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Publications

Global marine pollutants inhibit P-glycoprotein: Environmental levels, inhibitory effects, and cocrystal structure

The world’s oceans are a global reservoir of persistent organic pollutants to which Humans and other animals are exposed. Although it is well known that...

The reliability of estimating Ki values for direct, reversible inhibition of cytochrome P450 enzymes from corresponding IC50 values: A retrospective analysis of 343 experiments

Lois J. Haupt, Faraz Kazmi, Brian W. Ogilvie, David B. Buckley, Brian D. Smith, Sarah Leatherman, Brandy Paris, Oliver Parkinson, and Andrew Parkinson In the...

Further Characterization of the Metabolism of Desloratadine and its Cytochrome P450 and UDP-Glucuronosyltransferase (UGT) Inhibition Potential: Identification of Desloratadine as a Relatively Selective UGT2B10 Inhibitor

Presented by: Faraz Kazmi, Phyllis Yerino, Joanna E Barbara, and Andrew Parkinson Desloratadine (Clarinex), the major active metabolite of loratadine (Claritin), is a non-sedating antihistamine...

A long-standing mystery solved: The formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UGT2B10 is an obligatory requirement

Faraz Kazmi, Joanna E. Barbara, Phyllis Yerino and Andrew Parkinson Desloratadine (Clarinex®), the major active metabolite of loratadine (Claritin®), is a non-sedating long-lasting antihistamine widely used for...

Anti-CD28 Monoclonal Antibody-stimulated Cytokines Released from Blood Suppress CYP1A2, CYP2B6 and CYP3A4 in Human Hepatocytes In Vitro

Maciej Czerwiński, Faraz Kazmi, Andrew Parkinson, and David B. Buckley Like most infections and certain inflammatory diseases, some therapeutic proteins cause a cytokine-mediated suppression of...

Drugs as Victims and Perpetrators and the Pharmacokinetic Concept of Maximum Exposure

Brian W. Ogilvie, Andrew Parkinson This article describes the dramatic but predictable impact of two perpetrators on the disposition of a victim drug. For a...

In vitro inhibition of human liver cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes by rose bengal: system-dependent effects on inhibitory potential

Faraz Kazmi, Lois J. Haupt, Jennifer R. Horkman, Brian D. Smith, David B. Buckley, Eric A. Wachter, and Jamie M. Singer 1. Rose bengal (4,5,6,7-tetrachloro-2′,4′,5′,7′-tetraiodofluorescein)...

2012 EMA Final Agency Guideline, “Guideline on the Investigation of Drug Interactions”

European Medicines Agency Guideline on the Investigation of Drug Interactions, revised June 2012. You might also be interested in our 2018 poster comparing current regulatory...

Exploring the Utility of High-Resolution MS with Post-Acquisition Data Mining for Simultaneous Exogenous and Endogenous Metabolite Profiling

Exploring the Utility of High-Resolution MS with Post-Acquisition Data Mining for Simultaneous Exogenous and Endogenous Metabolite Profiling Presented by: Barbara JE, Buckley DB, Horrigan MJ...

Metabolism-Dependent Inhibition of CYP3A4 by Lapatinib: Evidence for Formation of a Metabolic Intermediate Complex with a Nitroso/Oxime Metabolite Formed via a Nitrone Intermediate

Barbara JE, Kazmi F, Parkinson A, Buckley DB Metabolism-dependent inhibition (MDI) of cytochrome P450 (P450) enzymes has the potential to cause clinically relevant drug-drug interactions....