Enantiospecific antitrypanosomal in vitro activity of eflornithine

Boberg, M. and Cal, M. and Kaiser, M. and Jansson-Lofmark, R. and Mäser, P. and Ashton, M.. (2021) Enantiospecific antitrypanosomal in vitro activity of eflornithine. PLoS Negl Trop Dis, 15 (7). e0009583.

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The polyamine synthesis inhibitor eflornithine is a recommended treatment for the neglected tropical disease Gambian human African trypanosomiasis in late stage. This parasitic disease, transmitted by the tsetse fly, is lethal unless treated. Eflornithine is administered by repeated intravenous infusions as a racemic mixture of L-eflornithine and D-eflornithine. The study compared the in vitro antitrypanosomal activity of the two enantiomers with the racemic mixture against three Trypanosoma brucei gambiense strains. Antitrypanosomal in vitro activity at varying drug concentrations was analysed by non-linear mixed effects modelling. For all three strains, L-eflornithine was more potent than D-eflornithine. Estimated 50% inhibitory concentrations of the three strains combined were 9.1 muM (95% confidence interval [8.1; 10]), 5.5 muM [4.5; 6.6], and 50 muM [42; 57] for racemic eflornithine, L-eflornithine and D-eflornithine, respectively. The higher in vitro potency of L-eflornithine warrants further studies to assess its potential for improving the treatment of late-stage Gambian human African trypanosomiasis.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Cal, Monica and Kaiser, Marcel and Mäser, Pascal
Item Type:Article, refereed
Article Subtype:Research Article
ISSN:1935-2735 (Electronic)1935-2727 (Linking)
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:19 Dec 2022 14:34
Deposited On:19 Dec 2022 14:34

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