Drug intelligence / Profile preview

Fexinidazole

Development stage
Approved
Lead developer
Drugs for Neglected Diseases initiative
Modality
Small Molecules
Administration
Oral
01

Overview

Fexinidazole is an orally bioavailable nitroimidazole derivative and antiprotozoal agent used for the treatment of both first-stage (hemolymphatic) and second-stage (meningoencephalitic) human African trypanosomiasis (HAT, also known as sleeping sickness) caused by *Trypanosoma brucei gambiense* in patients aged 6 years and older weighing at least 20 kg. It is the first all-oral therapy for both stages of *T.b. gambiense* sleeping sickness[1][2][3][4][5]. The drug acts as a prodrug that is activated by parasite bacterial-like nitroreductases to form reactive intermediates capable of damaging DNA, lipids, and proteins in the parasite[2][6]. Its main metabolites are fexinidazole sulfoxide and sulfone, which are believed to be therapeutically relevant[6]. Fexinidazole was developed through a partnership including DNDi (Drugs for Neglected Diseases initiative)[4].

Brand names
Fexinidazole
02

Targets

NTR1 (Nitroreductase-1)kDNA (Kinetoplast DNA)

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