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Inhibition of the organic anion-transporting polypeptide 1B1 by quercetin: an in vitro and in vivo assessment

Lan-Xiang Wu, Cheng-Xian Guo, Wang-Qing Chen, Jing Yu, Qiang Qu, Yao Chen, Zhi-Rong Tan, Guo Wang, Lan Fan, Qing Li, Wei Zhang, Hong-Hao Zhou
British journal of clinical pharmacology 2012 73(5):750

Bibliography

PubMed
PMID 22114872
PubMed Central
PMC3403202
DOI
10.1111/j.1365-2125.2011.04150.x
Funding
Funding was not specified in the indexed record or the disclosure metadata available for this entry.
Competing interests
A competing-interest declaration was not available in the indexed record or the disclosure metadata used for this entry.

Study snapshot

DesignPlacebo-controlled human pharmacokinetic study with cell-transport experiments
ModelMixed human intervention and laboratory research
Sample16 healthy men in the clinical study
InterventionQuercetin 500 mg/day for 14 days, followed by pravastatin 40 mg
Duration14 days plus probe-drug sampling
EndpointsExposure and pharmacokinetics

What the study showed, in plain terms

Published in 2012, this source examined safety, interactions and special populations. Design: Placebo-controlled human pharmacokinetic study with cell-transport experiments. Sample/model: 16 healthy men in the clinical study. The exposure or intervention was Quercetin 500 mg/day for 14 days, followed by pravastatin 40 mg. Follow-up or treatment period: 14 days plus probe-drug sampling.

Pravastatin exposure and peak concentration increased by approximately 24% and 31%; cell experiments supported OATP1B1 inhibition.

Small short-term study without clinical treatment outcomes. Interaction magnitude for other statins or transporter substrates cannot be inferred directly.

Continue with Quercetin Data Center

For topic-level interpretation, read Quercetin Side Effects and Safety: A Practical Guide. This is a related guide; the citation panel separately identifies articles that directly cite this paper.

Key findings

  • Pravastatin exposure and peak concentration increased by approximately 24% and 31%; cell experiments supported OATP1B1 inhibition.
  • The recorded outcome domains were Exposure and pharmacokinetics.
  • The result applies to the tested exposure: Quercetin 500 mg/day for 14 days, followed by pravastatin 40 mg; 14 days plus probe-drug sampling.

What this study can and cannot tell us

  • Small short-term study without clinical treatment outcomes. Interaction magnitude for other statins or transporter substrates cannot be inferred directly.
  • A change in blood exposure or a metabolic marker is not a demonstrated improvement in symptoms, disease events or lifespan. The tested formulation and co-administered medicines matter.
  • Source basis: Source check: accessible full text and indexed metadata. Missing method details, funding information or participant denominators are not inferred.

Citation network

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Dr. Khaled Mahmoud, MBBChCritical Care Medicine, Longevity Science & Editorial Direction Dr. Amr Yasser, PhDCardiometabolic, Musculoskeletal, Gut & Bioavailability Dr. Abdulla Mostafa, PhDCellular Senescence, Neurological, Mitochondrial & Brain-Ageing Biology