Document Detail

Role of organic cation transporters in drug-induced toxicity.
MedLine Citation:
PMID:  21241199     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: Membrane transporters are important determinants of in vivo drug disposition, therapeutic efficacy and adverse drug reactions. Many commonly used drugs are organic cations and substrates of organic cation transporters (OCTs). These transporters have a large binding site containing partially overlapping interaction domains for different substrates and are specifically distributed around the body. Consequently, drug interactions with these transporters can result in specific toxicity.
AREAS COVERED: This review describes the general properties of OCT and illustrates their importance for the development of important drug toxicities using the examples of metformin and cisplatin. Additionally, this review discusses the role of OCT polymorphisms in the modulation of these toxic effects.
EXPERT OPINION: Understanding how drugs interact with membrane transporters is pivotally important in explaining the mechanisms of specific toxicities and also in designing new drugs or new therapeutic protective protocols by specific competition at the transporter. Defining the pharmacogenomics of these transporters will be essential to personalized medicine, enabling physicians to choose drugs for patients based on efficacy, availability, cost, safety, tolerability and convenience.
Giuliano Ciarimboli
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review    
Journal Detail:
Title:  Expert opinion on drug metabolism & toxicology     Volume:  7     ISSN:  1744-7607     ISO Abbreviation:  Expert Opin Drug Metab Toxicol     Publication Date:  2011 Feb 
Date Detail:
Created Date:  2011-01-18     Completed Date:  2011-07-27     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  101228422     Medline TA:  Expert Opin Drug Metab Toxicol     Country:  England    
Other Details:
Languages:  eng     Pagination:  159-74     Citation Subset:  IM    
Medizinische Klinik und Poliklinik D, Experimentelle Nephrologie, Universitätsklinikum Münster, Domagkstr. 3a, 48149 Münster, Germany.
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MeSH Terms
Binding Sites
Drug Toxicity / genetics,  metabolism*
Kidney / metabolism
Molecular Targeted Therapy
Organic Cation Transport Proteins / chemistry,  genetics,  metabolism*
Pharmaceutical Preparations / metabolism*
Polymorphism, Genetic*
Reg. No./Substance:
0/Organic Cation Transport Proteins; 0/Pharmaceutical Preparations

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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