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

doi:10.1128/AAC.05139-14

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

Centre for Drug Candidate Optimisation

Research output: Contribution to journal › Article › Other › peer-review

8 Citations (Scopus)

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 language	English
Pages (from-to)	3645-3647
Number of pages	3
Journal	Antimicrobial Agents and Chemotherapy
Volume	59
Issue number	6
DOIs	https://doi.org/10.1128/AAC.05139-14
Publication status	Published - 2015

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Moraes, C. B., White, K. L., Braillard, S., Perez, C., Goo, J., Gaspar, L., Shackleford, D. M., Cordeiro-da-Silva, A., Thompson, R. C. A., Freitas-Junior, L. H., Charman, S. A., & Chatelain, E. (2015). Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties. Antimicrobial Agents and Chemotherapy, 59(6), 3645-3647. https://doi.org/10.1128/AAC.05139-14

@article{400d14f80c56431ea8f4117ca9a60f51,

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

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.",

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

year = "2015",

doi = "10.1128/AAC.05139-14",

language = "English",

volume = "59",

pages = "3645--3647",

journal = "Antimicrobial Agents and Chemotherapy",

issn = "0066-4804",

publisher = "American Society for Microbiology",

number = "6",

}

Moraes, CB, White, KL, Braillard, S, Perez, C, Goo, J, Gaspar, L, Shackleford, DM, Cordeiro-da-Silva, A, Thompson, RCA, Freitas-Junior, LH, Charman, SA & Chatelain, E 2015, 'Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties', Antimicrobial Agents and Chemotherapy, vol. 59, no. 6, pp. 3645-3647. https://doi.org/10.1128/AAC.05139-14

TY - JOUR

T1 - Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties

AU - Moraes, Carolina B

AU - White, Karen L

AU - Braillard, Stephanie

AU - Perez, Catherine

AU - Goo, Junghyun

AU - Gaspar, Luis

AU - Shackleford, David M

AU - Cordeiro-da-Silva, Anabela

AU - Thompson, R C Andrew

AU - Freitas-Junior, Lucio H

AU - Charman, Susan A

AU - Chatelain, Eric

PY - 2015

Y1 - 2015

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/84929598074

U2 - 10.1128/AAC.05139-14

DO - 10.1128/AAC.05139-14

M3 - Article

SN - 0066-4804

VL - 59

SP - 3645

EP - 3647

JO - Antimicrobial Agents and Chemotherapy

JF - Antimicrobial Agents and Chemotherapy

IS - 6

ER -

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

Abstract

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