Effect of the CYP2D610 Genotype on Tolterodine Pharmacokinetics

This study was conducted to investigate the effect of the reduced function allele CYP2D6*10, which can be the cause of an intermediate metabolizer (IM), on tolterodine pharmacokinetics. Tolterodine is mainly metabolized to an active 5-hydroxymethyl metabolite (5-HM) by CYP2D6, and 5-HM is also metab...

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Bibliographic Details
Published in:Drug metabolism and disposition 2010-09, Vol.38 (9), p.1456-1463
Main Authors: Oishi, Masayo, Chiba, Koji, Malhotra, Bimal, Suwa, Toshio
Format: Article
Language:English
Subjects:
Benzhydryl Compounds - pharmacokinetics
Case-Control Studies
Chromatography, High Pressure Liquid
Cresols - pharmacokinetics
Cytochrome P-450 CYP2D6 - genetics
Female
Genotype
Humans
Male
Muscarinic Antagonists - pharmacokinetics
Phenylpropanolamine - pharmacokinetics
Tolterodine Tartrate
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Summary:This study was conducted to investigate the effect of the reduced function allele CYP2D6*10, which can be the cause of an intermediate metabolizer (IM), on tolterodine pharmacokinetics. Tolterodine is mainly metabolized to an active 5-hydroxymethyl metabolite (5-HM) by CYP2D6, and 5-HM is also metabolized by CYP2D6. Asian and white healthy volunteers (n = 108) received once daily multiple doses of tolterodine, and the serum concentrations of tolterodine and 5-HM were measured. All subjects were genotyped for CYP2D6. Tolterodine exposures [area under the curve (AUC)] increased in order of CYP2D6*1/*1 [extensive metabolizer (EM)]
ISSN:0090-9556
1521-009X
DOI:10.1124/dmd.110.033407