Wenzler, TanjaYang, SihyungPatrick, Donald A.Braissant, OlivierIsmail, Mohamed A.Tidwell, Richard R.Boykin, David W.Wang, ZhuoBrun, Reto2015-12-312015-12-312014-05-27Wenzler, 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.02309-13https://hdl.handle.net/1808/19370This is the published version.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.Articlehttps://orcid.org/0000-0003-1751-4975openAccess