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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
medicine
Pharmacokinetics of ferroquine, a novel 4-aminoquinoline, in asymptomatic carriers of Plasmodium falciparum infections
Antimicrobial Agents and Chemotherapy, Volume 56, No. 6, Year 2012
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Description
Ferroquine (SSR97193), a ferrocene-quinoline conjugate, is a promising novel antimalarial currently undergoing clinical evaluation. This study characterizes its pharmacokinetic properties. Young male African volunteers with asymptomatic Plasmodium falciparum infection were administered a single oral dose (n = 40) or a repeated oral dose (n = 26) given over 3 days of ferroquine in two dose-escalation, double-blind, randomized, placebo-controlled clinical trials. In addition, a food interaction study was performed in a subsample of participants (n = 16). The studies were carried out in Lambaréné, Gabon. After single-dose administration of ferroquine, dose linearity was demonstrated in a dose range of 400 to 1,200 mg for maximum mean blood concentrations ([Cmax] 82 to 270 ng/ml) and in a dose range of 400 to 1,600 mg for overall exposure to ferroquine (area under the concentration-time curve [AUC], 13,100 to 49,200 ng • h/ml). Overall mean estimate for blood apparent terminal half-life of ferroquine was 16 days and 31 days for its active and major metabolite desmethylferroquine (SSR97213). In the 3-day repeated-dose study, Cmax and overall cumulated exposure to ferroquine (AUC cum) increased in proportion with the dose from day 1 to day 3 between 400 and 800 mg. No major food effect on ferroquine pharmacokinetics was observed after single administration of 100 mg of ferroquine except for a slight delay of time to maximum blood concentration (tmax) by approximately 3 h. The pharmacokinetics of ferroquine and its active main metabolite are characterized by sustained levels in blood, and the properties of ferroquine as a partner drug in antimalarial combination therapy should be evaluated. Copyright © 2012, American Society for Microbiology. All Rights Reserved.
Authors & Co-Authors
Supan, Christian
Gabon, Lambarene
Unité de Recherche Médicale, Albert Schweitzer Hospital
Germany, Tubingen
Eberhard Karls Universität Tübingen
Mombo-Ngoma, Ghyslain
Gabon, Lambarene
Unité de Recherche Médicale, Albert Schweitzer Hospital
Germany, Tubingen
Eberhard Karls Universität Tübingen
Gabon, Libreville
Faculte de Medecine et Des Sciences de la Sante
Dal-Bianco, Matthias P.
Gabon, Lambarene
Unité de Recherche Médicale, Albert Schweitzer Hospital
Germany, Tubingen
Eberhard Karls Universität Tübingen
Ospina Salazar, Carmen Lucelly
Gabon, Lambarene
Unité de Recherche Médicale, Albert Schweitzer Hospital
Germany, Tubingen
Eberhard Karls Universität Tübingen
Issifou, Saadou
Gabon, Lambarene
Unité de Recherche Médicale, Albert Schweitzer Hospital
Germany, Tubingen
Eberhard Karls Universität Tübingen
Mazuir, Florent
France, Gentilly
Sanofi S.a.
Filali-Ansary, Aziz
France, Gentilly
Sanofi S.a.
Biot, Christophe
France, Lille
Université de Lille
France, Paris
Cnrs Centre National de la Recherche Scientifique
Ter-Minassian, Daniel
France, Gentilly
Sanofi S.a.
Ramharter, Michael
Gabon, Lambarene
Unité de Recherche Médicale, Albert Schweitzer Hospital
Austria, Vienna
Medizinische Universität Wien
Kremsner, Peter G.
Gabon, Lambarene
Unité de Recherche Médicale, Albert Schweitzer Hospital
Germany, Tubingen
Eberhard Karls Universität Tübingen
Lell, Bertrand
Gabon, Lambarene
Unité de Recherche Médicale, Albert Schweitzer Hospital
Germany, Tubingen
Eberhard Karls Universität Tübingen
Statistics
Citations: 70
Authors: 12
Affiliations: 7
Identifiers
Doi:
10.1128/AAC.05359-11
ISSN:
00664804
e-ISSN:
10986596
Research Areas
Disability
Food Security
Health System And Policy
Study Locations
Gabon
Participants Gender
Male