ArticleAntimicrobial agents and chemotherapy2014
Activity of praziquantel enantiomers and main metabolites against Schistosoma mansoni.
Article in Antimicrobial agents and chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers.
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Who cites it
51 citing papers in PubMed.
- In vitro and in vivo human metabolism and pharmacokinetics of S- and R-praziquantel.Pharmacology research & perspectives · 2020Trial
- Extrapolation of praziquantel pharmacokinetics to a pediatric population: a cautionary tale.Journal of pharmacokinetics and pharmacodynamics · 2018Trial
- Strevertene A, a Streptomyces-Derived Macrolide, Reveals Selective Activity against the Human ParasiteACS omega · 2026Article
- Use of a cytochrome P450 humanized mouse model to refine schistosomiasis drug discovery.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Novel 1ACS infectious diseases · 2026Article
- Molecular containment of iron source inhibits larval survival of Schistosoma mansoni and egg-laying behavior of the female adult worms via ovarian atrophy.Tropical medicine and health · 2025Article
- Merck Open Global Health Library in vitro screening against Schistosoma mansoni identified two new substances with antischistosomal activities for further development.Parasites & vectors · 2025Article
- Praziquantel Fifty Years on: A Comprehensive Overview of Its Solid State.Pharmaceutics · 2023Review
- Metabolism of (R)-Praziquantel versus the Activation of a Parasite Transient Receptor Potential Melastatin Ion Channel.ChemMedChem · 2023Article
- Perspective on Schistosomiasis Drug Discovery: Highlights from a Schistosomiasis Drug Discovery Workshop at Wellcome Collection, London, September 2022.ACS infectious diseases · 2023Review
- Article
- Effect of pharmacogenetic variations on praziquantel plasma concentration and safety outcomes among school children in Rwanda.Scientific reports · 2023Article
- Natural variation in the binding pocket of a parasitic flatworm TRPM channel resolves the basis for praziquantel sensitivity.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- CaMKII regulates neuromuscular activity and survival of the human blood fluke Schistosoma mansoni.Scientific reports · 2022Article
- Pharmacokinetics of Ascending Doses of Praziquantel in Adults Infected with Opisthorchis felineus in Western Siberia, Russian Federation.Antimicrobial agents and chemotherapy · 2022Article
- R-praziquantel integrated population pharmacokinetics in preschool- and school-aged African children infected with Schistosoma mansoni and S. haematobium and Lao adults infected with Opisthorchis viverrini.Journal of pharmacokinetics and pharmacodynamics · 2022Article
- Mechanism of praziquantel action at a parasitic flatworm ion channel.Science translational medicine · 2021Article
- Article
- Evaluation of Human Liver Microtissues for Drug Screening onACS infectious diseases · 2021Article
- Clinically relevant enantiomer specific R- and S-praziquantel pharmacokinetic drug-drug interactions with efavirenz and ritonavir.Pharmacology research & perspectives · 2021Article
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
A racemic mixture of R and S enantiomers of praziquantel (PZQ) is currently the treatment of choice for schistosomiasis. Though the S enantiomer and the metabolites are presumed to contribute only a little to the activity of the drug, in-depth side-by-side studies are lacking. The aim of this study was to investigate the in vitro activities of PZQ and its main metabolites, namely, R- and S-cis- and R- and S-trans-4'-hydroxypraziquantel, against adult worms and newly transformed schistosomula (NTS). Additionally, we explored the in vivo activity and hepatic shift (i.e., the migration of the worms to the liver) produced by each PZQ enantiomer in mice. Fifty percent inhibitory concentrations of R-PZQ, S-PZQ, and R-trans- and R-cis-4'-hydroxypraziquantel of 0.02, 5.85, 4.08, and 2.42 μg/ml, respectively, for adult S. mansoni were determined in vitro. S-trans- and S-cis-4'-hydroxypraziquantel were not active at 100 μg/ml. These results are consistent with microcalorimetry data and studies with NTS. In vivo, single 400-mg/kg oral doses of R-PZQ and S-PZQ achieved worm burden reductions of 100 and 19%, respectively. Moreover, worms treated in vivo with S-PZQ displayed an only transient hepatic shift and returned to the mesenteric veins within 24 h. Our data confirm that R-PZQ is the main effector molecule, while S-PZQ and the metabolites do not play a significant role in the antischistosomal properties of PZQ.
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