Trial reportEuropean journal of clinical pharmacology2012
Intestinal OATP1A2 inhibition as a potential mechanism for the effect of grapefruit juice on aliskiren pharmacokinetics in healthy subjects.
Trial report in European journal of clinical pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed, 66 citations in OpenAlex.
- Effects of one-time apple juice ingestion on the pharmacokinetics of fexofenadine enantiomers.European journal of clinical pharmacology · 2014Trial
- Dietary Modulation of CYP3A4 and Its Impact on Statins and Antidiabetic Drugs: A Narrative Review.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Regulatory mechanism and therapeutic potentials of naringin against inflammatory disorders.Heliyon · 2024Review
- Network Analysis of the Herb-Drug Interactions of Citrus Herbs Inspired by the "Grapefruit Juice Effect".ACS omega · 2022Article
- Increased/Targeted Brain (Pro)Drug Delivery via Utilization of Solute Carriers (SLCs).Pharmaceutics · 2022Review
- The Challenge and Importance of Integrating Drug-Nutrient-Genome Interactions in Personalized Cardiovascular Healthcare.Journal of personalized medicine · 2022Review
- A guide to plasma membrane solute carrier proteins.The FEBS journal · 2021Review
- Effect ofPharmaceutics · 2020Article
- Organic Anion Transporting Polypeptides: Emerging Roles in Cancer Pharmacology.Molecular pharmacology · 2019Review
- Pharmacokinetic Interactions between Cardiovascular Medicines and Plant Products.Cardiovascular therapeutics · 2019Review
- Food-drug interactions precipitated by fruit juices other than grapefruit juice: An update review.Journal of food and drug analysis · 2018Review
- Phytotherapeutics: The Emerging Role of Intestinal and Hepatocellular Transporters in Drug Interactions with Botanical Supplements.Molecules (Basel, Switzerland) · 2017Review
- Renal Drug Transporters and Drug Interactions.Clinical pharmacokinetics · 2017Review
- Food and Drug Interactions.Journal of lifestyle medicine · 2017Review
- Functional identification of organic cation transporter 1 as an atenolol transporter sensitive to flavonoids.Biochemistry and biophysics reports · 2015Article
- Article
- Recent advances in 2D and 3D in vitro systems using primary hepatocytes, alternative hepatocyte sources and non-parenchymal liver cells and their use in investigating mechanisms of hepatotoxicity, cell signaling and ADME.Archives of toxicology · 2013Review
- Mechanisms underlying food-drug interactions: inhibition of intestinal metabolism and transport.Pharmacology & therapeutics · 2012Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo conduct a mechanistic investigation of the interaction between aliskiren and grapefruit juice in healthy subjects.
methodsTwenty-eight subjects received an oral dose of aliskiren 300 mg (highest recommended clinical dose) with 300 mL of either water or grapefruit juice in a two-way crossover design. Safety and pharmacokinetic analyses were performed. In vitro studies were performed in HEK293 cells to investigate the role of organic anion transporting polypeptide (OATP) transporter-mediated uptake of aliskiren.
resultsCo-administration of a single dose of aliskiren with grapefruit juice decreased the plasma concentration of aliskiren, with mean decreases in the AUC(inf), AUC(last), and C(max) of 38, 37, and 61%, respectively. The uptake of [¹⁴C]aliskiren into OATP2B1-expressing cells was essentially the same as that into control cells, and the inhibitor combination atorvastatin and rifamycin had no effect on [¹⁴C]aliskiren accumulation in either cell type. The uptake of [¹⁴C]aliskiren and [³H]fexofenadine was linear in OATP1A2-expressing cells and was reduced by naringin, with IC₅₀ values of 75.5 ± 11.6 and 24.2 ± 2.0 μM, respectively.
conclusionsGrapefruit juice decreases exposure of aliskiren partially via inhibition of intestinal OATP1A2.
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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.