| Evaluation of pregnane X receptor (PXR)-mediated CYP3A4 drug-drug interactions in drug development. | |
| | |
MedLine Citation:
|
PMID: 23330538 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
|
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. |
| | |
Authors:
|
Michael W Sinz |
Related Documents
:
|
8097638 - Basic aspects of epilepsy. 2360338 - Seizure with ciprofloxacin and theophylline combined therapy. 150228 - Drug therapy reviews: drug therapy of status epilepticus. 22247888 - A review on mucoadhesive polymer used in nasal drug delivery system. 9692518 - Positional changes and drug interventions in acute respiratory failure. 19371418 - Health facility-based active management of the third stage of labor: findings from a na... |
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 |
Affiliation:
|
Bristol Myers-Squibb Pharmaceutical Research, Wallingford, Connecticut, USA. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Modulating the Formation of Meili Wine Aroma by Pre-fermentative Freezing Process.
Next Document: Regulation of the cytosolic sulfotransferases by nuclear receptors.