ArticleParasites & vectors2015
Repurposing of anticancer drugs: in vitro and in vivo activities against Schistosoma mansoni.
Article in Parasites & vectors, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 70 citations in OpenAlex.
- Mapping therapeutic alternatives: a systematic review of preclinical drug repurposing for schistosomiasis.Naunyn-Schmiedeberg's archives of pharmacology · 2026Review
- Dual host and pathogen targeting by MEK1/2 inhibitors.Infection and immunity · 2026Review
- Curation of the Fasciola hepatica kinome as a resource for drug target discovery.BMC genomics · 2026Article
- Optimizing the therapeutic benefits of synriam combined with praziquantel in mice harbouring juvenile and mature Schistosoma mansoni.Scientific reports · 2025Article
- Potential biomarker and composite efficacy readout for human clinical trials of schistosomiasis vaccine in Africa.Scientific reports · 2025Article
- Structure activity relationships of antischistosomalResults in chemistry · 2024Article
- The synergistic effect of Ficus carica nanoparticles and Praziquantel on mice infected by Schistosoma mansoni cercariae.Scientific reports · 2024Article
- MEK-inhibitors decrease Nfix in muscular dystrophy but induce unexpected calcifications, partially rescued with Cyanidin diet.iScience · 2024Article
- A drug repurposing screen for whipworms informed by comparative genomics.PLoS neglected tropical diseases · 2023Article
- Using ChEMBL to Complement Schistosome Drug Discovery.Pharmaceutics · 2023Article
- Drug Repurposing and De Novo Drug Discovery of Protein Kinase Inhibitors as New Drugs against Schistosomiasis.Molecules (Basel, Switzerland) · 2022Review
- Identification of anti-schistosomal, anthelmintic and anti-parasitic compounds curated and text-mined from the scientific literature.Wellcome open research · 2022Article
- Evaluation of Human Liver Microtissues for Drug Screening onACS infectious diseases · 2021Article
- Identification of hit compounds with anti-schistosomal activity on in vitro generated juvenile worms in cell-free medium.PLoS neglected tropical diseases · 2021Article
- A survey of the kinome pharmacopeia reveals multiple scaffolds and targets for the development of novel anthelmintics.Scientific reports · 2021Article
- Diarylureas: Repositioning from Antitumor to Antimicrobials or Multi-Target Agents against New Pandemics.Antibiotics (Basel, Switzerland) · 2021Review
- In vivo assessment of the antischistosomal activity of curcumin loaded nanoparticles versus praziquantel in the treatment of Schistosoma mansoni.Scientific reports · 2020Article
- Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?RSC medicinal chemistry · 2020Review
- The antischistosomal potential of GSK-J4, an H3K27 demethylase inhibitor: insights from molecular modeling, transcriptomics and in vitro assays.Parasites & vectors · 2020Article
- Activity of Combinations of Antioxidants and Anthelmintic Drugs against the Adult Stage ofJournal of parasitology research · 2020Article
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundDrug discovery for the neglected tropical disease schistosomiasis has a high priority. Anticancer drugs, especially protein kinase inhibitors, might serve as a starting point for drug discovery owing to the importance of protein kinases in helminth growth and development. Furthermore, the Schistosoma mansoni genome encodes several genes for targets of drugs marketed for human use, including several anticancer drugs.
methodsIn this study, we screened the approved oncology drug set of the National Cancer Institute's Developmental Therapeutic Program for antischistosomal activity. Drugs were tested in vitro against the larval and adult stage of S. mansoni. IC50 values and albumin binding were determined for active compounds. Lead compounds were tested in the chronic S. mansoni mouse model.
resultsEleven of the 114 compounds tested revealed IC50 values ≤ 10 μM against both S. mansoni stages. Five of these lost activity against adult S. mansoni in the presence of serum albumin. Of 6 compounds studied in vivo, the highest activity was observed from two kinase inhibitors trametinib, and vandetanib, which reduced worm burden by 63.6 and 48.1% respectively, after a single oral dose of 400 mg/kg body weight.
conclusionOur study has confirmed that oncology drugs possess antischistosomal activity. There is space for further investigation, including elucidation of the mechanisms of action of schistosome-active cancer drugs, application of different treatment courses, and structure-activity relationship studies for improving drug potency.
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