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Cancer Treatment Reviews
Volume 26, Issue 3
, Pages 205-227
, June 2000
Selective oestrogen receptor modifiers (SERMs) and breast cancer therapy
References
- REFERENCES
- . A new anti-oestrogenic agent in late breast cancer. An early clinical appraisal of ICI46474. Br J Cancer. 1971;25:270–275
- Lancet. 1992;339:1–15
- . Tamoxifen for early breast cancer: an overview of the randomised trials. Lancet. 1998;351:1451–1467
- J Natl Cancer Inst. 1996;88:1543–1549
- . Prevention of breast cancer with tamoxifen: preliminary findings from the Italian randomised trial among hysterectomised women. Italian Tamoxifen Prevention Study. Lancet. 1998;352:93–97
- . Interim analysis of the incidence of breast cancer in the Royal Marsden Hospital tamoxifen randomised chemoprevention trial. Lancet. 1998;352:98–101
- . Tamoxifen for prevention of breast cancer: report of the National Surgical Adjuvant Breast, Bowel Project P-1 Study. J Natl Cancer Inst. 1998;90:1371–1388
- . The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. Multiple Outcomes of Raloxifene Evaluation. JAMA. 1999;281:2189–2197
- . Clinical pharmacology of selective estrogen receptor modulators. Drug Aging. 1999;14:323–336
- . Selective estrogen receptor modulators: a look ahead. Drugs. 1999;57:653–663
- . Selective estrogen receptor modulators: women’s panacea for the next millenium?. Am J Obstet Gynecol. 1999;180:763–770
- . Adjuvant tamoxifen in primary breast cancer: influence on plasma lipids and antithrombin III levels. Breast Cancer Res Treat. 1988;12:307–310
- . Effect of tamoxifen on estrogen binding, lipid and lipoprotein concentrations and blood clotting parameters in premenopausal women with breast pain. J Endocrinol. 1988;119:335–339
- . Effects of tamoxifen therapy on lipid and lipoprotein levels in postmenopausal patients with node-negative breast cancer. J Natl Cancer Inst. 1990;82:1327–1332
-
.
Long term effects of tamoxifen on blood lipid values in breast cancer.
Br Med J. 1992;305:225–226
- . Effect of tamoxifen on plasma lipids and lipoproteins in postmenopausal women with breast cancer. Cancer. 1994;73:659–663
- . Plasma levels of the atherogenic amino acid homocysteine in postmenopausal women with breast cancer treated with tamoxifen. Int J Cancer. 1994;60:365–368
- . Tamoxifen reduces plasma homocysteine levels in healthy women. Br J Cancer. 1998;77:2264–2266
- . Serum homocysteine levels in postmenopausal breast cancer patients treated with tamoxifen. Cancer Lett. 1999;145:73–77
- . Long-term adjuvant tamoxifen in early breast cancer: effect on bone mineral density in postmenopausal women. J Clin Oncol. 1990;8:1019–1024
- . Effects of tamoxifen on bone mineral density in postmenopausal women with breast cancer. N Engl J Med. 1992;326:852–856
-
.
Effect of long term tamoxifen treatment on bone turnover in women with breast cancer.
Br Med J. 1993;306:429–430
- . Effect of tamoxifen on bone mineral density measured by dual-energy X-ray absorptiometry in healthy premenopausal and postmenopausal women. J Clin Oncol. 1996;14:78–84
- . Tamoxifen, serum lipoproteins and cardiovascular risk. Br J Cancer. 1988;58:497–499
- . Response to a specific antioestrogen (ICI 182780) in tamoxifen-resistant breast cancer. Lancet. 1995;345:29–30
- . Multicenter phase-II efficacy trial of toremifene in tamoxifen-refractory patients with advanced breast cancer. J Clin Oncol. 1993;11:345–350
- . Toremifene and tamoxifen in advanced breast cancer – a double-blind cross-over trial. Breast Cancer Res Treat. 1993;25:57–63
-
.
Phase I study of a third-generation selective estrogen receptor modulator (SERM3, LY353381.HCI) in refractory, metastatic breast cancer.
Breast Cancer Res Treat. 1998;50:442
- . Idoxifene: report of a phase I study in patients with metastatic breast cancer. Cancer Res. 1995;55:1070–1074
- . Identification of an estrogen response element activated by metabolites of 17 beta-estradiol and raloxifene. Science. 1996;273:1222–1225
- . Identification of an estrogen response element activated by metabolites of 17 beta-estradiol and raloxifene (Vol 273, pg 1222, 1996). Science. 1997;275:1249–1249
- . Synthesis and pharmacology of conformationally restricted raloxifene analogues: Highly potent selective estrogen receptor modulators. J Med Chem. 1998;41:1272–1283
- . The selective estrogen receptor modulator, raloxifene: an overview of nonclinical pharmacology and reproductive and developmental testing. Reprod Toxicol. 1998;12:217–221
- . Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women. N Engl J Med. 1997;337:1641–1647 26–6
- . Treatment of established postmenopausal osteoporosis with raloxifene: a randomized study. J Bone Miner Res. 1998;13:1747–1754
- . Randomized, double-blind, placebo-controlled study of the effects of raloxifene and conjugated equine estrogen on plasma homocysteine levels in healthy postmenopausal women. Fertil Steril. 1998;70:1085–1089
- . Effects of raloxifene on serum lipids and coagulation factors in healthy postmenopausal women. JAMA. 1998;279:1445–1451
-
.
Raloxifene does not cause endometrial proliferation in postmenopausal women.
J Soc Gynecol Invest. 1996;3(Suppl. 2):147A
- . Assay for levormeloxifene, a selective estrogen receptor modulator, in human and monkey plasma employing high-performance liquid chromatography and solid-phase extraction. J Chromatogr B Biomed Sci Appl. 1999;729:315–322
- . Blocade of the stimulatory effects of estrogen, OH-tamoxifen, OH-toremifene, droloxifene, and raloxifene on alkaline phosphatase activity by the antiestrogen EM-800 in human endometrial adenocarcinoma ishikawa cells. Cancer Res. 1997;57:3494–3497
- . Characterization of the effects of the novel non-steroidal antiestrogen EM-800 on basal and estrogen-induced proliferation of T-47D, ZR-75-1 and MCF-7 human breast cancer cells in vitro. Int J Cancer. 1997;73:104–112
- . Ligand-independent activation of the estrogen receptors alpha and beta by mutations of a conserved tyrosine can be abolished by antiestrogens. Cancer Res. 1998;58:877–881
- . Basic guide to the mechanisms of antiestrogen action. Pharmacol Rev. 1998;50:151–196
- . Mechanisms of action of endocrine treatment in breast cancer. Crit Rev Oncol Hematol. 1995;21:158–193
- . Functional domains of the human estrogen receptor. Cell. 1987;51:941–951
- . The hormone-binding domains of the estrogen and glucocorticoid receptors contain an inducible transcription activation function. Cell. 1988;54:199–207
- . The steroid receptor coactivator-1 contains multiple receptor interacting and activation domains that cooperatively enhance the activation function 1 (AF1) and AF2 domains of steroid receptors. J Biol Chem. 1998;273:12101–12108
-
.
Antioestrogen ICI 164384 reduced cellular estrogen receptor content by increasing its turnover.
Proc Natl Acad Sci USA. 1992;89:4037–4041
-
.
Effects of antioestrogens on the DNA binding activity of oestrogen receptors in vitro.
Nucl Acid Res. 1992;20:3839–3844
- . A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991;51:3867–3873
- . Molecular basis of agonism and antagonism in the oestrogen receptor. Nature. 1997;389:753–758
-
.
Estrogen receptor variants.
J Mammary Gland Biol Neoplasi. 1998;3:73–83
- . Variant human breast tumor estrogen receptor with constitutive transcriptional activity. Cancer Res. 1991;51:105–109
- . In search of the perfect SERM: beyond tamoxifen and raloxifene. J Natl Cancer Inst. 1998;90:956–957
-
.
Analysis of estrogen receptor transcriptional enhancement by a nuclear hormone receptor coactivator.
Proc Natl Acad Sci USA. 1996;93:10069–10073
- . A regulatory role for RIP140 in nuclear receptor activation. Mol Endocrinol. 1998;12:864–881
- . Predictive value of SRC-1 for tamoxifen response of recurrent breast cancer. Breast Cancer Res Treat. 1998;48:87–92
- . RIP 140 enhances nuclear receptor-dependent transcription in vivo in yeast. Mol Endocrinol. 1997;11:193–202
- . Isoforms of steroid receptor co-activator 1 differ in their ability to potentiate transcription by the oestrogen receptor. EMBO J. 1998;17:232–243
-
.
Cloning of a novel receptor expressed in rat prostate and ovary.
Proc Natl Acad Sci USA. 1996;93:5925–5930
- . ER β identification and characterization of a novel human estrogen receptor. FEBS Letters. 1996;392:49–53
- . Estrogen receptor-beta messenger RNA expression in human breast tumor biopsies: relationship to steroid receptor status and regulation by progestins. Cancer Res. 1999;59:529–532
-
.
Estrogen receptor beta is coexpressed with ERalpha and PR and associated with nodal status, grade, and proliferation rate in breast cancer.
Am J, Pathol. 2000;156:29–35
- . Estrogen receptor-beta: implications for the prostate gland. Prostate. 1999;40:115–124
- . Differential ligand activation of estrogen receptors ER alpha and ER beta at AP1 sites. Science. 1997;277:1508–1510
- . Pharmacology of new aromatase inhibitors. Breast. 1996;5:202–208
- . Biologic activity of tamoxifen at low doses in healthy women. J Natl Cancer Inst. 1998;90:1461–1467
- . Effect of blood tamoxifen concentrations on surrogate biomarkers in a trial of dose dose reduction. J Clin Oncol. 1999;17:2633–2638
- . Influence of droloxifene (3-hydroxytamoxifen), 40 mg daily, on plasma gonadotrophins, sex hormone binding globulin and estrogen levels in postmenopausal breast cancer patients. J Steroid Biochem Mol Biol. 1995;55:193–195
- . Influence of aminoglutethimide on plasma levels of estrone sulphate and dehydroepiandrosterone sulphate in postmenopausal breast cancer patients. J Steroid Biochem Mol Biol. 1997;63:53–58
- . Influence of droloxifene on plasma levels of insulin-like growth factor (IGF)-I, pro-IGF-IIE, insulinlike growth factor binding protein (IGFBP)-1 and IGFBP-3 in breast cancer patients. J Steroid Biochem Mol Biol. 1996;57:167–171
- . Influence of tamoxifen on plasma levels of insulin-like growth factor I and insulin-like growth factor binding protein I in breast cancer patients. Cancer Res. 1992;52:4719–4723
- . Influence of tamoxifen, aminoglutethimide and goserelin on human plasma IGF-I levels in breast cancer patients. J Steroid Biochem Mol Biol. 1992;41:541–543
- . Alteration of endocrine parameters in premenopausal women with breast cancer during long term adjuvant therapy with tamoxifen as the single agent. J Natl Cancer Inst. 1991;83:1488–1491
- . Endocrine effects of adjuvant chemotherapy and long-term tamoxifen administration on node-positive patients with breast cancer. Cancer Res. 1987;47:624–630
- . Long-term adjuvant therapy with tamoxifen: effects on sex hormone binding globulin and antitrombin III. Cancer Res. 1987;47:4517–4519
-
.
Influence of tamoxifen on sex hormones, gonadotrophins and sex hormone binding globulin in postmenopausal breast cancer patients.
J Ster Biochem Mol Biol. 1995;52:491–496
- . Sequential combination of tamoxifen and high dose medroxyprogesterone acetate: therapeutic and endocrine effects in postmenopausal advanced breast cancer patients. Eur J Cancer Clin Oncol. 1987;23:1451–1459
- . Hormonal and receptor status in postmenopausal women with endometrial carcinoma before and after treatment with tamoxifen. Tumori. 1984;70:189–192
- . Endocrine effects of tamoxifen in postmenopausal breast cancer patients. Tumori. 1984;70:61–68
- . Paired-ion chromatographic analysis of tamoxifen and two major metabolites in plasma. J Chromatogr. 1980;181:41–49
- . Clinical analysis of tamoxifen, an anti-neoplastic agent, in plasma. Clin Chem. 1978;24:1518–1524
-
.
Analysis of tamoxifen in biological samples.
Symp Bologna (Oncol). 1985;83–89
- . Determination of tamoxifen and an hydroxylated metabolite in plasma from patients with advanced breast cancer using gas chromatography – mass spectrometry. J Endocrinol. 1979;83:401–408
- . Determination of tamoxifen in rat plasma by gas chromatography – mass spectrometry. J Endocrinol. 1978;78:293–294
- . Determination of tamoxifen and biologically active metabolites in human breast tumours and plasma. Eur J Cancer Clin Oncol. 1981;17:1183–1189
- . Analysis of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen levels in cytosol and KCI-nuclear extracts of breast tumors from tamoxifen treated patients by gas chromatography-mass spectrometry (GC-MS) using selected ion monitoring (SIM). J Steroid Biochem. 1987;28:609–618
- . Identification of 4-hydroxy-N-desmethyltamoxifen as a metabolite of tamoxifen in human bile. Cancer Res. 1988;48:2304–2308
- . Quantitative measurement of 4-hydroxy tamoxifen in human plasma and mammary tumours by combined gas chromatography/negative chemical ionization mass spectrometry. Biol Mass Spectrom. 1993;22:395–402
- . High-performance liquid chromatographic analysis of tamoxifen and major metabolites in human plasma. J Chromatogr. 1983;275:436–442
- . Determination of tamoxifen and metabolites in human serum by high-performance liquid chromatography with post-column fluorescence activation. J Chromatogr. 1983;272:351–358
-
.
Quantitation of tamoxifen, 4-hydroxytamoxifen, and N-desmethyltamoxifen in human plasma by high performance liquid chromatography.
Anal Letters. 1985;18:1915–1924
- . Determination of tamoxifen and four metabolites in serum by low-dispersion liquid chromatography. Clin Chem. 1987;33:1608–1614
- . Optimised analysis of tamoxifen and its main metabolites in the plasma and cytosol of mammary tumours. Br J Cancer. 1987;55:509–512
-
.
Determination of tamoxifen and five metabolites in plasma.
J Pharmaceut Biomed Anal. 1988;6:1065–1068
- . Tamoxifen metabolites in patients on long-term adjuvant therapy for breast cancer. Eur J Cancer. 1990;26:883–888
- . Quantification of tamoxifen and N-desmethyltamoxifen in human plasma by high-performance liquid chromatography, photochemical reaction and fluorescence detection, and its application to biopharmaceutical investigations. J Chromatogr. 1987;413:207–217
- . A comparative study of tamoxifen metabolism in female rat, mouse and human liver microsomes. Carcinogenesis. 1994;15:589–593
- . High performance liquid chromatography of tamoxifen and metabolites in plasma and tissues. biomed Chromatogr. 1993;7:311–314
-
.
High performance liquid chromatography of toremifene and metabolites.
J Liq Chromatogr. 1994;17:1773–1783
- . Tissue distribution of transdermal toremifene. Cancer Chemother Pharmacol. 1997;39:513–520
- . Determination of droloxifene and two metabolites in serum by high-pressure liquid chromatography. Ther Drug Monit. 1994;17:259–265
-
.
Sensitive method for the quantitation of droloxifene in plasma and serum by high-performance liquid chromatography employing fluorimetric detection.
J Chromatogr B Biomed Appl. 1995;674:253–260
- . Optimised separation of E-, Z-isomers of tamoxifen, and its principal metabolites using reversed-phase high performance liquid chromatography. J Pharm Biomed Anal. 1998;16:847–852
- . Disposition and metabolism of a new benzothiophene antiestrogen in rats, dogs and monkeys. Xenobiotica. 1984;14:841–847
-
.
Anti-hormonal agents. VI. Direct plasma analyses of tamoxifen by HPLC using an on-line ISRP extraction cartridge.
J Liquid Chromatogr. 1990;13:2253–2260
-
.
Solid phase extraction and high performance liquid chromatography of tamoxifen and its demethylated metabolites in plasma.
Analyt Lett. 1998;31:2679–2690
-
.
Rapid and simple method to determine tamoxifen and its major metabolites in human liver microsomesby high performance liquid chromatography with fluorescence detection.
Anal Lett. 1998;31:2067–2076
-
.
Direct determination of droloxifene in serum using HPLC with precolumn switching, post-column photochemical derivatization and fluorescence detection. Third European congress of biopharmaceutics and pharmacokinetics. Proceedings.
In:
Aiache JM, Hirtz J editor. Pharmaceutics. France: Clermont-Ferrand; 1987;p. 511–520
-
.
Solid-phase extraction and high-performance liquid chromatographic determination of tamoxifen and its major metabolites in plasma.
J Chromatogr. 1996;678:317–323
-
.
Quantitation of toremifene and its major metabolites in human plasma by high performance liquid chromatography following fluoriscent activation.
Anal Lett. 1983;20:871–879
- . Pharmacokinetic analysis of high-dose toremifene in combination with doxorubicin. Cancer Chemother Pharmacol. 1998;42:363–366
- . High-performance liquid chromatographic method for the determination of toremifene and its major human metabolites. J Chromatogr. 1991;565:482–487
- . The metabolism of tamoxifen in humans. Biochem Pharmacol. 1979;27:145–147
- . Studies on the metabolism and pharmacokinetics of tamoxifen in normal volunteers. Cancer Treat Rep. 1980;64:761–764
- . Measurement of tamoxifen in serum by thin-layer densitometry. J Endocrinol. 1980;84:35–42
- . Identification and biological activity of tamoxifen metabolites in human serum. Biochem Pharmacol. 1983;32:2045–2052
- . Rapid drug metabolite profiling using fast liquid chromatography, automated multiple-stage mass spectrometry and receptor-binding. J Chromatogr A. 1999;831:227–241
-
.
Determination of tamoxifen and metabolites in serum by capillary electrophoresis using a nonaqueous buffer system.
J Chromatogr. 1997;695:181–185
- . Liquid chromatography-thermospray mass spectrometry of toremifene and its derivatives. J Chromatogr A. 1996;724:358–363
- . Analysis of tamoxifen and its metabolites by on-line capillary electrophoresis-electrospray ionization mass spectrometry employing nonaquous media containing surfactants. Anal Chem. 1996;68:668–674
- . First-time-in-human dose selection: allometric thoughts and perspectives. J Clin Pharmacol. 1995;35:957–966
- . Metabolites, pharmacodynamics, and pharmacokinetics of tamoxifen in rats and mice compared to the breast cancer patient. Drug Metab Dispos. 1991;19:36–43
- . Decreased serum concentrations of tamoxifen and its metabolites induced by aminoglutethimide. Cancer Res. 1990;50:5851–5857
- . Distribution of 4-hydroxy-N-desmethyltamoxifen and other tamoxifen metabolites in human biological fluids during tamoxifen treatment. Cancer Res. 1989;49:2175–2183
-
.
UDP-glucuronosyltransferases.
Pharmacol Therap. 1989;43:261–289
- . The metabolism of tamoxifen. (I.C.I. 46,474) Part II: in female patients. Xenobiotica. 1973;3:711–714
- . The metabolism of tamoxifen. (I.C.I. 46,474) Part I: in laboratory animals. Xenobiotica. 1973;3:693–709
-
.
Pharmacokinetics of droloxifene in mice, rats, monkeys, premenopausal and postmenopausal patients.
Eur J Drug Metab Pharm. 1994;19:47–58
-
.
The disposition and metabolism of 14C-labeled raloxifene in humans.
Pharm Res. 1995;12(suppl):S–372
-
.
Pharmacokinetics of raloxifene in men and postmenopausal women volunteers.
Pharmacol Res. 1996;13(Suppl):430
- . Pharmacokinetics of toremifene. J Steroid Biochem. 1990;36:249–252
- . Metabolism of tamoxifen by isolated rat hepatocytes. Identification of the glucuronide of 4-hydroxytamoxifen. Biochem Pharmacol. 1990;39:1459–1465
- . Metabolism of the 4-iodo derivative of tamoxifen by isolated rat hepatocytes. Demonstration that the iodine atom reduces metabolic conversion and identification of four metabolites. Biochem Pharmacol. 1990;40:2277–2283
- . Clinical pharmacology of tamoxifen in patients with breast cancer: comparison of traditional and loading dose schedules. Cancer Treat Rep. 1980;64:765–773
-
.
Pharmacokinetics of droloxifene and its metabolites in breast cancer patients.
Am J Clin Oncol. 1991;14 (Suppl 2):21–29
-
.
Preliminary data on phase-I trial of the new antiestrogen droloxifene: tolerance, pharmacokinetics and metabolism.
Contr Oncol. 1986;23:73–78
- . Metabolism of toremifene in the rat. J Steroid Biochem. 1990;36:211–215
- . Review of the pharmacological properties of toremifene. J Steroid Biochem. 1990;36:191–195
-
Data on file, Lilly Research Laboratories, Eli Lilly and Company Limited.
- . A comparison of two doses of tamoxifen (Nolvadex) in postmenopausal woman with advanced breast cancer: 10 mg bd versus 20 mg bd. Br J Cancer. 1984;50:199–205
- . Age-related difference in tamoxifen disposition. Clin Pharmacol Ther. 1996;59:401–410
-
.
A phase I study of toremifene.
Breast Cancer Res Treat. 1990;16S:27–29
- . Pharmacokinetics of toremifene and its metabolites in patients with advanced breast cancer. Cancer Chemother Pharmacol. 1990;25:247–251
- . Toremifene. A review of its pharmacological properties and clinical efficacy in the management of advanced breast cancer. Drugs. 1997;54:141–160
- . Phase I clinical and pharmacokinetics study of high-dose toremifene in postmenopausal patients with advanced breast cancer. Cancer Chemother Pharmacol. 1992;30:174–178
-
.
Preclinical studies with toremifene as an antitumor agent.
Breast Cancer Res Treat. 1990;16:S9–S17
- . High-dose tamoxifen as an enhancer of etoposide cytotoxicity. Clinical effects and in vitro assessment in p-glycoprotein expressing cell lines. Br J Cancer. 1992;66:833–839
- . Intrapertioneal and intraportal administration of droloxifen to the sprague-dawley rat: assessing the first-pass effect. Xenobiotica. 1997;27:627–632
-
.
Serum concentrations of tamoxifen and major metabolite during long term nolvadex therapy, correlated with clinical response.
In:
Mouridsen HT, Palshof T editor. Breast Cancer-Experimental and Clinical Aspects.. Oxford: Pergamon Press; 1980;p. 89–92
- . Metabolite pharmacokinetics: Methods for simultaneous estimates of elimination rate constants of a drug and its metabolite. Drug Metab Dispos. 1980;8:39–43
-
.
A review of metabolite kinetics.
J Pharmacokin Biopharm. 1985;13:633–662
- . Distribution of tamoxifen and its metabolites in rat and human tissues during steady-state treatment. Cancer Res. 1991;51:4837–4844
- . New pharmacokinetic methods III. Two simple tests for “deep pool effect”. J Clin Pharmacol. 1990;30:680–685
-
.
Phase I study of the tolerance and pharmacokinetics of toremifene in patients with cancer.
Breast Cancer Res Treat. 1990;16:S19–S26
- . Raloxifene. Drugs Aging. 1998;12:335–341
-
.
Raloxifene pharmacokinetics and the associated endocrine effects in premenopausal women treated during the follicular, ovulatory, and luteal phases of the menstrual cycle [abstract].
Pharmacol Res. 1996;13(Suppl).:430
-
Haynes, B. P. Grimshaw, R. M. Griggs, L. J. Hardcastle, I. Nutley, B. P. Jarman, M. Johnston, S. R. D. Twelves, C. J. Soukop, M. Rea, D. W. Howel, A. Jones, A. Coombes, R. C. Pharmacokinetics of idoxifene and tamoxifen in a randomised phase II trial in breast cancer patients who have relapsed on tamoxifen. 10th NCI-EORTC symposium on new drugs in cancer therapy, June 16–19, Amsterdam 1998
- . High-affinity anti-oestrogen binding site distinct from the oestrogen receptor. Nature. 1980;288:273–275
- . The antioxydant action of tamoxifen and its metabolites. Inhibition of lipid peroxidation. FEBS Lett. 1990;263:192–194
-
.
An updated pKa listing of medicinal compounds.
Drug Intell Clin Pharmacy. 1986;20:683–686
- . Human albumin binding of tamoxifen in the presence of a perfluorochemical erythrocyte substitute. J Pharm Pharmacol. 1991;43:790–793
-
.
Toremifene – panel discussion and summary.
Breast Cancer Res Treat. 1990;16:S47–S54
- . Drug binding to human alpha-1-acid glycoprotein in health and desease. Pharmacol Rev. 1988;40:1–47
- . Reversal of acquired resistance to adriamycin in CHO cells by tamoxifen and 4-hydroxy tamoxifen: role of drug interaction with alpha 1 acid glycoprotein. Br J Cancer. 1990;62:712–717
- . Clinical pharmacokinetics of endocrine agents used in advanced breast cancer. Clin Pharmacokinet. 1992;22:327–358
- . Distribution of tamoxifen and metabolites into brain tissue and brain metastases in breast cancer patients. Br J Cancer. 1991;63:641–645
-
.
The distribution and metabolism of 14 C-labelled tamoxifen in spayed female mice.
Rev Endocrinol Rel Cancer. 1981;9:233–239
-
.
The distribution and metabolism of14C-labelled tamoxifen in spayed female mice.
Acta Pharmacol Toxicol. 1982;50:161–168
- . Species similarities and differences in pharmacokinetics. Drug Metab Dispos. 1995;23:1008–1021
-
.
Comparative double-tracer whole-body autoradiography: uptake of11C-,18F- and3H-labeled compounds in rat tumors.
Nucl Med Biol. 1988;15:577–585
- . Pharmacokinetics and biodistribution of radiolabelled idoxifene: prospects for the use of PET in the evaluation of a novel antioestrogen for cancer therapy. Nucl Med Biol. 1995;22:405–411
- . Facile geometric isomerization of phenolic non-steroidal estrogens and antiestrogens: limitations to the interpretation of experiments characterizing the activity of individual isomers. J Steroid Biochem. 1985;22:589–596
- . Tamoxifen antiestrogens. A comparison of the activity, pharmacokinetics, and metabolic activation of the cis and trans isomers of tamoxifen. J Steroid Biochem. 1982;16:1–13
- . Determination and pharmacology of a new hydroxylated metabolite of tamoxifen observed in patient sera during therapy for advanced breast cancer. Cancer Res. 1983;43:1446–1450
- . Biochemical and pharmacological effects of toremifene metabolites. Cancer Chemother Pharmacol. 1990;27:8–12
- . The role of human cytochrome P450 enzymes in the metabolism of anticancer agents: implications for drug interactions. Br J Clin Pharmacol. 1995;40:523–530
- . Variable contribution of cytochromes P450 2D6, 2C9 and 3A4 to the 4-hydroxylation of tamoxifen by human liver microsomes. Biochem Pharmacol. 1997;53:171–178
- . CYP2D6 catalyzes tamoxifen 4-hydroxylation in human liver. Cancer Res. 1997;57:3402–3406
- . The metabolism of tamoxifen by human cytochromes P450 is rationalized by molecular modelling of the enzyme-substrate interactions: potential importance to its proposed anti-carcinogenic/carcinogenic actions. Carcinogenesis. 1996;17:1357–1360
- . Polymorphic drug metabolism. Clin Pharm. 1989;8:852–863
- . Expression of cytochromes P450 in human breast tissue and tumors. Drug Metab Dispos. 1996;24:899–905
- . Tamoxifen and toremifene concentrations in plasma are greatly decreased by rifampin. Clin Pharmacol Ther. 1998;64:648–654
-
.
Pharmacology and toxicology of the antiestrogen droloxifene.
Contributions to Oncology. 1986;23:64–72
- . Pharmacological activities of droloxifene isomers. Anticancer Res. 1988;8:1271–1274
- . Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent. J Med Chem. 1989;32:2527–2533
-
.
Pharmacokinetics of idoxifene and identification of metabolites in patients during a loading dose study.
Proc Amer Assoc Cancer Res. 1996;37:117
- . Evaluation of the major metabolites of raloxifene as modulators of tissue selectivity. J Steroid Biochem Mol Biol. 1997;61:97–106
- . Metabolism of droloxifene in the CD-1 mouse, Fischer-344 rat and cynomolgus monkey. Xenobiotica. 1998;28:153–166
- . Function of the normal human microflora. Scand J Infect Dis Suppl. 1986;49:17–30
- . Metabolism of foreign compounds by gastrointestinal microorganisms. Pharmacol Rev. 1973;25:451–523
-
.
Pharmacokinetics of tamoxifen in pre-and post-menopausal women with breast cancer.
J Ster Mol Biol. 1995;55:229–231
- . Influence of age on toremifene pharmacokinetics. Cancer Chemother Pharmacol. 1997;40:185–188
- . Effect of impaired renal function on tamoxifen. J Surg Oncol. 1984;27:222–223
- . Elevated plasma tamoxifen levels in a patient with liver obstruction. Cancer Chemother Pharmacol. 1989;23:194–195
- . Effect of tamoxifen treatment on liver, lung and intestinal mixed-function oxydases in male and female rats. Drug Metab Dispos. 1981;9:327–330
- . Hydroxylated metabolites of tamoxifen are formed in vivo and bound to estrogen receptor in target tissues. J Biol Chem. 1981;256:859–868
-
.
Tamoxifen pharmacokinetics in advanced breast cancer patients.
In:
Pannuti F editors. Anti-oestrogens in oncology. Past, Present and Prospects.. Amsterdam: Excerpta Medica; 1985;p. 90–97
- . Influence of tamoxifen and its N-desmethyl and 4-hydroxy metabolites on rat liver microsomal enzymes. Biochem Pharmacol. 1984;33:115–123
- . Some chemical and biochemical aspects of liver microsomal metabolism of tamoxifen. Drug Metab Dispos. 1984;12:478–483
-
.
Life threatening interactions between tamoxifen and warfarin.
Br Med J. 1987;295:1141
-
.
Tamoxifen-warfarin interaction: the Aberdeen hospitals drug file.
Br Med J. 1989;298:1253
-
.
Life threatening interaction between tamoxifen and warfarin.
Br Med J. 1989;298:93
- . Interaction between tamoxifen and digitoxin?. Klin Wochenschr. 1986;64:1211
- . Identification of the cytochrome P450 IIIA family as the enzymes involved in the N-demethylation of tamoxifen in human liver microsomes. Biochem Pharmacol. 1991;41:1911–1919
-
.
Involvement of cytochrome P450 3A enzyme family in the major metabolic pathways of toremifene in human liver microsomes.
Biochem Pharm. 1994;47:1883–1895
-
.
Species differences in the covalent binding of (14C)tamoxifen to liver microsomes and the forms of cytochrome P450 involved.
Biochem Pharm. 1995;49:1035–1042
- . The aromatase inactivator 4-hydroxyandrostenedione (4-OH-A) inhibits tamoxifen metabolism by rat hepatic cytochrome P-450 3A: potential for drug-drug interaction of tamoxifen and 4-OH-A in combined anti-breast cancer therapy. Drug Metab Dispos. 1999;27:389–394
- . Inhibitory effect of combined treatment with the aromatase inhibitor exemestane and tamoxifen on DMBA-Induced mammary tumors in rats. J Steroid Biochem Mol Biol. 1993;44:677–680
- . The effect of combining aromatase inhibitors antioestrogens on tumour growth in a nude mice model for breast cancer. Breast Cancer Res Treat. 1999;57:183–192
- . Influence of aminoglutethimide on the metabolism of medroxyprogesterone acetate and megestrol acetate in post-menopausal patients with advanced breast cancer. Cancer Chemother Pharmacol. 1990;27:101–105
- . Influence of aminoglutethimide on plasma levels of medroxyprogesterone acetate: its correlation with serum cortisol. Cancer Treat Rep. 1985;69:85–90
- . Induction of cytochrome P450 2B1 in rat liver by the aromatase inhibitor aminoglutethimide. J Pharmacol Exp Ther. 1993;265:477–481
- . Aminoglutethimide enzyme induction: pharmacologial and endocrinological implications. Cancer Chemother Pharmacol. 1990;26:241–244
- . Induction of Cytochrome-P450 2B1 in rat liver by the aromatase inhibitor aminoglutethimide. J Pharmacol Exp Ther. 1993;265:477–481
- . Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab Dispos. 1997;25:598–602
-
.
Lack of effect of anastrozole, an aromatase inhibitor, on antipyrine pharmacokinetics in postmenopausal women.
Clin Pharmacol Therap. 1997;61:172
- . The effect of anastrozole on the pharmacokinetics of tamoxifen in post-menopausal women with early breast cancer. Br J Cancer. 1999;79:311–315
- . Evaluation of tamoxifen plus letrozole with assessment of pharmacokinetic interaction in postmenopausal women with metastatic breast cancer. Clin Cancer Res. 1999;5:1642–1649
- . Impact of tamoxifen on the pharmacokinetics and endocrine effects of the aromataseinhibitor letrozole in postmenopausal women with breast cancer. Clin Cancer Res. 1999;5:2338–2343
- . Medroxyprogesterone acetate (MAP) and tamoxifen (TMX) plasma levels after simultaneous treatment with ‘low’ TMX and ‘high’ MAP doses. Cancer Chemother Pharmacol. 1985;14:229–331
-
.
Raloxifene HCI, a new endocrine agent, is active in estrogen receptor positive (ER+) metastatic breast cancer.
Breast Cancer Res Treat. 1997;46:53
- . Effects of postmenopausal estrogen replacement on the concentrations and metabolism of plasma lipoproteins. N Engl J Med. 1991;325:1196–1204
- . Effects of estrogen or estrogen/progestin regimens on heart disease risk factors in postmenopausal women. The postmenopausal estrogen/progestin interventions (PEPI) trial. JAMA. 1995;273:199–208
- . Dose-response effects on serum lipids and lipoproteins following combined oestrogen-progestogen therapy in post-menopausal women. Maturitas. 1987;9:259–266
-
.
Hormonal and metabolic effects of transdermal estradiol/progestagen administration in postmenopausal women.
Int J Fertil. 1994;39:202–207
- . Effects of percutaneous estradiol and conjugated estrogens on the level of plasma proteins and triglycerides in postmenopausal women. Am J Obstet Gynecol. 1982;143:888–892
-
.
A comparison of liver protein induction in postmenopausal women during oral and percutaneous oestrogen replacement therapy.
Br J Obstet Gynecol. 1983;90:355–360
-
.
Effects of oral and transdermal oestrogen replacement therapy on plasma levels of insulin-like growth factors and IGF binding proteins 1 and 3: a cross-over study.
Clin Endocrinol. 1996;45:727–732
- . Lipoprotein(a) serum levels in post-menopausal women treated with oral estrogens administered at different times. Horm Metab Res. 1994;26:379–382
-
.
Lipoprotein(a) and postmenopausal oestrogen.
Acta Endocrinol. 1993;129:225–228
- . Postmenopausal cyclic estrogen-progestin therapy lowers lipoprotein (a). J Lab Clin Med. 1994;123:837–841
-
.
Effects of tamoxifen on cardiovascular risk factors in postmenopausal women after 5 years of treatment.
J Nat Cancer Inst. 1994;86:1534–1539
- . The effect of tamoxifen and hormone replacement therapy on serum cholesterol, bone mineral density and coagulation factors in healthy postmenopausal women participating in a randomised, controlled tamoxifen prevention study. Ann Oncol. 1996;7:671–675
- . Tamoxifen, toremifen lower serum cholesterol by inhibition ao delta8-cholesterol conversion to lathosterol in women with breast cancer. J Clin Oncol. 1995;13:2900–2905
- . Antiatherogenic effects of adjuvant antiestrogens: a randomized trial comparing the effects of tamoxifen and toremifene on plasma lipid levels in postmenopausal women with node-positive breast cancer. J Clin Oncol. 1996;14:429–433
- . Severe lipemia induced by tamoxifen. Cancer. 1986;57:2123–2126
- . Effect of tamoxifen on serum lipid metabolism. J Clin Endocrinol Metab. 1998;83:1633–1635
- . Tamoxifen-induced fatty liver in patients with breast cancer [letter]. Lancet. 1998;351:725
- . Hormone replacement therapy may reduce high serum homocysteine in postmenopausal women. Eur J Clin Invest. 1994;24:733–736
- . A randomized controlled study of the effects of 17beta-estradiol-dydrogesterone on plasma homocysteine in postmenopausal women. Obstet Gynecol. 1998;91:432–436
- . Homocysteine and cardiovascular disease. Annu Rev Med. 1998;49:31–62
- . Calcium antagonism by the antiestrogen tamoxifen. Cancer Chemother Pharmacol. 1986;18:17–20
- . Cardiac and vascular morbidity in women receiving adjuvant tamoxifen for breast cancer in a randomised trial. BMJ. 1995;311:977–980
-
.
Coronary heart disease mortality and adjuvant tamoxifen therapy.
J Nat Cancer Inst. 1997;89:776–782
- . Cardiac and thromboembolic morbidity among postmenopausal women with early-stage breast cancer in a randomized trial of adjuvant tamoxifen. J Natl Cancer Inst. 1993;85:1398–1406
- . Endocrine consequences of continuous antiestrogen therapy with tamoxifen in premenopausal women. J Clin Invest. 1979;64:398–404
- . Clodronate improves bone mineral density in postmenopausal breast cancer patients treated with adjuvant antioestrogens. Br J Cancer. 1997;75:602–605
- . A controlled trial of raloxifene (LY 139481) HCl: impact on bone turnover and serum lipid profile in healthy postmenopausal women. J Bone Miner Res. 1996;11:835–842
- . Hormone therapy to prevent disease and prolong life in postmenopausal women. Ann Intern Med. 1992;117:1016–1037
- . Effects of tamoxifen on uterus and ovaries of postmenopausal women in a randomised breast cancer prevention trial. Lancet. 1994;343:1318–1321
-
.
Time-dependent effect of tamoxifen therapy on endometrial pathology in asymptomatic postmenopausal breast cancer patients.
Int J Gyn Pathol. 1996;15:152–157
- . Comparison between the effects of tamoxifen and toremifene on the uterus in postmenopausal breast cancer patients. Gynecol Oncol. 1995;59:261–266
- . Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998;339:1609–1618
- . Ovarian cysts in premenopausal and postmenopausal tamoxifen-treated women with breast cancer. Am J Obstet Gynecol. 1996;174:141–144
- . Tamoxifen treatment in premenopausal breast cancer patients may be associated with ovarian overstimulation, cystic formations and fibroid overgrowth. Br J Cancer. 1994;69:620–621
-
.
Endometrial cancer in Tamoxifen-Treated breast cancer patients – findings from the national surgical adjuvant breast and bowel project (NSABP) b-14.
J Nat Cancer Inst. 1994;86:527–537
- . Adjuvant tamoxifen therapy for early stage breast cancer and second primary malignancies. Stockholm breast cancer study group. J Natl Cancer Inst. 1995;87:645–651
- . Five versus more than five years of tamoxifen therapy for breast cancer patients with negative lymph nodes and estrogen receptor-positive tumors. J Natl Cancer Inst. 1996;88:1529–1542
- . Endometrial carcinoma and tamoxifen: clearing up a controversy. Clin Cancer Res. 1995;1:467–472
- . Adjuvant tamoxifen in early breast cancer: occurence of new primary cancers. Lancet. 1989;1:117–120
- . The triphenylethylene drug tamoxifen is a strong liver carcinogen in the rat. Carcinogenesis. 1993;14:315–317
- . Major difference in the hepatocarcinogenicity and DNA adduct forming ability between toremifene and tamoxifen in female Crl-CD(BR) rats. Cancer Res. 1993;53:4534–4541
- . Tamoxifen-induced DNA adducts in endometrial samples from breast cancer patients. Cancer Res. 1996;56:4374–4377
- . High-grade endometrial carcinoma in tamoxifen-treated breast cancer patients. J Clin Oncol. 1993;11:485–490
- . Tamoxifen and endometrial cancer: most cancers are early stage and highly curable. Eur J Cancer. 1998;34:S49–S50
- . Adverse events reported by postmenopausal women in controlled trials with raloxifene. Obstet Gynecol. 1999;93:558–565
-
.
Vaginal complaints in healthy postmenopausal women: data from a 3-year trial comparing raloxifene with conjugated estrogens or placebo.
Program of the North American Menopause Society, Toronto, CA,. 1998;
- . Reproductive endocrine and endometrial effects of raloxifene hydrochloride, a selective estrogen receptor modulator, in women with regular menstrual cycles. J Clin Endocrinol Metab. 1998;83:6–13
-
Novo, Nordisk. Bagsvaerd, D. Novo Nordisk levormeloxifene phase 2 clinical trial: Novo Nordisk presents phase 2 data on levormeloxifen to clinical investigators [press release]. PRNewswire 1998 June 19.
-
.
Endocrine treatment of breast cancer in women.
Endocrine Rev. 1990;11:221–265
- . Anastrozole versus megestrol acetate in the treatment of postmenopausal women with advanced breast carcinoma: Results of a survival update based on a combined analysis of data from two mature phase III trials. Cancer. 1998;83:1142–1152
- . Letrozole, a new oral aromatase inhibitor for advanced breast cancer: Double-blind randomized trial showing a dose effect and improved efficacy and tolerability compared with megestrol acetate. J Clin Oncol. 1998;16:453–461
-
.
Survival advantage of exemestane (AromasinR) over megestrol acetate (MA) in postmenopausal women with advanced breast cancer (ABC) refractory to tamoxifen (TAM): results of a phase III randomized double-blind study.
Proc Am Soc Clin Oncol. 1999;18:412
- . Duration of remission to ICI 182,780 compared to megestrol acetate in tamoxifen resistant breast cancer. Breast. 1997;6:186–189
- . Comparison of toremifene and tamoxifen in post-menopausal patients with advanced breast cancer: a randomized double-blind, the ‘nordic’ phase III study. Br J Cancer. 1997;76:270–277
- . Randomized comparison of tamoxifen and two separate doses of toremifene in postmenopausal patients with metastatic breast cancer. J Clin Oncol. 1995;13:2556–2566
- . Droloxifene, a new anti-oestrogen in postmenopausal advanced breast cancer – preliminary results of a double-blind dose-finding phase-II trial. Eur J Cancer. 1992;28A:1404–1407
- . Influence of droloxifene on metastatic breast cancer as first-line endocrine treatment. Acta Oncol. 1998;37:365–368
- . Droloxifene – a new anti-estrogen. Acta Oncol. 1992;31:425–428
- . Phase II evaluation of Ly 156756 in metastatic breast cancer. Oncology. 1988;45:344–345
- . Controlled trial of tamoxifen as single adjuvant agent in management of early breast cancer. Lancet. 1985;1:836–840
- . Prevention of breast cancer with tamoxifen-an update on the Royal Marsden Hospital pilot programme. Eur J Cancer. 1990;26:680–684
- . Tamoxifen in treatment of intraductal breast cancer: National Surgical Adjuvant Breast and Bowel Project B-24 randomised controlled trial. Lancet. 1999;353:1993–2000
-
.
Tamoxifen for prevention of breast cancer: Report of the National Surgical Adjuvant Breast and Bowel Project P-1 study.
J Nat Cancer Inst. 1999;91:730
- . Is tamoxifen effective in prevention of breast cancer?. Lancet. 1998;352:80–81
- . Time-course of local recurrence following conservative surgery and radiotherapy for early stage breast cancer. Int J Radiat Oncol Biol Phys. 1988;15:255–261
-
.
Primary prevention international tamoxifen study to continue.
Lancet. 1998;352:1138
- . Principles of pharmacoeconomic analysis of drug therapy. PharmacoEconomics. 1992;1:20–32
- . Tamoxifen should be cost-effective in reducing breast cancer risk in high-risk women. J Clin Oncol. 2000;18:284–286
-
.
Selective estrogen receptor modulators: Clinical spectrum.
Endocrine Rev. 1999;20:418–434
- . American Society of Clinical Oncology Technology Assessment on Breast Cancer Risk Reduction Strategies: Tamoxifen and Raloxifene. J Clin Oncol. 1999;17:1939
-
.
A randomized clinical trial evaluating tamoxifen in the treatment of patients with node-negative breast cancer who have estrogen-receptor-positive tumors.
New Engl J Med. 1989;320:479–484
- . Tamoxifen: a review of its pharmacological properties and therapeutic use in the treatment of breast cancer. Drugs. 1978;16:1–24
- . Tamoxifen in advanced breast cancer. Cancer Treat Rev. 1978;5:131–141
- . Role, mechanism of action of tamoxifen in premenopausal women with metastatic breast carcinoma. Cancer Res. 1986;46:3152–3156
- . Symptoms associated with tamoxifen treatment in postmenopausal women. Arch Intern Med. 1991;151:1842–1847
- . Venous and arterial thrombosis in patients who received adjuvant therapy for breast cancer. J Clin Oncol. 1991;9:286–294
- Br J Cancer. 1988;57:608–611
- . Tamoxifen associated venous thrombosis and activated protein C resistance due to factor Leiden. Cancer. 1997;79:2024–2027
- . Raloxifene hydrochloride, a selective estrogen receptor modulator: safety assessment of effects on cognitive function and mood in postmenopausal women. Psychoneuroendocrinology. 1999;24:115–128
- . Tamoxifen retinopathy. Cancer Treat Rep. 1978;62:315–320
- . A controlled study on the ocular effects of tamoxifen in conventional dosage in the treatment of breast carcinoma. Eur J Cancer Clin Oncol. 1989;25:1805–1808
- . Tamoxifen-associated eye disease. A review. J Clin Oncol. 1996;14:1018–1026
- . Long-term tamoxifen citrate use and potential ocular toxicity. Am J Ophthalmol. 1998;125:493–501
- . Retinopathy associated with low-dose tamoxifen. Am J Ophthalmol. 1993;116:372–373
-
.
Tamoxifen retinopathy at low dosage.
Am J Ophthalmol. 1987;8:185–186
- . Teratogenic effects of clomiphene, tamoxifen, and diethylstilbestrol on the developing human female genital tract. Hum Pathol. 1987;18:1132–1143
- IARC Monogr Eval Carcinog Risks Hum. 1996;66:253–365
-
.
Occurence of genital tract abnormalities and bladder hernia in female mice exposed neonatally to tamoxifen.
Toxicol. 1986;42:1–11
-
.
Abnormal development of the os penis in male mice treated neonatally with tamoxifen.
Acta Anat. 1990;139:201–208
- . Ambiguous genitalia in infant exposed to tamoxifen in utero. Lancet. 1997;350:183
- . Is body composition an important variable in the pharmacokinetics of anticancer drugs? A review and suggestions for further research. Cancer Chemother Pharmacol. 1994;34:3–13
PII: S0305-7372(99)90162-7
doi: 10.1053/ctrv.1999.0162
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Cancer Treatment Reviews
Volume 26, Issue 3
, Pages 205-227
, June 2000
