rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2010-10-27
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pubmed:abstractText |
Imatinib is a clinically important inhibitor of tyrosine kinases that are dysregulated in chronic myelogenous leukaemia and gastrointestinal stromal tumours. Inter-individual variation in imatinib pharmacokinetics is extensive, and influences drug safety and efficacy. Hepatic cytochrome P450 (CYP) 3A4 has been implicated in imatinib N-demethylation, but the clearance of imatinib decreases during prolonged therapy. CYP3A phenotype correlates with imatinib clearance at the commencement of therapy, but not at steady state. The present study evaluated the possibility that multiple CYPs may contribute to imatinib oxidation in liver.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Aryl Hydrocarbon Hydroxylases,
http://linkedlifedata.com/resource/pubmed/chemical/CYP2C8 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/CYP3A4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 CYP3A,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 Enzyme System,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/imatinib
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1476-5381
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pubmed:author |
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pubmed:copyrightInfo |
© 2010 The Authors. British Journal of Pharmacology © 2010 The British Pharmacological Society.
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pubmed:issnType |
Electronic
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pubmed:volume |
161
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1059-69
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pubmed:dateRevised |
2011-11-1
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pubmed:meshHeading |
pubmed-meshheading:20977456-Aryl Hydrocarbon Hydroxylases,
pubmed-meshheading:20977456-Chromatography, Liquid,
pubmed-meshheading:20977456-Cytochrome P-450 CYP3A,
pubmed-meshheading:20977456-Cytochrome P-450 Enzyme System,
pubmed-meshheading:20977456-Enzyme Inhibitors,
pubmed-meshheading:20977456-Humans,
pubmed-meshheading:20977456-Microsomes, Liver,
pubmed-meshheading:20977456-Models, Molecular,
pubmed-meshheading:20977456-Oxidation-Reduction,
pubmed-meshheading:20977456-Piperazines,
pubmed-meshheading:20977456-Protein Kinase Inhibitors,
pubmed-meshheading:20977456-Pyrimidines,
pubmed-meshheading:20977456-Tandem Mass Spectrometry
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pubmed:year |
2010
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pubmed:articleTitle |
Participation of CYP2C8 and CYP3A4 in the N-demethylation of imatinib in human hepatic microsomes.
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pubmed:affiliation |
Pharmacogenomics and Drug Development Group, Faculty of Pharmacy, University of Sydney, NSW, Australia.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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