ArticleEuropean journal of drug metabolism and pharmacokinetics2012
Ketotifen is an antimalarial prodrug of norketotifen with blood schizonticidal and liver-stage efficacy.
Article in European journal of drug metabolism and pharmacokinetics, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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Who cites it
8 citing papers in PubMed, 18 citations in OpenAlex.
- Promising antimalarial hits from phenotypic screens: a review of recently-described multi-stage actives and their modes of action.Frontiers in cellular and infection microbiology · 2023Review
- Activation of Mast Cells PromoteFrontiers in cellular and infection microbiology · 2019Article
- Cytochrome P450 2D-mediated metabolism is not necessary for tafenoquine and primaquine to eradicate the erythrocytic stages of Plasmodium berghei.Malaria journal · 2016Article
- Human dihydrofolate reductase influences the sensitivity of the malaria parasite Plasmodium falciparum to ketotifen - A cautionary tale in screening transgenic parasites.International journal for parasitology. Drugs and drug resistance · 2016Article
- Recent developments on dry eye disease treatment compounds.Saudi journal of ophthalmology : official journal of the Saudi Ophthalmological Society · 2014Article
- Antimalarial drug discovery - approaches and progress towards new medicines.Nature reviews. Microbiology · 2013Review
- Recent advances in malaria drug discovery.Bioorganic & medicinal chemistry letters · 2013Review
- A class of tricyclic compounds blocking malaria parasite oocyst development and transmission.Antimicrobial agents and chemotherapy · 2013Article
Corrections and comments
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Authors and funding
22 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ketotifen is known to exhibit antimalarial activity in mouse and monkey malaria models. However, the low plasma levels and short half life of the drug do not adequately explain its in vivo efficacy. We synthesized most of the known metabolites of ketotifen and evaluated their antimalarial activity and pharmacokinetics in mice. Norketotifen, the de-methylated metabolite of ketotifen, was a more potent antimalarial in vitro as compared to ketotifen, and exhibited equivalent activity in vivo against asexual blood and developing liver-stage parasites. After ketotifen dosing, norketotifen levels were much higher than ketotifen relative to the IC50s of the compounds against Plasmodium falciparum in vitro. The data support the notion that the antimalarial activity of ketotifen in mice is mediated through norketotifen.
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Registered trials
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.