ArticleJournal of pharmaceutical sciences2021
Drug Metabolites Potently Inhibit Renal Organic Anion Transporters, OAT1 and OAT3.
Article in Journal of pharmaceutical sciences, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 27 citations in OpenAlex.
- The SLC-ome of membrane transport: from molecular discovery to physiology and clinical applications.Physiological reviews · 2026Review
- Role of metabolites in drug-drug interactions.Drug metabolism and pharmacokinetics · 2026Review
- Nuclear receptor-neurotransmitter coupling links behavior to metabolic state.bioRxiv : the preprint server for biology · 2025Article
- Effect of Meloxicam on the Pharmacokinetics of Cefquinome in Endotoxemic Sheep.Veterinary medicine and science · 2025Article
- Contribution of Organic Anion Transporter 3 in Delayed Elimination of Methotrexate by Concomitant Administration of Febuxostat.Biopharmaceutics & drug disposition · 2025Article
- Potential Interaction of Pinocembrin with Drug Transporters and Hepatic Drug-Metabolizing Enzymes.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Research Methods and New Advances in Drug-Drug Interactions Mediated by Renal Transporters.Molecules (Basel, Switzerland) · 2023Review
- Recent Advances in Synthetic Drugs and Natural Actives Interacting with OAT3.Molecules (Basel, Switzerland) · 2023Review
- The Interplay between Uremic Toxins and Albumin, Membrane Transporters and Drug Interaction.Toxins · 2022Review
- Article
- Evaluation for Potential Drug-Drug Interaction of MT921 Using In Vitro Studies and Physiologically-Based Pharmacokinetic Models.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Drugs in COVID-19 Clinical Trials: Predicting Transporter-Mediated Drug-Drug Interactions Using In Vitro Assays and Real-World Data.Clinical pharmacology and therapeutics · 2021Article
- The Role of Uptake and Efflux Transporters in the Disposition of Glucuronide and Sulfate Conjugates.Frontiers in pharmacology · 2021Review
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
Abstract
Human OAT1 and OAT3 play major roles in renal drug elimination and drug-drug interactions. However, there is little information on the interactions of drug metabolites with transporters. The goal of this study was to characterize the interactions of drug metabolites with OAT1 and OAT3 and compare their potencies of inhibition with those of their corresponding parent drugs. Using HEK293 cells stably transfected with OAT1 and OAT3, 25 drug metabolites and their corresponding parent drugs were screened for inhibitory effects on OAT1-and OAT3-mediated 6-carboxyfluorescein uptake at a screening concentration of 200 μM for all but 3 compounds. 20 and 24 drug metabolites were identified as inhibitors (inhibition > 50%) of OAT1 and OAT3, respectively. Seven drug metabolites were potent inhibitors of either or both OAT1 and OAT3 with K
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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.