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Updated: Mar 9, 2026

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Published on: March 28, 2017
Correlations between the enantio- and regio-selective metabolisms of warfarin
Harumi Takahashi1, Minami Ohara1, Soichi Shibata2
1Department of Biopharmaceutics, Meiji Pharmaceutical University, Tokyo, Japan.
Aim:
To clarify whether the activities of multiple CYPs associated with warfarin metabolism would be correlated with each other.
Methods:
Oral clearances (CLpo) of warfarin enantiomers were estimated in 378 Chinese, Caucasians and African-Americans. The partial metabolic clearances (CLm) for 7-hydroxywarfarin enantiomers were also measured. In addition, CLpo and CLm were determined in a patient on warfarin and rifampicin.
Results:
Correlations between CLpo for warfarin enantiomers existed across the three populations. In addition, there was a significant correlation between the CLm for 7-hydroxylation of warfarin enantiomers. Under induced conditions by rifampicin, there were significant correlations between the enantio- and regio-selective metabolisms of warfarin.
Conclusion:
Metabolic activities of CYP2C9, CYP1A2 and CYP3A4 may be regulated by common transcriptional mechanism(s).
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