TY  - BOOK
AU  - Smith, D Max
TI  - A Scoping Review of the Evidence Behind CYP2D6 Inhibitor Classifications
SN  - 0009-9236
PY  - 2020///
KW  - IN PROCESS -- NOT YET INDEXED
KW  - MedStar Health
KW  - Pharmacogenomics
KW  - Journal Article
N1  - Available online from MWHC library: 1996 - 2006, Available in print through MWHC library: 1999 - 2006
N2  - The FDA lists 22 medications as clinical inhibitors of CYP2D6, with classifications of strong, moderate, and weak. It is accepted that strong inhibitors result in nearly null enzymatic activity, but reduction caused by moderate and weak inhibitors is less well characterized. The objective was to identify if the classification of currently listed FDA moderate and weak inhibitors is supported by publicly available primary literature. We conducted a literature search and reviewed product labels (PLs) for AUC-fold changes caused by inhibitors in humans and identified 89 inhibitor-substrate pairs. Observed AUC-fold change of the substrate was used to create an observed inhibitor classification per FDA-defined AUC-fold change thresholds. We then compared the observed inhibitor classification with the classification listed in the FDA Table of Inhibitors. We found 62% of the inhibitors within the pairs matched the listed FDA classification. We explored reasons for discordance and suggest modifications to the FDA table of clinical inhibitors for cimetidine, desvenlafaxine, and fluvoxamine. Copyright (c) 2020 The Authors Clinical Pharmacology & Therapeutics (c) 2020 American Society for Clinical Pharmacology and Therapeutics
UR  - https://dx.doi.org/10.1002/cpt.1768
ER  -