Trial reportClinical pharmacokinetics2020
Validation of a Drug Transporter Probe Cocktail Using the Prototypical Inhibitors Rifampin, Probenecid, Verapamil, and Cimetidine.
Trial report in Clinical pharmacokinetics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers, 1 of them a synthesis that pooled it.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
27 citing papers in PubMed, 1 synthesis or guideline pooled it, 48 citations in OpenAlex.
- A Systematic Review and Classification of the Effects of P-glycoprotein Inhibitors and Inducers in Humans, Using Digoxin, Fexofenadine, and Dabigatran as Probe Drugs.Clinical pharmacokinetics · 2025Pooled it
- Using Pharmacovigilance Data for Signal Detection of Drug Interactions for Rosuvastatin.Basic & clinical pharmacology & toxicology · 2026Article
- Lack of Modulation of In Vivo Activity of Organic Anion Transporters 1 and 3 in Pregnancy Using Furosemide as a Probe.Journal of clinical pharmacology · 2026Article
- Coproporphyrin I PBPK model in the open systems pharmacology suite enables precise prediction of OATP 1B- mediated drug interactions through calibratedFrontiers in pharmacology · 2026Article
- Predicting OCT2/MATEs-Mediated Drug Interactions in Healthy Volunteers and Patients with Chronic Kidney Disease: Insights from Extended Clearance Concept, Endogenous Biomarkers, and In Vitro Inhibition Studies (Perspectives from the International Transporter Consortium).Clinical pharmacology and therapeutics · 2025Review
- Putative new biomarkers for renal transporter-mediated drug-drug interactions: Characterization as substrates of organic cation transporter 2, multidrug and toxin extrusion protein 1, and other important drug transporters.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Quantitative Contributions of Hepatic and Renal Organic Cation Transporters to the Clinical Pharmacokinetic Cimetidine-Metformin Interaction.Clinical pharmacology and therapeutics · 2025Article
- Validating Low-Dose Iohexol as a Marker for Glomerular Filtration Rate by In Vitro and In Vivo Studies.Clinical and translational science · 2025Article
- Effects of Cimetidine and Dolutegravir on the Endogenous Drug-Drug Interaction Biomarkers for Organic Cation Transporter 2 and Multidrug and Toxin Extrusion Protein 1 in Healthy Volunteers.Clinical pharmacology and therapeutics · 2025Article
- New Biomarkers for Renal Transporter-Mediated Drug-Drug Interactions: Metabolomic Effects of Cimetidine, Probenecid, Verapamil, and Rifampin in Humans.Clinical pharmacology and therapeutics · 2025Article
- Prediction of Inhibitory Activity against the MATE1 Transporter via Combined Fingerprint- and Physics-Based Machine Learning Models.Journal of chemical information and modeling · 2024Article
- Innovative Approaches to Optimize Clinical Transporter Drug-Drug Interaction Studies.Pharmaceutics · 2024Review
- Understanding adefovir pharmacokinetics as a component of a transporter phenotyping cocktail.European journal of clinical pharmacology · 2024Article
- Membrane transporters in drug development and as determinants of precision medicine.Nature reviews. Drug discovery · 2024Review
- Effect of Cimetidine on Metformin Pharmacokinetics and Endogenous Metabolite Levels in Rats.Drug metabolism and disposition: the biological fate of chemicals · 2024Article
- Pharmacokinetic and Pharmacodynamic Drug-Drug Interactions: Research Methods and Applications.Metabolites · 2023Review
- Assessment of the drug-drug interaction potential for therapeutic proteins with pro-inflammatory activities.Clinical and translational science · 2023Review
- Construction and Evaluation of a Novel Organic Anion Transporter 1/3 CRISPR/Cas9 Double-Knockout Rat Model.Pharmaceutics · 2022Article
- Evaluation of the Effect of Abrocitinib on Drug Transporters by Integrated Use of Probe Drugs and Endogenous Biomarkers.Clinical pharmacology and therapeutics · 2022Article
- Determining the Effects of Chronic Kidney Disease on Organic Anion Transporter1/3 Activity Through Physiologically Based Pharmacokinetic Modeling.Clinical pharmacokinetics · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
15 authors at 6 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectiveA novel cocktail containing four substrates of key drug transporters was previously optimized to eliminate mutual drug-drug interactions between the probes digoxin (P-glycoprotein substrate), furosemide (organic anion transporter 1/3), metformin (organic cation transporter 2, multidrug and toxin extrusion protein 1/2-K), and rosuvastatin (organic anion transporting polypeptide 1B1/3, breast cancer resistance protein). This clinical trial investigated the effects of four commonly employed drug transporter inhibitors on cocktail drug pharmacokinetics.
methodsIn a randomized open-label crossover trial in 45 healthy male subjects, treatment groups received the cocktail with or without single oral doses of rifampin, verapamil, cimetidine or probenecid. Concentrations of the probe drugs in serial plasma samples and urine fractions were measured by validated liquid chromatography-tandem mass spectrometry assays to assess systemic exposure.
resultsThe results were generally in accordance with known in vitro and/or clinical drug-drug interaction data. Single-dose rifampin increased rosuvastatin area under the plasma concentration-time curve up to the last quantifiable concentration (AUC
conclusionsTaking all the interaction results together, the transporter cocktail is considered to be validated as a sensitive and specific tool for evaluating transporter-mediated drug-drug interactions in drug development. CLINICAL
trial registrationEudraCT number 2017-001549-29.
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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.