleeping sickness, 18 months after treatment; these results were published in the Lancet in 2017.
Fexinidazole Winthrop, a Sanofi-Aventis product developed with the DNDi, received a positive endorsement from the European Medicines Agency on November 15th, 2018, for use in non-European markets. It was approved for the treatment of Trypanosoma brucei gambiense human African trypanosomiasis (HAT) in the Democratic Republic of the Congo (DRC) in December 2018.
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- "CHMP Summary of Opinion - Fexinidazole Winthrop" (PDF). Retrieved 19 November 2018.
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- "Fexinidazole, the first all-oral treatment for sleeping sickness, approved in Democratic Republic of Congo | DNDi". Drugs for Neglected Diseases initiative (DNDi). Retrieved 2019-06-04.