Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties

Carolina B Moraes, Karen L White, Stephanie Braillard, Catherine Perez, Junghyun Goo, Luis Gaspar, David M Shackleford, Anabela Cordeiro-da-Silva, R C Andrew Thompson, Lucio H Freitas-Junior, Susan A Charman, Eric Chatelain

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Abstract

With the aim of improving the available drugs for the treatment of Chagas disease, individual enantiomers of nifurtimox were characterized. The results indicate that the enantiomers are equivalent in their in vitro activity against a panel of Trypanosoma cruzi strains; in vivo efficacy in a murine model of Chagas disease; in vitro toxicity and absorption, distribution, metabolism, and excretion characteristics; and in vivo pharmacokinetic properties. There is unlikely to be any therapeutic benefit of an individual nifurtimox enantiomer over the racemic mixture.
Original languageEnglish
Pages (from-to)3645-3647
Number of pages3
JournalAntimicrobial Agents and Chemotherapy
Volume59
Issue number6
DOIs
Publication statusPublished - 2015

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