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In light of the article "Understanding CYP2D6 and Its Role in Tamoxifen Metabolism" (Smith, 2013), we feel it imperative to comment on the recent, unexpected approval by the U.S. Food and Drug Administration (2013) of the selective serotonin reuptake inhibitor paroxetine as a nonhormonal treatment for menopausal hot flashes. Paroxetine is a strong inhibitor of CYP2D6, the same enzyme system that converts tamoxifen to its active form, endoxifen. Thus, women receiving tamoxifen therapy for hormone-positive breast cancer should be informed of the risk of reducing tamoxifen efficacy with concomitant use of paroxetine to treat their tamoxifen-induced hot flashes (Kaplan & Mahon, 2013). National Comprehensive Cancer Network (2013) guidelines currently recommend against coadministration of strong inhibitors of CYP2D6 with tamoxifen. In addition, a systematic, evidence-based review of interventions to manage hot flashes in women with breast cancer and men with prostate cancer found only two agents likely to be effective, the serotonin-norepinephrine reuptake inhibitor venlafaxine, and gabapentin. Paroxetine was among the many interventions ranked evidence not established (Kaplan et al., 2011).
This article was published in the following journal.
Name: Oncology nursing forum
Oxycodone is partly metabolized to the active metabolite oxymorphone by hepatic CYP2D6 in the liver. Significant genetic variability in CYP2D6 activity affects oxymorphone formation. This study aimed ...
Tamoxifen bioactivation to endoxifen is mediated primarily by CYP2D6; however, considerable variability remains unexplained. Our aim was to perform a comprehensive assessment of the effect of genetic ...
Purpose Endoxifen is a tamoxifen metabolite with potent antiestrogenic activity. Patients and Methods We performed a phase I study of oral Z-endoxifen to determine its toxicities, maximum tolerated do...
Non-adherence to tamoxifen is common in breast cancer survivors and is associated with poor clinical outcomes. This study aimed to understand womens' experiences of taking tamoxifen and to identify fa...
Bupropion, an antidepressant drug has been approved as a racemate containing equal amounts of R- and S- enantiomers. Recently, the chirality of bupropion has received significant attention in the deli...
The investigators plan to examine endoxifen and 4-OH-Tam as a function of the tamoxifen dose in patients with a genetic CYP2D6 polymorphism. The investigators also plan to investigate oth...
Primary objectives of this study is to evaluate the effects of CYP2D6 genotypes on time to progression after tamoxifen treatment in pre- or postmenopausal women with metastatic breast canc...
The purpose of this study is to investigate the impact of CYP2D6 Genotype on the clinical effects of tamoxifen using with samples from prospective randomized multicenter study(ASTRRA).
Tamoxifen is an important drug for the treatment of breast cancer. Used adjuvantly after operation in early breast cancer, tamoxifen reduces annual recurrence rate by half and cancer death...
The aim of the study is to examine whether tamoxifen-treated Israeli breast cancer patients who are CYP2D6 poor metabolizers (CYP2D6*4/*4 genotype) are at higher cancer relapse risk during...
One of the SELECTIVE ESTROGEN RECEPTOR MODULATORS with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the ENDOMETRIUM.
Naturally occurring genetic variations associated with drug response (e.g., dosage, extent and rate of metabolic processes). While these variants are not markers for GENETIC PREDISPOSITION TO DISEASE they influence PHARMACOKINETICS and pharmacodynamics and often occur on genes encoding drug metabolism enzymes and transporters (e.g., ANGIOTENSIN CONVERTING ENZYME; CYTOCHROME P-450 CYP2D6).
Drugs and compounds which inhibit or antagonize the biosynthesis or actions of CYTOCHROME P-450 CYP2D6.
Drugs and compounds that induce the synthesis of CYTOCHROME P-450 CYP2D6.
A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.
Enzymes are proteins that catalyze (i.e., increase the rates of) chemical reactions. In enzymatic reactions, the molecules at the beginning of the process, called substrates, are converted into different molecules, called products. Almost all chemical re...
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