Investigations of the metabolites of the trypanocidal drug melarsoprol

  title={Investigations of the metabolites of the trypanocidal drug melarsoprol},
  author={Jennifer Keiser and {\"O}rjan Ericsson and Christian Burri},
  journal={Clinical Pharmacology \& Therapeutics},
Melarsoprol remains the first‐choice drug for trypanosomiasis (human African sleeping sickness). To contribute to the sparse pharmacologic data and to better understand the cause of the frequent serious adverse reactions, we investigated the metabolism of this 50–year‐old organoarsenic compound. 
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The 10-day treatment schedule of melarsoprol for the treatment of late-stage gambiense sleeping sickness is found to be more cost- effective than the standard treatment and a highly cost-effective treatment option for implementation necessary in areas with scarce resources.
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The current drugs against African trypanosomes are reviewed, the mechanisms of drug resistance are discussed, and key issues for the control oftrypanosomiasis in face of the limited options for chemotherapy are addressed.
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Only when this economic barrier can be lowered will new drugs emerge for use against sleeping sickness, as most representatives of the pharmaceutical industry believe that selling drugs to the victims of sleeping sickness will not yield sufficient income to justify expenses needed for the development of novel reagents.


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Discrepancy in plasma melarsoprol concentrations between HPLC and bioassay methods in patients with T. gambiense sleeping sickness indicates that melarsoprol is metabolized
In patients with late‐stage Trypanosoma gambiense sleeping sickness, the aim was to unravel to what extent the bioassay codetermines biologically active metabolites of melarsoprol.
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The results of these first pharmacokinetic studies on melarsoprol were used to simulate possible alternative therapy schemes which might avoid some of the problems that arise with melarsiprol use.
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Clinical and laboratory findings point rather to a drug-related, delayed immune response in patients treated with melarsoprol for human African trypanosomiasis developing a severe reactive arsenical encephalopathy (RAE).
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