Trial reportPharmacology research & perspectives2021
Identification of the metabolites of ivermectin in humans.
Trial report in Pharmacology research & perspectives, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT06434519 (Evaluation of the Effect of Moisturizers on the Absorption of Metronidazole Into the Stratum Corneum of Rosacea Patients With Tape Stripping and Liquid Chromatography-mass Spectrometry), which is not on this map. Cited by 27 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Evaluation of the Effect of Moisturizers on the Absorption of Metronidazole Into the Stratum Corneum of Rosacea Patients With Tape Stripping and Liquid Chromatography-mass Spectrometry
Who cites it
27 citing papers in PubMed, 49 citations in OpenAlex.
- Trial
- Entomological impact of mass administration of ivermectin and dihydroartemisinin-piperaquine in The Gambia: a cluster-randomized controlled trial.Parasites & vectors · 2022Trial
- Identification of the metabolites of ivermectin in humans.Pharmacology research & perspectives · 2021Trial
- Symbiotic Stenotrophomonas maltophilia is associated with ivermectin resistance in the parasitic nematode Haemonchus contortus via metabolic detoxification.International journal for parasitology. Drugs and drug resistance · 2026Article
- An Adaptable Porous Metal-Organic Framework for Structural Visualization of Beyond Rule of 5 Molecules on the Microgram Scale.Journal of the American Chemical Society · 2026Article
- Interactive effects of ivermectin and nitrogen levels on phytoplankton biomass and stress responses.Ecotoxicology (London, England) · 2026Article
- Evaluation of the safety and insecticidal efficacy of ivermectin-treated bird feed formulations in different avian species.Parasites & vectors · 2026Article
- The role of CYP3A-CYP2E1 interactions in activation of CYP3A enzymes by chronic alcohol exposure.bioRxiv : the preprint server for biology · 2026Article
- Lethal effects of ivermectin structures on malaria vectors and in silico analysis of interactions with their glutamate-gated chloride ion channels.Scientific reports · 2026Article
- Optimizing endectocide and ectocide compound evaluation in Anopheles malaria vectors.Parasites & vectors · 2025Article
- Evaluation of in vitro drug-drug interactions of ivermectin and antimalarial compounds.Malaria journal · 2025Article
- The current findings on the gut-liver axis and the molecular basis of NAFLD/NASH associated with gut microbiome dysbiosis.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- In-host modeling of dengue virus and non-structural protein 1 and the effects of ivermectin in patients with acute dengue fever.CPT: pharmacometrics & systems pharmacology · 2024Article
- Human Cytochrome P450 Cancer-Related Metabolic Activities and Gene Polymorphisms: A Review.Cells · 2024Review
- Transmission-blocking activities of artesunate, chloroquine, and methylene blue onAntimicrobial agents and chemotherapy · 2024Article
- Efficacy of ivermectin and its metabolites againstAntimicrobial agents and chemotherapy · 2024Article
- Safety, pharmacokinetics, and potential neurological interactions of ivermectin, tafenoquine, and chloroquine in Rhesus macaques.Antimicrobial agents and chemotherapy · 2024Article
- Article
- Activity of Ivermectin and Its Metabolites against Asexual Blood Stage Plasmodium falciparum and Its Interactions with Antimalarial Drugs.Antimicrobial agents and chemotherapy · 2023Article
- Pharmacokinetics of ivermectin metabolites and their activity against Anopheles stephensi mosquitoes.Malaria journal · 2023Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 4 institutions in 5 countries.
Funding
Abstract
Mass drug administration of ivermectin has been proposed as a possible malaria elimination tool. Ivermectin exhibits a mosquito-lethal effect well beyond its biological half-life, suggesting the presence of active slowly eliminated metabolites. Human liver microsomes, primary human hepatocytes, and whole blood from healthy volunteers given oral ivermectin were used to identify ivermectin metabolites by ultra-high performance liquid chromatography coupled with high-resolution mass spectrometry. The molecular structures of metabolites were determined by mass spectrometry and verified by nuclear magnetic resonance. Pure cytochrome P450 enzyme isoforms were used to elucidate the metabolic pathways. Thirteen different metabolites (M1-M13) were identified after incubation of ivermectin with human liver microsomes. Three (M1, M3, and M6) were the major metabolites found in microsomes, hepatocytes, and blood from volunteers after oral ivermectin administration. The chemical structure, defined by LC-MS/MS and NMR, indicated that M1 is 3″-O-demethyl ivermectin, M3 is 4-hydroxymethyl ivermectin, and M6 is 3″-O-demethyl, 4-hydroxymethyl ivermectin. Metabolic pathway evaluations with characterized cytochrome P450 enzymes showed that M1, M3, and M6 were produced primarily by CYP3A4, and that M1 was also produced to a small extent by CYP3A5. Demethylated (M1) and hydroxylated (M3) ivermectin were the main human in vivo metabolites. Further studies are needed to characterize the pharmacokinetic properties and mosquito-lethal activity of these metabolites.
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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.