Source:http://linkedlifedata.com/resource/pubmed/id/17425754
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2007-4-11
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pubmed:abstractText |
The intestinal efflux pump P-glycoprotein (P-gp), the product of the multi-drug resistance-1 (MDR-1) gene, significantly influences the pharmacokinetics of several drugs. Ciclosporin is a substrate for P-gp and is metabolized by cytochrome P450 (CYP) 3A enzymes. P-gp activity is affected by several known single nucleotide polymorphisms (SNPs) and haplotypes. MDR-1 genotypes of SNPs C1236T, G2677T/A and C3435T, as well as haplotypes C-G-C and T-T-T and CYP3A5*1 genotype (predictive of CYP3A5 expression), were related to ciclosporin blood concentrations measured at both 0 and 2 h after drug dosing in 197 stable renal transplant patients. Significant differences (of a magnitude unlikely to be relevant clinically) in dose-normalized blood ciclosporin concentrations were found only between MDR-1 genotypes of the C1236T SNP and between haplotype groups C-G-C and T-T-T in patients that were expressers of CYP3A5. MDR-1 SNPs and haplotypes and also CYP3A5*1 genotype, do not appear to have a major influence on ciclosporin pharmacokinetics.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/CYP3A5 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclosporine,
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/Immunosuppressive Agents,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein
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pubmed:status |
MEDLINE
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pubmed:issn |
0902-0063
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
252-7
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:17425754-Adult,
pubmed-meshheading:17425754-Aged,
pubmed-meshheading:17425754-Aged, 80 and over,
pubmed-meshheading:17425754-Cyclosporine,
pubmed-meshheading:17425754-Cytochrome P-450 CYP3A,
pubmed-meshheading:17425754-Cytochrome P-450 Enzyme System,
pubmed-meshheading:17425754-Female,
pubmed-meshheading:17425754-Genes, MDR,
pubmed-meshheading:17425754-Genotype,
pubmed-meshheading:17425754-Haplotypes,
pubmed-meshheading:17425754-Humans,
pubmed-meshheading:17425754-Immunosuppressive Agents,
pubmed-meshheading:17425754-Kidney Transplantation,
pubmed-meshheading:17425754-Middle Aged,
pubmed-meshheading:17425754-P-Glycoprotein
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pubmed:articleTitle |
Multi-drug resistance gene-1 (MDR-1) haplotypes and the CYP3A5*1 genotype have no influence on ciclosporin dose requirements as assessed by C0 or C2 measurements.
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pubmed:affiliation |
Analytical Unit, Cardiac & Vascular Science, St George's University of London, London, UK. frederic@sgul.ac.uk
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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