Trial reportClinical pharmacology and therapeutics2012
OATP1B1 polymorphism as a determinant of erythromycin disposition.
Trial report in Clinical pharmacology and therapeutics, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 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
17 citing papers in PubMed, 1 synthesis or guideline pooled it, 33 citations in OpenAlex.
- Abundance of Hepatic Transporters in Caucasians: A Meta-Analysis.Drug metabolism and disposition: the biological fate of chemicals · 2016Pooled it
- Pharmacogenomics of antibacterial and antiviral therapies: Clinical actionability, evidence gaps, and future directions.Pharmacological reviews · 2026Review
- Evaluating the Utility and Constraints of the Competitive Counter Flow (CCF) Assay in OATP1B1 Substrate Profiling.The AAPS journal · 2026Article
- Current status of antimicrobial resistance in Indian healthcare system: combating antimicrobial resistance with precision medicine.Frontiers in antibiotics · 2026Review
- OATP1B-type Transport Function Is a Determinant of Aromatase Inhibitor-Associated Arthralgia Susceptibility.Cancer research communications · 2025Article
- Genetic Variations and Antibiotic-Related Adverse Events.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Predicting disruptions to drug pharmacokinetics and the risk of adverse drug reactions in non-alcoholic steatohepatitis patients.Acta pharmaceutica Sinica. B · 2023Review
- Interaction of Antifungal Drugs with CYP3A- and OATP1B-Mediated Venetoclax Elimination.Pharmaceutics · 2022Article
- Influence of Probenecid on the Pharmacokinetics and Pharmacodynamics of Sorafenib.Pharmaceutics · 2020Article
- Pharmacogenomics of Antibiotics.International journal of molecular sciences · 2020Review
- Role of equilibrative nucleoside transporter 1 (ENT1) in the disposition of cytarabine in mice.Pharmacology research & perspectives · 2019Article
- Interaction Between Sex and Organic Anion-Transporting Polypeptide 1b2 on the Pharmacokinetics of Regorafenib and Its Metabolites Regorafenib-N-Oxide and Regorafenib-Glucuronide in Mice.Clinical and translational science · 2019Article
- PharmGKB summary: Macrolide antibiotic pathway, pharmacokinetics/pharmacodynamics.Pharmacogenetics and genomics · 2017Article
- Drug Transporters and Na+/H+ Exchange Regulatory Factor PSD-95/Drosophila Discs Large/ZO-1 Proteins.Pharmacological reviews · 2015Review
- Inhibition of OATP1B1 by tyrosine kinase inhibitors: in vitro-in vivo correlations.British journal of cancer · 2014Article
- Organic anion transporting polypeptide 1B transporters modulate hydroxyurea pharmacokinetics.American journal of physiology. Cell physiology · 2013Article
- Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide.Clinical cancer research : an official journal of the American Association for Cancer Research · 2013Article
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Authors and funding
12 authors at 5 institutions in 3 countries.
Funding
Abstract
Previous studies have demonstrated that the pharmacokinetic profile of erythromycin, a probe for CYP3A4 activity, is affected by inhibitors or inducers of hepatic solute carriers. We hypothesized that these interactions are mediated by OATP1B1 (gene symbol, SLCO1B1), a polypeptide expressed on the basolateral surface of hepatocytes. Using stably transfected Flp-In T-Rex293 cells, erythromycin was found to be a substrate for OATP1B1*1A (wild type) with a Michaelis-Menten constant of ~13 µmol/l, and that its transport was reduced by ~50% in cells expressing OATP1B1*5 (V174A). Deficiency of the ortholog transporter Oatp1b2 in mice was associated with a 52% decrease in the metabolic rate of erythromycin (P = 0.000043). In line with these observations, in humans the c.521T>C variant in SLCO1B1 (rs4149056), encoding OATP1B1*5, was associated with a decline in erythromycin metabolism (P = 0.0072). These results suggest that impairment of OATP1B1 function can alter erythromycin metabolism, independent of changes in CYP3A4 activity.
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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.