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Updated: May 17, 2026

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Published on: March 28, 2017
Measurement of in vitro cytochrome P450 2B6 activity
Robert L Walsky1, R Scott Obach
1Pfizer Global Research and Development, Groton, Connecticut, USA.
Abstract:
Cytochrome P450 2B6 (CYP2B6) is responsible for the metabolism of a number of therapeutically relevant drugs and environmental chemicals. While not as frequently involved in xenobiotic metabolism as other more commonly studied P450 enzymes such as CYP3A, CYP2D6, or CYP2C9, its importance is becoming increasingly realized. Bupropion hydroxylase activity is an excellent indicator of in vitro CYP2B6 activity, and the metabolite formed is easily measured by HPLC/MS/MS. This assay allows the use of very low concentrations of human liver microsomes or recombinant enzyme, and it represents a selective, sensitive approach to assessing in vitro CYP2B6 activity, with minimal sample preparation.
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