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The Anti-Trypanosome Drug Fexinidazole Shows Potential for Treating Visceral Leishmaniasis

Overview of attention for article published in Science Translational Medicine, February 2012
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About this Attention Score

  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (92nd percentile)
  • Above-average Attention Score compared to outputs of the same age and source (53rd percentile)

Mentioned by

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1 policy source
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9 X users
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1 patent
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4 Wikipedia pages

Citations

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132 Dimensions

Readers on

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181 Mendeley
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Title
The Anti-Trypanosome Drug Fexinidazole Shows Potential for Treating Visceral Leishmaniasis
Published in
Science Translational Medicine, February 2012
DOI 10.1126/scitranslmed.3003326
Pubmed ID
Authors

Susan Wyllie, Stephen Patterson, Laste Stojanovski, Frederick R. C. Simeons, Suzanne Norval, Robert Kime, Kevin D. Read, Alan H. Fairlamb

Abstract

Safer and more effective oral drugs are required to treat visceral leishmaniasis, a parasitic disease that kills 50,000 to 60,000 people each year in parts of Asia, Africa, and Latin America. Here, we report that fexinidazole, a drug currently in phase 1 clinical trials for treating African trypanosomiasis, shows promise for treating visceral leishmaniasis. This 2-substituted 5-nitroimidazole drug is rapidly oxidized in vivo in mice, dogs, and humans to sulfoxide and sulfone metabolites. Both metabolites of fexinidazole were active against Leishmania donovani amastigotes grown in macrophages, whereas the parent compound was inactive. Pharmacokinetic studies with fexinidazole (200 mg/kg) showed that fexinidazole sulfone achieves blood concentrations in mice above the EC(99) (effective concentration inhibiting growth by 99%) value for at least 24 hours after a single oral dose. A once-daily regimen for 5 days at this dose resulted in a 98.4% suppression of infection in a mouse model of visceral leishmaniasis, equivalent to that seen with the drugs miltefosine and Pentostam, which are currently used clinically to treat this tropical disease. In African trypanosomes, the mode of action of nitro drugs involves reductive activation via a NADH (reduced form of nicotinamide adenine dinucleotide)-dependent bacterial-like nitroreductase. Overexpression of the leishmanial homolog of this nitroreductase in L. donovani increased sensitivity to fexinidazole by 19-fold, indicating that a similar mechanism is involved in both parasites. These findings illustrate the potential of fexinidazole as an oral drug therapy for treating visceral leishmaniasis.

X Demographics

X Demographics

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 181 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Brazil 2 1%
United States 2 1%
United Kingdom 1 <1%
Unknown 176 97%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 38 21%
Researcher 30 17%
Student > Bachelor 26 14%
Student > Master 20 11%
Student > Doctoral Student 9 5%
Other 29 16%
Unknown 29 16%
Readers by discipline Count As %
Agricultural and Biological Sciences 44 24%
Chemistry 32 18%
Biochemistry, Genetics and Molecular Biology 25 14%
Pharmacology, Toxicology and Pharmaceutical Science 16 9%
Medicine and Dentistry 13 7%
Other 18 10%
Unknown 33 18%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 14. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 30 October 2023.
All research outputs
#2,547,009
of 25,436,226 outputs
Outputs from Science Translational Medicine
#3,001
of 5,440 outputs
Outputs of similar age
#19,016
of 253,777 outputs
Outputs of similar age from Science Translational Medicine
#33
of 69 outputs
Altmetric has tracked 25,436,226 research outputs across all sources so far. Compared to these this one has done well and is in the 89th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 5,440 research outputs from this source. They typically receive a lot more attention than average, with a mean Attention Score of 86.6. This one is in the 44th percentile – i.e., 44% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 253,777 tracked outputs that were published within six weeks on either side of this one in any source. This one has done particularly well, scoring higher than 92% of its contemporaries.
We're also able to compare this research output to 69 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 53% of its contemporaries.