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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
agricultural and biological sciences
Efficacy of the diamidine DB75 and its prodrug DB289, against murine models of human African trypanosomiasis
Acta Tropica, Volume 108, No. 1, Year 2008
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Description
The choice of drugs for the treatment of sleeping sickness is extremely limited. To redress this situation, the recently synthesised diamidine, 2,5-bis(4-amidinophenyl)-furan (DB75, furamidine) and its methamidoxime prodrug, 2,5-bis(4-amidinophenyl)-furan-bis-O-methylamidoxime (DB289, pafuramidine) were, together with pentamidine, evaluated for efficacy in acute rodent models. The activity was compared in three common mouse models that mimic the first stage of human African trypanosomiasis. The mice were infected with the pleomorphic T .b. rhodesiense strains KETRI2537 and STIB900 or with the monomorphic T. b. brucei strain STIB795. Importantly, DB75 showed activity superior to that of pentamidine at comparable doses in all three mouse models. Complete cures were achieved with oral dosing of the prodrug DB289 in all three models without any overt toxicity. This shows that the prodrug strategy was successful in terms of reducing toxicity and increasing efficacy and oral bioavailability. © 2008 Elsevier B.V. All rights reserved.
Authors & Co-Authors
Thuita, John Kibuthu
Kenya, Nairobi
Kenya Agricultural Research Institute
Karanja, Simon Muturi
Kenya, Nairobi
Jomo Kenyatta University of Agriculture and Technology
Wenzler, Tanja
Switzerland, Allschwil
Swiss Tropical and Public Health Institute Swiss Tph
Mdachi, Raymond Ellie
Kenya, Nairobi
Kenya Agricultural Research Institute
Ngotho, Maina
Kenya, Nairobi
Kenya Agricultural Research Institute
Kagira, John Maina
Kenya, Nairobi
Kenya Agricultural Research Institute
Tidwell, Richard R.
United States, Chapel Hill
The University of North Carolina at Chapel Hill
Brun, Reto
Switzerland, Allschwil
Swiss Tropical and Public Health Institute Swiss Tph
Statistics
Citations: 90
Authors: 8
Affiliations: 4
Identifiers
Doi:
10.1016/j.actatropica.2008.07.006
ISSN:
0001706X
Research Areas
Health System And Policy