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Primaquine synergises the activity of chloroquine against chloroquine-resistant P. falciparum

Bray, Patrick, Deed, S., Fox, E., Kalkanidis, M., Mungthin, M., Deady, L. W. and Tilley, L. (2005) 'Primaquine synergises the activity of chloroquine against chloroquine-resistant P. falciparum'. Biochemical Pharmacology, Vol 70, Issue 8, pp. 1158-1166.

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Abstract

In recent years, resistance to the antimalarial drug, chloroquine, has become widespread. It is, therefore, imperative to find compounds that could replace chloroquine or work synergistically with this drug to overcome chloroquine resistance. We have examined the interaction between chloroquine, a 4-aminoquinoline, and a number of 8-aminoquinolines, including primaquine, a drug that is widely used to treat Plasmodium vivax infections. We find that primaquine is a potent synergiser of the activity of chloroquine against chloroquine-resistant Plastnodium falciparum. Analysis of matched transfectants expressing mutant and wild-type alleles of the P.falciparum chloroquine resistance transporter (PfCRT) indicate that primaquine exerts its activity by blocking PfCRT, and thus enhancing chloroquine accumulation. Our data suggest that a novel formulation of two antimalarial drugs already licensed for use in humans could be used to treat chloroquine-resistant parasites. (c) 2005 Elsevier Inc. All rights reserved.

Item Type: Article
Uncontrolled Keywords: malaria 8-aminoquinoline primaquine chloroquine drug resistance resistance reversing agent drug/metabolite transporter superfamily schizontocidal antimalarial activities parasite plasmodium-falciparum malaria parasites multidrug-resistance drug-resistance beta-hematin reversal tafenoquine combination
Subjects: QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials
QW Microbiology and Immunology > QW 45 Microbial drug resistance. General or not elsewhere classified.
WC Communicable Diseases > Tropical and Parasitic Diseases > WC 770 Therapy
Faculty: Department: Groups (2002 - 2012) > Molecular & Biochemical Parasitology Group
Digital Object Identifer (DOI): https://doi.org/10.1016/j.bcp.2005.07.021
Depositing User: Ms Julia Martin
Date Deposited: 11 Aug 2011 09:19
Last Modified: 06 Feb 2018 13:02
URI: https://archive.lstmed.ac.uk/id/eprint/1860

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