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

No abstract is available for this paper.

• Publication year

  2004

• Venue

  Breast Cancer Research and Treatment

• Publication date

  2004-05-01

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1023/B:BREA.0000025406.31193.e8PMID 15111773
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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

  2003influential reference
• Paroxetine controlled release in the treatment of menopausal hot flashes: a randomized controlled trial.

  2003cited by this paper
• Quantification of tamoxifen and three metabolites in plasma by high-performance liquid chromatography with fluorescence detection: application to a clinical trial.

  2003cited by this paper
• Genotyping for polymorphic drug metabolizing enzymes from paraffin-embedded and immunohistochemically stained tumor samples.

  2003cited by this paper
• Hot flushes.

  2002cited by this paper
• Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism

  2002cited by this paper
• Tamoxifen for prevention of breast cancer: report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study.

  1999cited by this paper
• Tamoxifen in the Treatment of Breast Cancer

  1998cited by this paper
• Tamoxifen in the treatment of breast cancer.

  1998cited by this paper
• Polymorphism of the cytochrome P450 CYP2D6 gene in a European population: characterization of 48 mutations and 53 alleles, their frequencies and evolution.

  1997cited by this paper
• Dose-dependent inhibition of CYP1A2, CYP2C19 and CYP2D6 by citalopram, fluoxetine, fluvoxamine and paroxetine

  1996influential reference
• Effect of tamoxifen on the multidrug-resistant phenotype in human breast cancer cells: isobologram, drug accumulation, and M(r) 170,000 glycoprotein (gp170) binding studies.

  1994cited by this paper
• Debrisoquine/Sparteine Hydroxylation Genotype and Phenotype: Analysis of Common Mutations and Alleles of CYP2D6 in a European Population

  1991cited by this paper
• Oestrogenic activity of tamoxifen and its metabolites on gene regulation and cell proliferation in MCF-7 breast cancer cells.

  1989cited by this paper
• Distribution of 4-hydroxy-N-desmethyltamoxifen and other tamoxifen metabolites in human biological fluids during tamoxifen treatment.

  1989cited by this paper
• Tamoxifen in the treatment of breast cancer.

  1988cited by this paper
• Identification of 4-hydroxy-N-desmethyltamoxifen as a metabolite of tamoxifen in human bile.

  1988cited by this paper
• The pharmacology and clinical uses of tamoxifen.

  1984cited by this paper
• Metabolites of tamoxifen in animals and man: Identification, pharmacology, and significance

  1982cited by this paper
• HOT FLUSHES

  1981cited by this paper
• 17α-Estradiol Is a Biologically Active Estrogen in Human Breast Cancer Cells in Tissue Culture*

  1980cited by this paper
• 17 alpha-Estradiol is a biologically active estrogen in human breast cancer cells in tissue culture.

  1980cited by this paper
• Serum concentrations of tamoxifen and major metabolite during long-term nolvadex therapy, correlated with clinical response.

  1980cited by this paper
• Serum concentrations of tamoxifen and major metabolite during long-term nolvadex therapy, correlated with clinical response.

  1980cited by this paper
• A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding.

  1976cited by this paper
• Dose-dependent inhibition of CYP 1 A 2 , CYP 2 C 19 and CYP 2 D 6 by citalopram , fluoxetine , fluvoxamine and paroxetine

  year unknowncited by this paper

• Biological and computer-aided evaluation of 3-methoxy-13α-estrone-16α-diphenylphosphine oxide as a new antiestrogenic agent

  2025cites this paper
• Supplementation of Tamoxifen with low-dose Endoxifen in breast cancer patients with impaired tamoxifen metabolism (TAMENDOX): a randomized controlled phase 1/2 trial.

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• Implementation of model-informed precision dosing for tamoxifen therapy in patients with breast cancer: A prospective intervention study

  2025cites this paper
• Mono-CYP CHO Model: A Recombinant Chinese Hamster Ovary Cell Platform for Investigating CYP-Specific Tamoxifen Metabolism

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• Uncovering the transcriptomic basis of endoxifen resistance in ER+ breast cancer cells: Insights from bioinformatics analysis.

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• Optical and random laser properties of the novel multifunctional endoxifen derivative (FLTX3) and its potential for the diagnosis of breast cancer resistance.

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• Lack of effects of S-equol-containing supplement on the pharmacokinetics of oral hormone therapy drugs for breast cancer

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• Persistent synergistic antiproliferative and apoptosis induction effects of PGV-1 and tamoxifen or 4-hydroxytamoxifen on ER-positive breast cancer cells

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• Impact of Endocrine Therapy for Cancer on Periodontal Health: A Systematic Review

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• Highly multiplexed design of an allosteric transcription factor to sense novel ligands

  2024cites this paper
• CYP2D6 Phenotype and Breast Cancer Outcomes: A Bias Analysis and Meta-Analysis.

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  2023cites this paper
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  2023cites this paper
• Breast Cancer Risk Reduction: Current Status and Emerging Trends to Increase Efficacy and Reduce Toxicity of Preventive Medication.

  2023cites this paper
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  2023cites this paper
• Early increase in tamoxifen dose in CYP2D6 poor metaboliser breast cancer patients and survival: A propensity score matching analysis.

  2023cites this paper
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  2023cites this paper
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  2023cites this paper
• Refined tamoxifen administration in mice by encouraging voluntary consumption of palatable formulations

  2023cites this paper
• Presurgical Oral Tamoxifen vs Transdermal 4-Hydroxytamoxifen in Women With Ductal Carcinoma In Situ: A Randomized Clinical Trial.

  2023cites this paper
• Innovative Thiosemicarbazones that Induce Multi-Modal Mechanisms to Down-Regulate Estrogen-, Progesterone-, Androgen- and Prolactin-Receptors in Breast Cancer.

  2023cites this paper
• CYP2C19*17 association with higher plasma 4-hydroxy tamoxifen in Pakistani (estrogen-positive) breast cancer patients

  2023cites this paper
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  2022cites this paper
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  2022cites this paper
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  2022cites this paper
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  2022cites this paper
• HSF1 is a driver of leukemia stem cell self-renewal in acute myeloid leukemia

  2022cites this paper
• Comparison of adverse drug reactions between tamoxifen and toremifene in breast cancer patients with different CYP2D6 genotypes: A propensity‐score matched cohort study

  2021cites this paper
• Preliminary Pharmacogenomic-Based Predictive Models of Tamoxifen Response in Hormone-dependent Chilean Breast Cancer Patients

  2021cites this paper
• A critical assessment of the estrogenic potency of benzyl salicylate

  2021cites this paper
• Computational Treatment Simulations to Assess the Need for Personalized Tamoxifen Dosing in Breast Cancer Patients of Different Biogeographical Groups

  2021influential citation
• Pharmacogenetics of tamoxifen therapy in Asian populations: from genetic polymorphism to clinical outcomes

  2021cites this paper
• Metabolic reprograming confers tamoxifen resistance in breast cancer.

  2021cites this paper
• Endoxifen, an Estrogen Receptor Targeted Therapy: from Bench to Bedside.

  2021cites this paper
• Photolytic Fate of (E)- and (Z)-Endoxifen in Water and Treated Wastewater Exposed to Sunlight.

  2021cites this paper
• Effect of Genetic Variability in 20 Pharmacogenes on Concentrations of Tamoxifen and Its Metabolites

  2021cites this paper
• Pharmacological Inhibition of MCT4 Reduces 4-Hydroxytamoxifen Sensitivity by Increasing HIF-1α Protein Expression in ER-Positive MCF-7 Breast Cancer Cells.

  2021cites this paper
• Endocrine disrupting potential of veterinary drugs by in vitro stably transfected human androgen receptor transcriptional activation assays.

  2021cites this paper
• Phase 1 study of Z-endoxifen in patients with advanced gynecologic, desmoid, and hormone receptor-positive solid tumors

  2021cites this paper
• Antioxidant and anti-Inflammation Potentials of Moringa oleifera Aqueous Extract Against breast cancer chemotherapy drug Induced Kidney and Liver Toxicity in Experimental Rats

  2021cites this paper
• Human Family 1–4 cytochrome P450 enzymes involved in the metabolic activation of xenobiotic and physiological chemicals: an update

  2021cites this paper
• Therapeutic Drug Monitoring of Endoxifen for Tamoxifen Precision Dosing: Feasible in Patients with Hormone-Sensitive Breast Cancer

  2021cites this paper
• Generating a Precision Endoxifen Prediction Algorithm to Advance Personalized Tamoxifen Treatment in Patients with Breast Cancer

  2021cites this paper
• Evaluating the Risk of Breast Cancer Recurrence and Metastasis After Adjuvant Tamoxifen Therapy by Integrating Polymorphisms in Cytochrome P450 Genes and Clinicopathological Characteristics

  2021cites this paper
• The crucial role of epigenetic regulation in breast cancer anti-estrogen resistance: current findings and future perspectives.

  2020cites this paper
• Recent advances in the personalized treatment of estrogen receptor-positive breast cancer with tamoxifen: a focus on pharmacogenomics

  2020cites this paper
• Endoxifen and fulvestrant regulate estrogen-receptor α and related DEADbox proteins

  2020cites this paper
• Bifluorescent Analysis of ⍺-Synuclein Aggregation In Vivo

  2020cites this paper
• Managing menopausal symptoms in patients with hormone receptor-positive gynecologic cancers

  2020cites this paper
• Antitumor activity of Z-endoxifen in aromatase inhibitor-sensitive and aromatase inhibitor-resistant estrogen receptor-positive breast cancer

  2020cites this paper
• Obesity alters endoxifen plasma levels in young breast cancer patients: A pharmacometric simulation approach.

  2020cites this paper
• Integrated Data Analysis of Six Clinical Studies Points Toward Model-Informed Precision Dosing of Tamoxifen

  2020cites this paper
• Predicting steady‐state endoxifen plasma concentrations in breast cancer patients by CYP2D6 genotyping or phenotyping. Which approach is more reliable?

  2020cites this paper
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  2020cites this paper
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  2020cites this paper
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  2020cites this paper
• Interaction tamoxifène – clou de girofle : à propos d’un cas d’effet indésirable

  2020cites this paper
• Targeted degradation of activating estrogen receptor α ligand-binding domain mutations in human breast cancer

  2020cites this paper
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  2020cites this paper
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  2020cites this paper
• Clinical Practice Considerations

  2019cites this paper
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  2019cites this paper
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  2019cites this paper
• Estrogens and breast cancer: Mechanisms involved in obesity-related development, growth and progression.

  2019cites this paper
• Pharmacogenomics

  2019cites this paper
• Photodegradation of (E)- and (Z)-Endoxifen in water by ultraviolet light: Efficiency, kinetics, by-products, and toxicity assessment.

  2019cites this paper
• The Effect of Polymorphism in UGT1A4 on Clinical Outcomes of Adjuvant Tamoxifen Therapy for Patients With Breast Cancer in China

  2019cites this paper
• CYP2D6 Genotype-Guided Tamoxifen Dosing in Hormone Receptor-Positive Metastatic Breast Cancer (TARGET-1): A Randomized, Open-Label, Phase II Study.

  2019cites this paper
• The effect of tamoxifen and luteinizing hormone-releasing hormone (LHRH) analogue on estrogen level in women with breast cancer

  2019cites this paper
• Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).

  2019cites this paper
• Non-CYP2D6 Variants Selected by a GWAS Improve the Prediction of Impaired Tamoxifen Metabolism in Patients with Breast Cancer

  2019cites this paper
• The potential influence of breast cancer estrogen receptors’ distribution on active DNA demethylation

  2019cites this paper
• Pharmacogenomics, CYP2D6, and Tamoxifen: A Survey of the Reasons Sustaining European Clinical Practice Paradigms

  2019cites this paper
• The Principles behind Targeted Therapy for Cancer Treatment

  2019cites this paper
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• Incorporation of metabolic enzymes to improve predictivity of reporter gene assay results for estrogenic and anti-androgenic activity.

  2018cites this paper
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  2018cites this paper
• Tamoxifen and CYP2D6: A Controversy in Pharmacogenetics.

  2018cites this paper
• Pharmacogenomics and Pharmacoepigenomics: Impact on Therapeutic Strategies

  2018cites this paper
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  2018cites this paper
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  2018cites this paper
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• Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton.

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• Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives.

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• CYP2D6 as a treatment decision aid for ER-positive non-metastatic breast cancer patients: a systematic review with accompanying clinical practice guidelines

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  2018cites this paper
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  2018cites this paper
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