Fexinidazole

Fexinidazole is a medication used to treat African trypanosomiasis (sleeping sickness) cause by "Trypanosoma brucei gambiense". It is effective against both first and second stage disease. Some evidence also supports its use in Chagas disease. It is taken by mouth.
Common side effects include nausea, vomiting, headache, and trouble sleeping. Other side effects may include QT prolongation, psychosis, and low white blood cells. It is unclear if use during pregnancy or breast feeding is safe. Fexinidazole is in the antiparasitic and the nitroimidazole family of medications. It is believed to work by turning on certain enzymes within the parasites that result in their death.
Fexinidazole was first described in 1978. It was given a positive opinion by the European Medicines Agency in 2018. It is on the World Health Organization's List of Essential Medicines, the safest and most effective medicines needed in a health system. Development for sleeping sickness was funded by the Drugs for Neglected Diseases initiative in collaboration with Sanofi.
Medical use.
Sleeping sickness.
A trial in Africa found fexinidazole to be 91% effective at treating sleeping sickness. Though less effective than nifurtimox with eflornithine in severe disease, fexinidazole has the benefit that it can be taken by mouth.
Fexinidazole is the first drug candidate for the treatment of advanced-stage sleeping sickness in thirty years.
Other.
It has activity against "Trypanosoma cruzi", "Tritrichomonas foetus", "Trichomonas vaginalis", "Entamoeba histolytica", and "Trypanosoma brucei". It has not been found to be useful for visceral leishmaniasis.
Mechanism of action.
The biologically relevant active metabolites in vivo are the sulfoxide and sulfone.
History.
Fexinidazole was discovered by the German pharmaceutical company Hoechst AG, but its development as a pharmaceutical was halted in the 1980s.
Society and culture.
Fexinidazole Winthrop, a Sanofi-Aventis product developed with the Drugs for Neglected Diseases Initiative (DNDi), received a positive endorsement from the European Medicines Agency in 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. Fexinidazole was included in the 'role of honour' in Préscrire magazine's 2020 prize list.