Drug intelligence / Profile preview

diloxanide

Development stage
Phase 3
Lead developer
Boots
Modality
Small Molecules
Administration
Oral
01

Overview

Diloxanide is an anti-protozoal small molecule used primarily as a luminal amebicide for the treatment of intestinal infections caused by *Entamoeba histolytica*. It is most often used as a second-line agent for asymptomatic carriers in regions where amoebiasis is uncommon and may be given after initial therapy with metronidazole or tinidazole in symptomatic cases. Diloxanide furoate, the ester form, acts as a prodrug that is hydrolyzed in the gastrointestinal tract to release active diloxanide. The drug achieves high concentrations within the intestinal lumen and works by destroying trophozoites of *E. histolytica*, thereby preventing their conversion into cysts and subsequent excretion. Its mechanism of action remains incompletely understood but may involve inhibition of protein synthesis in *E. histolytica* trophozoites due to structural similarity with chloramphenicol at its dichloroacetamide group[1][2][3][6]. Diloxanide was introduced into medical use in 1956 and appears on the World Health Organization's List of Essential Medicines[1].

Brand names
Furamide
Other names
diloxanide furoate2,2-dichloro-N-(4-hydroxyphenyl)-N-methylacetamide
02

Targets

80S ribosome (Ribosome and ribosomal components)

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