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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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Bibliographic Details
Published in:European journal of clinical pharmacology 2012-06, Vol.68 (6), p.943-949
Main Authors: Yin, Ophelia Qi Ping, Mak, Valiant Wah Lun, Hu, Miao, Fok, Benny Siu Pong, Chow, Moses Sing Sum, Tomlinson, Brian
Format: Article
Language:English
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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  
ISSN:0031-6970
1432-1041
DOI:10.1007/s00228-011-1202-5