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Impact of CYP2D6 polymorphisms on the pharmacokinetics of lovastatin in Chinese subjects
Purpose Although CYP3A4/5 enzymes play the predominant role in the metabolism of simvastatin and lovastatin, polymorphisms in CYP2D6 were reported to be associated with the cholesterol-lowering effect and/or tolerability of simvastatin. This study was performed to examine whether common CYP2D6 polym...
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Published in: | European journal of clinical pharmacology 2012-06, Vol.68 (6), p.943-949 |
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Main Authors: | , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | Purpose
Although CYP3A4/5 enzymes play the predominant role in the metabolism of simvastatin and lovastatin, polymorphisms in
CYP2D6
were reported to be associated with the cholesterol-lowering effect and/or tolerability of simvastatin. This study was performed to examine whether common
CYP2D6
polymorphisms affect the pharmacokinetics of lovastatin, which is taken as the inactive prodrug lovastatin lactone and converted to active lovastatin acid.
Methods
A single-dose pharmacokinetic study was performed with lovastatin in 23 Chinese healthy male subjects. Plasma concentrations of lovastatin lactone and acid were determined by an LC-MS-MS method in samples collected over 24 h after single oral doses of 40-mg lovastatin.
Results
Compared with the
CYP2D6 wt/wt
group, the area under the plasma concentration–time curve (AUC
0-∞
) values for lovastatin lactone increased (
P
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ISSN: | 0031-6970 1432-1041 |
DOI: | 10.1007/s00228-011-1202-5 |