Endoxifen (4-hydroxy-N-desmethyl-tamoxifen) has anti-estrogenic effects in breast cancer cells with potency similar to 4-hydroxy-tamoxifen

Tamoxifen for Prevention of Breast Cancer: Report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study

1998 • 5,487 citations

Two distinct estrogen-regulated promoters generate transcripts encoding the two functionally different human progesterone receptor forms A and B.

1990 • 1,510 citations

Tamoxifen in the Treatment of Breast Cancer

1998 • 1,295 citations

Overview of the main outcomes in breast-cancer prevention trials

2003 • 941 citations

Active Tamoxifen Metabolite Plasma Concentrations After Coadministration of Tamoxifen and the Selective Serotonin Reuptake Inhibitor Paroxetine

2003 • 829 citations

Progesterone Receptor Status Significantly Improves Outcome Prediction Over Estrogen Receptor Status Alone for Adjuvant Endocrine Therapy in Two Large Breast Cancer Databases

2003 • 716 citations

Weighing the Risks and Benefits of Tamoxifen Treatment for Preventing Breast Cancer

1999 • 676 citations

Comprehensive Evaluation of Tamoxifen Sequential Biotransformation by the Human Cytochrome P450 System in Vitro: Prominent Roles for CYP3A and CYP2D6

2004 • 638 citations

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

2004 • 444 citations

Tamoxifen and metabolites in MCF7 cells: correlation between binding to estrogen receptor and inhibition of cell growth.

1982 • 393 citations

The Opposing Transcriptional Activities of the Two Isoforms of the Human Progesterone Receptor Are Due to Differential Cofactor Binding

2000 • 375 citations

Distribution of tamoxifen and its metabolites in rat and human tissues during steady-state treatment.

1991 • 361 citations

Prognostic significance of progesterone receptor levels in estrogen receptor-positive patients with metastatic breast cancer treated with tamoxifen: results of a prospective Southwest Oncology Group study.

1992 • 360 citations

Tamoxifen Therapy for Breast Cancer and Endometrial Cancer Risk

1999 • 348 citations

A third transactivation function (AF3) of human progesterone receptors located in the unique N-terminal segment of the B-isoform.

1994 • 313 citations

Bioactivities, estrogen receptor interactions, and plasminogen activator-inducing activities of tamoxifen and hydroxy-tamoxifen isomers in MCF-7 human breast cancer cells.

1984 • 274 citations

Metabolism of Tamoxifen by Recombinant Human Cytochrome P450 Enzymes: Formation of the 4-Hydroxy, 4′-Hydroxy andN-Desmethyl Metabolites and Isomerization oftrans-4-Hydroxytamoxifen

2002 • 236 citations

Distribution of 4-hydroxy-N-desmethyltamoxifen and other tamoxifen metabolites in human biological fluids during tamoxifen treatment.

1989 • 227 citations

A Randomized Trial of Low-Dose Tamoxifen on Breast Cancer Proliferation and Blood Estrogenic Biomarkers

2003 • 211 citations

Advances in estrogen receptor biology: prospects for improvements in targeted breast cancer therapy

2003 • 204 citations

Tamoxifen and risk of idiopathic venous thromboembolism

1998 • 183 citations

Tamoxifen antiestrogens. A comparison of the activity, pharmacokinetics, and metabolic activation of the cis and trans isomers of tamoxifen

1982 • 169 citations

Identification of 4-hydroxy-N-desmethyltamoxifen as a metabolite of tamoxifen in human bile.

1988 • 112 citations

An amino-terminal truncated progesterone receptor isoform, PRc, enhances progestin-induced transcriptional activity.

1996 • 111 citations

Quantification of tamoxifen and three metabolites in plasma by high-performance liquid chromatography with fluorescence detection: application to a clinical trial

2003 • 92 citations

Facile geometric isomerization of phenolic non-steroidal estrogens and antiestrogens: Limitations to the interpretation of experiments characterizing the activity of individual isomers

1985 • 89 citations

Structure-function relationships of hydroxylated metabolites of tamoxifen that control the proliferation of estrogen-responsive T47D breast cancer cells in vitro.

1990 • 82 citations

Evidence for the existence of a third progesterone receptor protein in human breast cancer cell line T47D.

1994 • 70 citations

Differential Expression of Progestin Receptor Isoforms in the Hypothalamus, Pituitary, and Endometrium of Rhesus Macaques*

1998 • 67 citations

Regulation of progesterone receptor mRNA by oestradiol and antioestrogens in breast cancer cell lines

1989 • 66 citations

Evaluation of tamoxifen plus letrozole with assessment of pharmacokinetic interaction in postmenopausal women with metastatic breast cancer.

1999 • 59 citations

Direct determination of tamoxifen and its four major metabolites in plasma using coupled column high-performance liquid chromatography

1994 • 55 citations

Progesterone Receptor Quantification as a Strong Prognostic Determinant in Postmenopausal Breast Cancer Women under Tamoxifen Therapy

2002 • 50 citations

Tamoxifen and toremifene concentrations in plasma are greatly decreased by rifampin*

1998 • 46 citations

Clinical implication of expression of progesterone receptor form A and B mRNAs in secondary spreading of gynecologic cancers

1997 • 42 citations

Structure-activity relationships of nonisomerizable derivatives of tamoxifen: importance of hydroxyl group and side chain positioning for biological activity.

1991 • 38 citations

Insulin-like growth factors control the regulation of oestrogen and progesterone receptor expression by oestrogens

1997 • 35 citations

New approaches to the endocrine prevention and treatment of breast cancer

2003 • 31 citations

Comparison of the selective estrogen receptor modulator arzoxifene (LY353381) with tamoxifen on tumor growth and biomarker expression in an MCF-7 human breast cancer xenograft model.

2003 • 26 citations

Specific high-performance liquid chromatographic analysis of tamoxifen and its major metabolites by “on-line” extraction and post-column photochemical reaction

1989 • 23 citations

Quantitative estrogen and progesterone receptor levels related to progression-free interval in advanced breast cancer patients treated with megestrol acetate or tamoxifen.

1988 • 16 citations

Induction of the progesterone receptor gene in estrogen target cells monitored by branched DNA signal amplification☆ ☆This work originated at the R.W. Johnson Pharmaceutical Research Institute, Raritan, New Jersey, USA.

2001 • 9 citations