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In Vitro and In Vivo Evaluation of 28DAP010, a Novel Diamidine for Treatment of Second-Stage African Sleeping Sickness
Wenzler, Tanja Yang, Sihyung Patrick, Donald A. Braissant, Olivier Ismail, Mohamed A. Tidwell, Richard R. Boykin, David W. Wang, Zhuo Brun, Reto
Wenzler, Tanja
Yang, Sihyung
Patrick, Donald A.
Braissant, Olivier
Ismail, Mohamed A.
Tidwell, Richard R.
Boykin, David W.
Wang, Zhuo
Brun, Reto
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Abstract
African sleeping sickness is a neglected tropical disease transmitted by tsetse flies. New and better drugs are still needed especially for its second stage, which is fatal if untreated. 28DAP010, a dipyridylbenzene analogue of DB829, is the second simple diamidine found to cure mice with central nervous system infections by a parenteral route of administration. 28DAP010 showed efficacy similar to that of DB829 in dose-response studies in mouse models of first- and second-stage African sleeping sickness. The in vitro time to kill, determined by microcalorimetry, and the parasite clearance time in mice were shorter for 28DAP010 than for DB829. No cross-resistance was observed between 28DAP010 and pentamidine on the tested Trypanosoma brucei gambiense isolates from melarsoprol-refractory patients. 28DAP010 is the second promising preclinical candidate among the diamidines for the treatment of second-stage African sleeping sickness.
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This is the published version.
Date
2014-05-27
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American Society for Microbiology
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Wenzler, T., S. Yang, D. A. Patrick, O. Braissant, M. A. Ismail, R. R. Tidwell, D. W. Boykin, M. Z. Wang, and R. Brun. "In Vitro and In Vivo Evaluation of 28DAP010, a Novel Diamidine for Treatment of Second-Stage African Sleeping Sickness." Antimicrobial Agents and Chemotherapy 58.8 (2014): 4452-463. http://dx.doi.org/10.1128/AAC.02309-13