ArticleThe Journal of infectious diseases2015
Targeting Filarial Abl-like Kinases: Orally Available, Food and Drug Administration-Approved Tyrosine Kinase Inhibitors Are Microfilaricidal and Macrofilaricidal.
Article in The Journal of infectious diseases, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 33 citations in OpenAlex.
- The pipeline for drugs for control and elimination of neglected tropical diseases: 2. Oral anti-infective drugs and drug combinations for off-label use.Parasites & vectors · 2023Review
- Toward novel treatment against filariasis: Insight into genome-wide co-evolutionary analysis of filarial nematodes andFrontiers in microbiology · 2023Article
- Advances in preclinical platforms ofFrontiers in tropical diseases · 2021Article
- Multimodal biomarker discovery for active Onchocerca volvulus infection.PLoS neglected tropical diseases · 2021Article
- High-resolution AP-SMALDI MSI as a tool for drug imaging in Schistosoma mansoni.Analytical and bioanalytical chemistry · 2021Article
- Protein Kinases: Potential Drug Targets AgainstFrontiers in cellular and infection microbiology · 2021Review
- Drug-induced reactive oxygen species-mediated inhibitory effect on growth of Trypanosoma evansi in axenic culture system.Parasitology research · 2020Article
- Study of therapeutic effect of different concentrations of imatinib on Balb/c model of cutaneous leishmaniasis.AIMS microbiology · 2020Article
- Targeting Kinases inFrontiers in veterinary science · 2020Article
- Article
- Reference gene analysis and its use for kinase expression profiling in Fasciola hepatica.Scientific reports · 2019Article
- The ABL kinase inhibitor imatinib causes phenotypic changes and lethality in adult Schistosoma japonicum.Parasitology research · 2019Article
- Flubendazole as a macrofilaricide: History and background.PLoS neglected tropical diseases · 2019Review
- Heterogeneity in the in vitro susceptibility of Loa loa microfilariae to drugs commonly used in parasitological infections.Parasites & vectors · 2018Article
- Alternative treatment strategies to accelerate the elimination of onchocerciasis.International health · 2018Article
- Mining Filarial Genomes for Diagnostic and Therapeutic Targets.Trends in parasitology · 2018Review
- Reduction of Loa loa Microfilaremia with Imatinib - A Case Report.The New England journal of medicine · 2017Article
- Susceptibility Testing of Medically Important Parasites.Clinical microbiology reviews · 2017Review
- Defining the target and the effect of imatinib on the filarial c-Abl homologue.PLoS neglected tropical diseases · 2017Article
- Lessons from the genomes and transcriptomes of filarial nematodes.Molecular and biochemical parasitology · 2017Review
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
Abstract
backgroundElimination of onchocerciasis and lymphatic filariasis is targeted for 2020. Given the coincident Loa loa infections in Central Africa and the potential for drug resistance development, the need for new microfilaricides and macrofilaricides has never been greater. With the genomes of L. loa, Onchocerca volvulus, Wuchereria bancrofti, and Brugia malayi available, new drug targets have been identified.
methodsThe effects of the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib on B. malayi adult males, adult females, L3 larvae, and microfilariae were assessed using a wide dose range (0-100 µM) in vitro.
resultsFor microfilariae, median inhibitory concentrations (IC50 values) on day 6 were 6.06 µM for imatinib, 3.72 µM for dasatinib, and 81.35 µM for nilotinib; for L3 larvae, 11.27 µM, 13.64 µM, and 70.98 µM, respectively; for adult males, 41.6 µM, 3.87 µM, and 68.22 µM, respectively; and for adult females, 42.89 µM, 9.8 µM, and >100 µM, respectively. Three-dimensional modeling suggests how these tyrosine kinase inhibitors bind and inhibit filarial protein activity.
conclusionsGiven the safety of imatinib in humans, plans are underway for pilot clinical trials to assess its efficacy in patients with filarial infections.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.