halofantrine

Halofantrine is a synthetic antimalarial drug belonging to the phenanthrene class of compounds, structurally related to quinine and lumefantrine. It acts as a blood schizonticide and is used for the treatment of malaria caused by Plasmodium falciparum and Plasmodium vivax, particularly in cases where other antimalarials may not be effective due to resistance. The precise mechanism of action is not fully understood but is believed to involve inhibition of heme polymerization within the parasite, leading to toxic accumulation of free heme. Crystallographic studies suggest binding to hematin in vitro; it has also been shown to bind plasmepsin, a hemoglobin-degrading enzyme unique to malarial parasites. Halofantrine can cause significant QT interval prolongation and cardiotoxicity even at recommended doses; therefore, its use requires careful cardiac monitoring. Developed by SRI International for the Walter Reed Army Institute of Research between 1965–1975, it was later marketed under the brand name Halfan by GlaxoSmithKline[2][3][5][7][9].

Brand names

Halfan

Other names

HalofantrinaHalofantrinum3-(Dibutylamino)-1-(1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl)propan-1-ol