Cytochrome P450 3A Time-Dependent Inhibition Assays are Too Sensitive for Identification of Drugs Causing Clinically Significant Drug-Drug Interactions: A Comparison of Human Liver Microsomes and Hepatocytes and Definition of Boundaries for Inactivation Rate Constants

Heather Eng; Elaine Tseng; Matthew A. Cerny; Theunis C. Goosen; R. Scott Obach

doi:10.1124/dmd.121.000356

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Cytochrome P450 3A Time-Dependent Inhibition Assays are Too Sensitive for Identification of Drugs Causing Clinically Significant Drug-Drug Interactions: A Comparison of Human Liver Microsomes and Hepatocytes and Definition of Boundaries for Inactivation Rate Constants

Heather Eng, Elaine Tseng, Matthew A. Cerny, Theunis C. Goosen and R. Scott Obach

Drug Metabolism and Disposition April 2, 2021, DMD-AR-2021-000356; DOI: https://doi.org/10.1124/dmd.121.000356

Heather Eng

1Pharmacokinetics, Dynamics, and Metabolism, Pfizer Global Research and Development, United States of America

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For correspondence: r.scott.obach@pfizer.com

Elaine Tseng

2Pfizer, United States of America

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Matthew A. Cerny

3PDM, Pfizer Global Research and Development, United States of America

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Theunis C. Goosen

4Pharmacokinetics, Dynamics & Metabolism, Pfizer, Inc, United States of America

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R. Scott Obach

5Groton Laboratories, Pfizer Global Research and Development, United States of America

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For correspondence: r.scott.obach@pfizer.com

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Drug Metabolism and Disposition

Vol. 49, Issue 5

1 May 2021

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