ArticleDrug metabolism and disposition: the biological fate of chemicals2020
Role of Oatp2b1 in Drug Absorption and Drug-Drug Interactions.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 24 papers.
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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.
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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.
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Who cites it
24 citing papers in PubMed, 39 citations in OpenAlex.
- Altered Bile Acid Transport in Liver Disease.Biomedicines · 2026Review
- OATP2B1 Deficiency Ameliorates Irinotecan-Induced Gastrointestinal Toxicity.Clinical and translational science · 2026Article
- Insights and perspectives into the etiology of TKI-induced cardiotoxicity.ASPET discovery · 2026Article
- Drug-drug interactions in targeted cancer therapies: a focus on tyrosine kinase inhibitors.Expert review of clinical pharmacology · 2025Review
- Advancing Predictions of Oral Drug Absorption, CYP3A4 Induction, and Transporter-Mediated Interactions Using a Human Primary Intestinal 3D Model (EpiIntestinal™).Clinical pharmacology and therapeutics · 2025Article
- Insights Into Atorvastatin Pharmacokinetics in Rats Reveal Regulation of CYP3A1 by Humanization of SLCO2B1.Pharmacology research & perspectives · 2025Article
- Changed expression of placental transporters and disrupted epigenetic patterns in a rat model of schizophrenia.Frontiers in pharmacology · 2025Article
- Metabolism characterization and toxicity of N-hydap, a marine candidate drug for lung cancer therapy by LC-MS method.Natural products and bioprospecting · 2024Article
- Conversion of Olmesartan to Olmesartan Medoxomil, A Prodrug that Improves Intestinal Absorption, Confers Substrate Recognition by OATP2B1.Pharmaceutical research · 2024Article
- Importance of N-Glycosylation for the Expression and Function of Human Organic Anion Transporting Polypeptide 2B1.ACS pharmacology & translational science · 2023Article
- Transporter‑mediated drug‑drug interactions involving poly (ADP‑ribose) polymerase inhibitors (Review).Oncology letters · 2023Review
- Itraconazole-Induced Increases in Gilteritinib Exposure Are Mediated by CYP3A and OATP1B.Molecules (Basel, Switzerland) · 2022Article
- The intestinal absorption mechanism of chicoric acid and its bioavailability improvement with chitosan.Heliyon · 2022Article
- Increased/Targeted Brain (Pro)Drug Delivery via Utilization of Solute Carriers (SLCs).Pharmaceutics · 2022Review
- Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition.Cancer research communications · 2021Article
- Hepatic drug-metabolizing enzymes and drug transporters in Wilson's disease patients with liver failure.Pharmacological reports : PR · 2021Article
- Imaging-Based Characterization of aPharmaceutics · 2021Article
- Hepatic organic anion transporting polypeptides mediate disposition of milk thistle flavonolignans and pharmacokinetic silymarin-drug interactions.Phytotherapy research : PTR · 2021Article
- Organic Anion Transporting Polypeptide 2B1 (OATP2B1) Genetic Variants:Frontiers in pharmacology · 2021Article
- Organic Cation Transporter 1 an Intestinal Uptake Transporter: Fact or Fiction?Frontiers in pharmacology · 2021Review
Corrections and comments
- Erratum issued
Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
The organic anion transporting polypeptide (OATP)2B1 is localized on the basolateral membrane of hepatocytes and is expressed in enterocytes. Based on its distribution pattern and functional similarity to OATP1B-type transporters, OATP2B1 might have a role in the absorption and disposition of a range of xenobiotics. Although several prescription drugs, including hydroxymethylglutaryl-coenzyme A-CoA reductase inhibitors (statins) such as fluvastatin, are OATP2B1 substrates in vitro, evidence supporting the in vivo relevance of this transporter remains limited, and most has relied on substrate-inhibitor interactions resulting in altered pharmacokinetic properties of the victim drugs. To address this knowledge deficit, we developed and characterized an Oatp2b1-deficient mouse model and evaluated the impact of this transporter on the absorption and disposition of fluvastatin. Consistent with the intestinal localization of Oatp2b1, we found that the genetic deletion or pharmacological inhibition of Oatp2b1 was associated with decreased absorption of fluvastatin by 2- to 3-fold. The availability of a viable Oatp2b1-deficient mouse model provides an opportunity to unequivocally determine the contribution of this transporter to the absorption and drug-drug interaction potential of drugs. SIGNIFICANCE STATEMENT: The current investigation suggests that mice deficient in Oatp2b1 provide a valuable tool to study the in vivo importance of this transporter. In addition, our studies have identified novel potent inhibitors of OATP2B1 among the class of tyrosine kinase inhibitors, a rapidly expanding class of drugs used in various therapeutic areas that may cause drug-drug interactions with OATP2B1 substrates.
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What OpenQuestion holds
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.