Drug intelligence / Profile preview

desbutylhalofantrine

Development stage
Discontinued
Modality
Small Molecules
Administration
Intravenous
01

Overview

**Desbutylhalofantrine** is the primary active metabolite of the antimalarial drug halofantrine, formed via N-debutylation primarily by CYP3A4 and CYP2D6 enzymes. It retains potent antimalarial activity against the erythrocytic stage of Plasmodium parasites, including chloroquine-resistant strains of *P. falciparum* and *P. berghei*, by forming toxic complexes with parasite cell membranes leading to lysis. Unlike halofantrine, which carries significant cardiotoxicity risks such as QT prolongation, desbutylhalofantrine exhibits lower cardiac toxicity and has been studied in plasma from patients treated with halofantrine, where it contributes meaningfully to therapeutic efficacy with plasma concentrations correlating with treatment outcomes.

Other names
N-desbutylhalofantrine
02

Targets

Heme

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