With the aim of improving 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 T. cruzi strains, in vivo efficacy in a murine model of Chagas disease, in vitro toxicity and “absorption, distribution, metabolism, and excretion’ (ADME) characteristics, and in vivo pharmacokinetic properties. There is unlikely to be any therapeutic benefit of an individual nifurtimox enantiomer over the racemic mixture.
Moraes, C.B.; White, K.L.; Braillard, S.; Perez, C.; Goo, J.; Gaspar, L.; Shackleford, D.M.; Cordeiro-da-Silva, A.; Thompson, R.C.; Freitas-Junior, L.; Charman, S.A.; Chatelain, E. Enantiomers of Nifurtimox Do Not Exhibit Stereoselective Anti-Trypanosoma cruzi Activity, Toxicity, or Pharmacokinetic Properties. Antimicrobial Agents and Chemotherapy (2015) 59 (6) 3645-3647. [DOI: 10.1128/AAC.05139-14]
Enantiomers of nifurtimox do not exhibit stereoselective anti-T. cruzi activity, toxicity or pharmacokinetic properties