Products
Fexinidazole is about to be approved by the EMA in 2018 in tablet form (Fexinidazole Winthrop). This is the first new approval in this field in decades. For the first time, a peroral therapy is available. The drug has been developed since 2005 in a collaboration between DNDi (Drugs for Neglected Diseases initiative), Sanofi and partners from Africa. DNDi is a non-profit research and development organization. The active ingredient originated from a program at Hoechst in the 1970s that was not pursued further. Hoechst is now part of Sanofi.
Structure and properties
Fexinidazole (C12H13N3O3S, Mr = 279.3 g/mol) structurally belongs to the 5-nitroimidazoles. It is a prodrug that is biotransformed by CYP450 isozymes to the two active metabolites, fexinidazole sulfoxide and sulfone.
Effects
Fexinidazole has antiparasitic properties. The effects are due to the formation of reactive amines that exert toxic and mutagenic effects on parasites.
Indications
For the treatment of African trypanosomiasis with the causative agent (sleeping sickness).
Dosage
According to the SmPC. Tablets are administered once daily for 10 days.
Contraindications
For complete precautions, see the drug label.
Adverse effects
The most common possible adverse effects include vomiting, nausea, headache, weakness, dizziness, and a tremor.
