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Updated: Nov 15, 2025

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Published on: January 27, 2013
Drug-Drug Interactions at Organic Cation Transporter 1
Shiwei Zhou1,2,3, Sujuan Zeng1, Yan Shu1,2
1Key Laboratory of Oral Medicine, School and Hospital of Stomatology, Guangzhou Medical University, Guangzhou, China.
Abstract:
The interaction between drugs and various transporters is one of the decisive factors that affect the pharmacokinetics and pharmacodynamics of drugs. The organic cation transporter 1 (OCT1) is a member of the Solute Carrier 22A (SLC22A) family that plays a vital role in the membrane transport of organic cations including endogenous substances and xenobiotics. This article mainly discusses the drug-drug interactions (DDIs) mediated by OCT1 and their clinical significance.
Insights
Organic cation transporter 1 (OCT1) influences drug behavior. This review explores OCT1-mediated drug-drug interactions (DDIs) and their clinical importance, highlighting transporter roles in pharmacokinetics and pharmacodynamics.
Area of Science:
- Pharmacology
- Molecular Biology
- Drug Metabolism
Background:
- Drug interactions significantly impact pharmacokinetics and pharmacodynamics.
- Organic cation transporter 1 (OCT1), part of the Solute Carrier 22A (SLC22A) family, is crucial for transporting organic cations.
- OCT1 facilitates the movement of endogenous substances and xenobiotics across cell membranes.
Purpose of the Study:
- To review drug-drug interactions (DDIs) mediated by OCT1.
- To discuss the clinical significance of OCT1-mediated DDIs.
Main Methods:
- Literature review of studies investigating OCT1.
- Analysis of reported OCT1-mediated drug-drug interactions.
- Evaluation of the clinical implications of these interactions.
Main Results:
- OCT1 plays a key role in the disposition of various drugs.
- Several drugs have been identified as OCT1 substrates, inhibitors, or inducers.
- These interactions can lead to significant alterations in drug plasma concentrations and therapeutic outcomes.
Conclusions:
- OCT1-mediated DDIs are clinically relevant and can affect patient treatment.
- Understanding OCT1's role is essential for predicting and managing drug interactions.
- Further research is needed to fully elucidate the clinical impact of OCT1 in drug therapy.
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