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Praziquantel for schistosomiasis, single drug revisited metabolism, mode of action and resistance

13 March 2017 - 11:34am
Antimicrobial Agents and Chemotherapy (06 March 2017), AAC.02582-16, doi:10.1128/aac.02582-16

Schistosomiasis, a major neglected tropical disease, affects more than 250 million people worldwide. Treatment for schistosomiasis has relied on the anthelmintic drug praziquantel (PZQ) for more than a generation. PZQ is the drug of choice for treatment of schistosomiasis; it is effective against all major forms of schistosomiasis, although PZQ is less active against juvenile compared to mature parasites. A pyrazino-isoquinoline derivative, PZQ is not considered to be toxic and generally causes few or transient, mild side effects. Increasingly, mass drug administration targeting endemic populations in sub-Saharan Africa has led to the appearance of reduced efficacy of PZQ, which portends the selection of drug-resistant forms of these pathogens. The synthesis of improved derivatives of PZQ is attracting attention: i) synthesis of drug analogues, ii) rational design of pharmacophores, and iii) the discovery of new compounds from large-scale screenings programmes. This article reviews reports from 1970s to the present on the metabolism and mechanism of action of PZQ and its derivatives against schistosomes.
Nuno Vale, Maria Gouveia, Gabriel Rinaldi, Paul Brindley, Fátima Gärtner, José Correia da Costa
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