Abstract
The 8-aminoquinoline tafenoquine showed significant in vitro activity against Leishmania species, including L. donovani amastigotes in macrophages, with 50% inhibitory concentrations (IC(50)s) between 0.1 and 4.0 μM for both pentavalent antimony (SbV)-sensitive and SbV-resistant strains and by oral administration in BALB/c mice, with 50% effective dose (ED(50)) values of 1.2 to 3.5 mg/kg for 5 days. Tafenoquine was less active against intracellular Trypanosoma cruzi amastigotes, with an IC(50) of 21.9 μM.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aminoquinolines / pharmacology*
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Aminoquinolines / therapeutic use
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Animals
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Antiprotozoal Agents / pharmacology*
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Antiprotozoal Agents / therapeutic use
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Female
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Inhibitory Concentration 50
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Leishmania donovani / drug effects*
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Leishmaniasis / drug therapy
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Leishmaniasis / parasitology
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Macrophages / parasitology*
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Mice
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Mice, Inbred BALB C
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Primaquine / pharmacology
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Primaquine / therapeutic use
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Trypanosoma cruzi / drug effects*
Substances
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Aminoquinolines
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Antiprotozoal Agents
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tafenoquine
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Primaquine
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8-aminoquinoline