Involvement of cytochrome P450 3A enzyme family in the major metabolic pathways of toremifene in human liver microsomes
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Comparative metabolic study between two selective estrogen receptor modulators, toremifene and tamoxifen, in human liver microsomes
2015, Drug Metabolism and PharmacokineticsCitation Excerpt :Plasma concentrations of these active TOR metabolites have not yet been determined. For both TAM and TOR, the main metabolite in the plasma of patients is the NDM metabolite [10,21,22], which is also supported by our in vitro study. Combining the plasma concentration and the anti-estrogenic activity of these metabolites, endoxifen is thought to be the most important with regard to eliciting the clinical effects of TAM therapy in vivo.
Review of therapeutic drug monitoring of anticancer drugs part two - Targeted therapies
2014, European Journal of CancerCitation Excerpt :The majority of newer targeted drugs are extensively metabolised by CYP-enzymes20, whose activity is known to exhibit large inter-individual variability. For instance, tamoxifen is metabolised by CYP2D6 and CYP3A4 [60,61] and toremifene by CYP1A1/2 and CYP3A4 [62]. CYP2A6 is the principal clearance mechanism for letrozole and the plasma concentrations of this drug have shown high interpatient variability [63].
From in vitro hepatic metabolic studies towards human health risk assessment: Two case studies of diuron and carbosulfan
2013, Pesticide Biochemistry and PhysiologyCitation Excerpt :The higher the correlation between the activities, the larger the probability that the respective CYP enzyme is responsible for the metabolism of the xenobiotic. Another approach is to correlate the levels of an individual CYP determined by Western blot analysis against the metabolic activity [32,37,63–66]. Pooled human liver microsomes or individual liver microsomal samples could be used to examine the effect of CYP-selective chemical inhibitors or selective inhibitory antibodies.
Mass spectrometric characterization of urinary toremifene metabolites for doping control analyses
2011, Journal of Chromatography ACitation Excerpt :The use of this approach allowed for the detection and elucidation of several previously unreported metabolites for some doping agents [11,12]. In the case of toremifene, pharmacokinetic and pharmacodynamic studies with detection of toremifene and its metabolites in plasma and faeces, have been reported [13–25]. Few analytical methods for the urinary detection of toremifene administration have been developed [3,14,26–29].
Drug interactions between chemotherapeutic regimens and antiepileptics
2008, Clinical TherapeuticsCytochromes P450 from family 4 are the main omega hydroxylating enzymes in humans: CYP4F3B is the prominent player in PUFA metabolism
2008, Journal of Lipid ResearchCitation Excerpt :Four human liver microsomes were assayed for PUFA metabolism. They were obtained from a liver microsome bank built up over many years in our laboratory (36). Ethical committee approval was obtained before studies in accordance with French law.