Assessment of Activity Levels for CYP2D6*1, CYP2D6*2, and CYP2D6*41 Genes by Population Pharmacokinetics of Dextromethorphan [PDF]
Clinical Pharmacology & Therapeutics, 2010 The pharmacokinetics of dextromethorphan (DM) is markedly influenced by cytochrome P450 2D6 (CYP2D6) enzyme polymorphisms. The aim of this study was to quantify the effects of the CYP2D6*1, *2, and *41 variants on DM metabolism in vivo and to identify other sources of pharmacokinetic variability.
Abduljalil, K +8 more
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Interrogation of CYP2D6 Structural Variant Alleles Improves the Correlation Between CYP2D6 Genotype and CYP2D6‐Mediated Metabolic Activity [PDF]
Clinical and Translational Science, 2020 The cytochrome P450 2D6 (CYP2D6) gene locus is challenging to accurately genotype due to numerous single nucleotide variants and complex structural variation.
Rachel Dalton +17 more
doaj +3 more sources
CYP2D6 Phenotyping Using Urine, Plasma, and Saliva Metabolic Ratios to Assess the Impact of CYP2D6∗10 on Interindividual Variation in a Chinese Population [PDF]
Frontiers in Pharmacology, 2017 Purpose: Asian populations have around 40–60% frequency of reduced function allele CYP2D6∗10 compared to 1–2% in Caucasian populations. The wide range of CYP2D6 enzyme activities in subjects with the CYP2D6∗10 variant is a big concern for clinical ...
Pei Hu, Rui Chen, Xin Zheng
doaj +2 more sources
Induction of CYP2D6 in pregnancy*
Clinical Pharmacology & Therapeutics, 1997 Expression of the drug-metabolizing enzyme cytochrome P4502D6 (CYP2D6) is predominantly under genetic control, and enzyme-inducing drugs have little influence on its activity. We studied the activity of CYP2D6 during pregnancy. One hundred forty pregnant women were genotyped for CYP2D6.
M, Wadelius, E, Darj, G, Frenne, A, Rane
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Clinical and Translational ScienceTramadol, the 41st most prescribed drug in the United States in 2021 is a prodrug activated by CYP2D6, which is highly polymorphic. Previous studies showed enzyme‐inhibitor affinity varied between different CYP2D6 allelic variants with dextromethorphan ...
Noor Ahmed Nahid +4 more
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Development of a CYP2D6-enhanced HepaRG cell model with improved CYP2D6 metabolic capacity.
PLoS ONEDrug-induced liver injury is a major concern in drug development, and the limitations of animal models have driven interest in human-derived in vitro models for toxicity assessment.
Chizuka Obara +5 more
doaj +3 more sources
Metoclopramide is metabolized by CYP2D6 and is a reversible inhibitor, but not inactivator, of CYP2D6 [PDF]
Xenobiotica, 2013 1. Metoclopramide is a widely used clinical drug in a variety of medical settings with rare acute dystonic events reported. The aim of this study was to assess a previous report of inactivation of CYP2D6 by metoclopramide, to determine the contribution of various CYPs to metoclopramide metabolism, and to identify the mono-oxygenated products of ...
Mara R, Livezey +5 more
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Distinct Associations of Age and CYP2D6 Genotype With Parent Venlafaxine Exposure and O-Demethylation in Japanese Psychiatric Patients. [PDF]
Neuropsychopharmacol RepThis TDM study suggests that, in Japanese psychiatric patients receiving venlafaxine, age is associated with dose‐corrected parent‐drug exposure, whereas CYP2D6 genotype predominantly determines the ODV/VEN metabolic ratio. ABSTRACT Background Venlafaxine (VEN) is converted to O‐desmethylvenlafaxine (ODV) mainly through CYP2D6‐mediated O‐demethylation.
Ishihara Y +8 more
europepmc +2 more sources
Expression of Human CYP2D6 in Artificial Cells Based on Polymer-Lipid Hybrid Vesicles. [PDF]
ChembiochemExpression of eGFP and human cytochrome P450 2D6 (CYP2D6) within the lumen of giant polymer‐lipid hybrid vesicles using a Leishmania tarentolae‐based cell‐free protein expression system is illustrated. Both proteins were expressed in the vesicle lumen, and low‐polymer‐content hybrid vesicles were the most suitable scaffolds for CYP2D6 expression with ...
Dahl S +7 more
europepmc +2 more sources
Is CYP2D6 phenotype predictable from CYP2D6 genotype? [PDF]
Microchemical Journal, 2018 Abstract Genetic polymorphism of cytochrome P450s results in clinically significant modifications in patients' drug metabolizing capacities. CYP2D6 has a crucial role in the elimination of several clinically important drugs (antiarrhythmics, beta-adrenergic blockers, psychopharmacons and analgesics); however, the prediction of the phenotypic ...
Ádám Ferenc Kiss +6 more
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