Sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistance

Sitamaquine is a 8-aminoquinoline in development for the treatment of visceral leishmaniasis by oral route, no activity being observed on the experimental cutaneous leishmaniasis experimental models. Recent data explain how sitamaquine accumulate in Leishmania parasites, however its molecular target...

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Main Authors: Loiseau P.M., Cojean S., Schrével J.
Format: Article
Language:English
Published: EDP Sciences 2011-05-01
Series:Parasite
Subjects:
Online Access:http://dx.doi.org/10.1051/parasite/2011182115
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spelling doaj-0fc4eabd227449cc96e875a408db2f432021-03-02T01:16:08ZengEDP SciencesParasite1252-607X1776-10422011-05-0118211511910.1051/parasite/2011182115parasite2011182p115Sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistanceLoiseau P.M.Cojean S.Schrével J.Sitamaquine is a 8-aminoquinoline in development for the treatment of visceral leishmaniasis by oral route, no activity being observed on the experimental cutaneous leishmaniasis experimental models. Recent data explain how sitamaquine accumulate in Leishmania parasites, however its molecular targets remain to be identified. An advantage of sitamaquine is its short elimination half-life, preventing a rapid resistance emergence. The antileishmanial action of its metabolites is not known. The selection of a sitamaquine-resistant clone of L. donovani in laboratory and the phase II clinical trials pointing out some adverse effects such as methemoglobinemia and nephrotoxicity are considered for a further development decision.http://dx.doi.org/10.1051/parasite/2011182115sitamaquineleishmaniasisaminoquinolinedrug action
collection DOAJ
language English
format Article
sources DOAJ
author Loiseau P.M.
Cojean S.
Schrével J.
spellingShingle Loiseau P.M.
Cojean S.
Schrével J.
Sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistance
Parasite
sitamaquine
leishmaniasis
aminoquinoline
drug action
author_facet Loiseau P.M.
Cojean S.
Schrével J.
author_sort Loiseau P.M.
title Sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistance
title_short Sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistance
title_full Sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistance
title_fullStr Sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistance
title_full_unstemmed Sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistance
title_sort sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistance
publisher EDP Sciences
series Parasite
issn 1252-607X
1776-1042
publishDate 2011-05-01
description Sitamaquine is a 8-aminoquinoline in development for the treatment of visceral leishmaniasis by oral route, no activity being observed on the experimental cutaneous leishmaniasis experimental models. Recent data explain how sitamaquine accumulate in Leishmania parasites, however its molecular targets remain to be identified. An advantage of sitamaquine is its short elimination half-life, preventing a rapid resistance emergence. The antileishmanial action of its metabolites is not known. The selection of a sitamaquine-resistant clone of L. donovani in laboratory and the phase II clinical trials pointing out some adverse effects such as methemoglobinemia and nephrotoxicity are considered for a further development decision.
topic sitamaquine
leishmaniasis
aminoquinoline
drug action
url http://dx.doi.org/10.1051/parasite/2011182115
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