Document Detail

P-glycoprotein related drug interactions: clinical importance and a consideration of disease states.
MedLine Citation:
PMID:  20397967     Owner:  NLM     Status:  MEDLINE    
IMPORTANCE OF THE FIELD: P-glycoprotein (P-gp) is the most characterized drug transporter in terms of its clinical relevance for pharmacokinetic disposition and interaction with other medicines. Clinically significant P-gp related drug interactions appear restricted to digoxin. P-gp may act as a major barrier to current and effective drug treatment in a number of diseases including cancer, AIDS, Alzheimer's and epilepsy due to its expression in tumors, lymphocytes, cell membranes of brain capillaries and the choroid plexus. AREAS COVERED IN THIS REVIEW: This review summarizes the current understanding of P-gp structure/function, clinical importance of P-gp related drug interactions and the modulatory role this transporter may contribute towards drug efficacy in disease states such as cancer, AIDS, Alzheimer's and epilepsy. WHAT THE READER WILL GAIN: The reader will gain an understanding that the clinical relevance of P-gp in drug interactions is limited. In certain disease states, P-gp in barrier tissues can modulate changes in regional distribution. TAKE HOME MESSAGE: P-gp inhibition in isolation will not result in clinically important alterations in systemic exposure; however, P-gp transport may be of significance in barrier tissues (tumors, lymphocytes, brain) resulting in attenuated efficacy.
Caroline A Lee; Jack A Cook; Eric L Reyner; Dennis A Smith
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Expert opinion on drug metabolism & toxicology     Volume:  6     ISSN:  1744-7607     ISO Abbreviation:  Expert Opin Drug Metab Toxicol     Publication Date:  2010 May 
Date Detail:
Created Date:  2010-04-19     Completed Date:  2010-07-08     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101228422     Medline TA:  Expert Opin Drug Metab Toxicol     Country:  England    
Other Details:
Languages:  eng     Pagination:  603-19     Citation Subset:  IM    
Pfizer Global Research & Development, Department of Pharmacokinetics, Dynamics & Metabolism, 10646 Science Center Drive, San Diego, CA 92121, USA.
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MeSH Terms
Binding Sites
Biological Transport
Digoxin / pharmacokinetics
Drug Interactions
Gene Expression
P-Glycoprotein / genetics,  metabolism*
Pharmaceutical Preparations / metabolism*
Polymorphism, Genetic
Protein Binding
Reg. No./Substance:
0/P-Glycoprotein; 0/Pharmaceutical Preparations; 20830-75-5/Digoxin

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

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