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Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties. 2015
Carolina B Moraes, and
Karen L White, and
Stéphanie Braillard, and
Catherine Perez, and
Junghyun Goo, and
Luis Gaspar, and
David M Shackleford, and
Anabela Cordeiro-da-Silva, and
R C Andrew Thompson, and
Lucio Freitas-Junior, and
Susan A Charman, and
Eric Chatelain
Center for Neglected Diseases Drug Discovery, Institut Pasteur Korea, Bundang-gu, Seongnam-Si, Gyeonggi-do, South Korea.
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.
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