CYP2D6 genotype, antidepressant use, and tamoxifen metabolism during adjuvant breast cancer treatment

…, JM Rae, DF Hayes, DA Flockhart - Journal of the …, 2005 - academic.oup.com
Background: The efficacy of tamoxifen therapy for the treatment of breast cancer varies widely
among individuals. Plasma concentrations of the active tamoxifen metabolite endoxifen …

Clinical significance of the cytochrome P450 2C19 genetic polymorphism

Z Desta, X Zhao, JG Shin, DA Flockhart - Clinical pharmacokinetics, 2002 - Springer
Cytochrome P450 2C19 (CYP2C19) is the main (or partial) cause for large differences in
the pharmacokinetics of a number of clinically important drugs. On the basis of their ability to …

Active tamoxifen metabolite plasma concentrations after coadministration of tamoxifen and the selective serotonin reuptake inhibitor paroxetine

…, DF Hayes, Z Desta, DA Flockhart - Journal of the …, 2003 - academic.oup.com
Background: Tamoxifen, a selective estrogen receptor modulator (SERM), is converted to 4-hydroxy-tamoxifen
and other active metabolites by cytochrome P450 (CYP) enzymes. …

[HTML][HTML] Pharmacogenetics of tamoxifen biotransformation is associated with clinical outcomes of efficacy and hot flashes

…, FJ Couch, WL Lingle, DA Flockhart… - Journal of Clinical …, 2005 - nlp.case.edu
Purpose Polymorphisms in tamoxifen metabolizing genes affect the plasma concentration of
tamoxifen metabolites, but their effect on clinical outcome is unknown. Methods We …

Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6

…, BA Ward, NV Soukhova, DA Flockhart - Journal of Pharmacology …, 2004 - ASPET
We performed comprehensive kinetic, inhibition, and correlation analyses in human liver
microsomes and experiments in expressed human cytochromes P450 (P450s) to identify …

The cytochrome P450 2B6 (CYP2B6) is the main catalyst of efavirenz primary and secondary metabolism: implication for HIV/AIDS therapy and utility of efavirenz as a …

…, JC Gorski, DR Jones, SD Hall, DA Flockhart… - … of Pharmacology and …, 2003 - ASPET
We used human liver microsomes (HLMs) and recombinant cytochromes P450 (P450s) to
identify the routes of efavirenz metabolism and the P450s involved. In HLMs, efavirenz …

[HTML][HTML] Association of vascular endothelial growth factor and vascular endothelial growth factor receptor-2 genetic polymorphisms with outcome in a trial of paclitaxel …

…, S Badve, A Thor, DA Flockhart… - Journal of Clinical …, 2008 - ncbi.nlm.nih.gov
Purpose No biomarkers have been identified to predict outcome with the use of an
antiangiogenesis agent for cancer. Vascular endothelial growth factor (VEGF) genetic variability has …

The impact of cytochrome P450 2D6 metabolism in women receiving adjuvant tamoxifen

…, AM Nibbe, Z Desta, A Nguyen, DA Flockhart… - Breast cancer research …, 2007 - Springer
Background Tamoxifen is biotransformed to the potent anti-estrogen, endoxifen, by the
cytochrome P450 (CYP) 2D6 enzyme. CYP2D6 genetic variation and inhibitors of the enzyme …

Quantitative effect of CYP2D6 genotype and inhibitors on tamoxifen metabolism: Implication for optimization of breast cancer treatment

…, DF Hayes, V Stearns, DA Flockhart - Clinical …, 2006 - Wiley Online Library
Background and Objectives N‐Desmethyltamoxifen (NDM), a major primary metabolite of
tamoxifen, is hydroxylated by cytochrome P450 (CYP) 2D6 to yield endoxifen. Because of its …

Pharmacological Characterization of 4-hydroxy-N-desmethyl Tamoxifen, a Novel Active Metabolite of Tamoxifen

…, RV Weatherman, Z Desta, DA Flockhart… - Breast cancer research …, 2004 - Springer
The antiestrogen tamoxifen is extensively metabolized in patients to form a series of
compounds with altered affinity for estrogen receptors (ERs), the primary target of this drug. …