Document Detail

Evaluation of pregnane X receptor (PXR)-mediated CYP3A4 drug-drug interactions in drug development.
MedLine Citation:
PMID:  23330538     Owner:  NLM     Status:  In-Data-Review    
The increased capacity to rapidly eliminate drugs can have a profound effect on the efficacious exposure of coadministered drugs, especially in today's medical world of polypharmacy. There are numerous drug-drug interactions (DDIs) related to a loss of therapeutic efficacy and many of these are caused by pregnane X receptor (PXR)-mediated transcriptional activation of drug-metabolizing enzymes or drug transporters. Evaluation of PXR activation and subsequent induction of proteins involved in drug elimination and distribution have become routine in drug discovery and drug development. The assays used to evaluate PXR directly are high throughput and provide useful information on the ability of a drug's potential to precipitate a DDI. In addition, they may serve as useful tools to support structure-activity or structure-liability relationships to eliminate or minimize the potential of new drug candidates to cause induction and, ultimately, a DDI.
Michael W Sinz
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Drug metabolism reviews     Volume:  45     ISSN:  1097-9883     ISO Abbreviation:  Drug Metab. Rev.     Publication Date:  2013 Feb 
Date Detail:
Created Date:  2013-01-21     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0322067     Medline TA:  Drug Metab Rev     Country:  England    
Other Details:
Languages:  eng     Pagination:  3-14     Citation Subset:  IM    
Bristol Myers-Squibb Pharmaceutical Research, Wallingford, Connecticut, USA.
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