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...
Main Authors: | , , |
---|---|
Format: | Article |
Language: | English |
Published: |
EDP Sciences
2011-05-01
|
Series: | Parasite |
Subjects: | |
Online Access: | http://dx.doi.org/10.1051/parasite/2011182115 |
id |
doaj-0fc4eabd227449cc96e875a408db2f43 |
---|---|
record_format |
Article |
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 |
work_keys_str_mv |
AT loiseaupm sitamaquineasaputativeantileishmanialdrugcandidatefromthemechanismofactiontotheriskofdrugresistance AT cojeans sitamaquineasaputativeantileishmanialdrugcandidatefromthemechanismofactiontotheriskofdrugresistance AT schrevelj sitamaquineasaputativeantileishmanialdrugcandidatefromthemechanismofactiontotheriskofdrugresistance |
_version_ |
1724244839879409664 |