Selective estrogen receptor modulators: An alternative to hormone replacement therapy

Proceedings of the Society for Experimental Biology and Medicine

Volumn 217, Issue 1, 1998, Pages 45-52

  Bryant, Henry U ^a   Dere, Willard H ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

RALOXIFENE; TAMOXIFEN;

BONE METABOLISM; CONFERENCE PAPER; CORONARY ARTERY DISEASE; DRUG EFFECT; ESTROGEN THERAPY; FEMALE; HUMAN; LIPID METABOLISM; OSTEOPOROSIS; POSTMENOPAUSE; REPRODUCTION;

EID: 0031973426     PISSN: 00379727     EISSN: None     Source Type: Journal    
DOI: 10.3181/00379727-217-44204     Document Type: Conference Paper

References (56)

1. Fries JF. Aging, natural death, and the compression of morbidity. New Engl J Med 303:130-135, 1980.
2. Byyny RL, Speroff L. The rectangularization of life. In: A Clinical Guide for the Care of Older Women: Primary and Preventive Care, 2nd edition. Baltimore: Williams and Wilkins, pp1-19, 1996.
3. Longcope C, Franz C, Morello C, Baker R, Johnston CC. Steroid and gonadotropin levels in women during the peri-menopausal years. Maturitas 8:189-196, 1986.
4. Sherman BM, West JH, Korenman SG. The menopausal transition: Analysis of LH, FSH, estradiol and progesterone concentrations during menstrual cycles of older women. J Clin Endocrinol Metab 42:629-636, 1976.
5. Lerner DJ, Kannel WB. Patterns in coronary heart disease-morbidity and mortality in the sexes: A 26-year follow-up of the Framingham population. Am Heart J 111:383-390, 1986.
6. Riggs BL. Overview of osteoporosis. West J Med 154:63-77, 1991.
7. Lindsay R. The burden of osteoporosis: Cost. Am J Med 98 (Suppl 2A):9S-11S, 1995.
8. Ray NF, Chan JK, Thamer M, Melton LJ. Medical expenditures for the treatment of osteoporotic fractures in the United States in 1995: Report from the National Osteoporosis Foundation. J Bone Mineral Res 12:24-35, 1997.
9. Lindsay R, Aitken JM, Anderson JB. Long-term prevention of post-menopausal osteoporosis by estrogen. Lancet 1:1038-1041, 1976.
10. Munk-Jensen N, Pors Nielsen S, Obel EB, Eriksen PB. Reversal of postmenopausal vertebral loss by oestrogen and progestogen: A double blind, placebo-controlled study. BMJ 296:1150-1152, 1988.
11. Barrett-Connor E, Bush TL. Estrogen and coronary heart disease in women. JAMA 265:1861-1867, 1991.
12. Stampfer MJ, Colditz GA. Estrogen replacement therapy and coronary disease: A quantitative assessment of the epidemiological evidence. Prev Med 20:47-63, 1991.
13. Sherwin BB. Estrogen and/or androgen replacement therapy and cognitive functioning in surgically menopausal women. Psychoneuroendocrinology 13:345-357, 1988.
14. Upton GV. The perimenopause: Physiologic correlates and clinical management. J Reprod Med 27:1-27, 1982.
15. Colditz GA, Hankinson SE, Hunter DJ, Willett WC, Manson JE, Stampfer MJ, Hennekens C, Rosner B, Speizer FE. The use of estrogens and progestins and the risk of breast cancer in postmenopausal women. N Engl J Med 332:1589-1593, 1995.
16. Barrett-Connor E. Hormone replacement and cancer. Br Med Bull 48:345-355, 1992.
17. US Congress, Office of Technology Assessment. Effectiveness and costs of osteoporosis screening and hormone replacement therapy, Volume II: Evidence on benefits, risks, and costs. Washington, DC: US Government Printing Office, August 1995.
18. Beresford SAA, Weiss NS, McKnight B. Risk of endometrial cancer in relation to use of oestrogen combined with cyclic progestagen therapy in postmenopausal women. Lancet 349:458-461, 1997.
19. Felson DT, Zhang Y, Hannan MT, Kiel DP, Wilson PWF, Andersen JJ. The effect of postmenopausal estrogen therapy on bone density in elderly women. N Engl Med J 329:1141-1146, 1993.
20. Sato M, Rippy MK, Bryant HU. Raloxifene, tamoxifen, nafoxidine, and estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. FASEB J 10:905-912, 1996.
21. Bryant HU, Glasebrook AL, Yang NN, Sato M. A pharmacological review of raloxifene. Journal of Bone and Mineral Metabolism 14:1-9, 1996.
22. Sato M, Glasebrook AL, Bryant HU. Raloxifene: A selective estrogen receptor modulator. Journal of Bone and Mineral Metabolism 12 (Suppl 2):S9-S20, 1995.
23. Mitlak BH, Cohen FJ. In search of optimal long-term female hormone replacement: The potential of selective estrogen receptor modulators. Horm Res (in press), 1997.
24. Black LJ, Sato M, Rowley ER, Magee DE, Bekele A, Williams DC, Cullinan DJ, Bendele R, Kauffman RF, Bensch WR, Frolik CA, Termine JD, Bryant HU. Raloxifene (LY139481 HCl) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin Invest 93:63-69, 1994.
25. Bryant HU, Dodge JA, Sato M, Glasebrook AL. Comparative pharmacological profiles for a spectrum of estrogen receptor active agents in ovariectomized rats. Osteoporos Int 6 (Suppl 1):233, 1996.
26. Evans G, Bryant HU, Magee D, Sato M, Turner RT. The effects of raloxifene on tibia histomoiphometry in ovariectomized rats. Endocrinology 134:2283-2288, 1993.
27. Frolik CA, Bryant HU, Black EC, Magee DE, Chandrasekhar S. Time dependent changes in biochemical bone markers and serum cholesterol in ovariectomized rats: Effects of raloxifene HCl, tamoxifen, estrogen and alendronate. Bone 18:621-627, 1996.
28. Turner CH, Sato M, Bryant HU. Raloxifene preserves bone strength and bone mass in ovariectomized rats. Endocrinology 135:2001-2005, 1994.
29. Draper MW, Flowers DE, Huster WJ, Neild JA, Harper KD, Arnaud C. A controlled trial of raloxifene (LY139481) HCl: Impact on bone turnover and serum lipid profile in healthy postmenopausal women. J Bone Mineral Res 11:835-842, 1996.
30. Powles TJ, Hickish T, Kanis JA, Tidy A, Ashley S. Effect of tamoxifen on bone mineral density measured by dual-energy x-ray absorptiometry in healthy premenopausal and postmenopausal women. J Clin Oncol 14:78-84, 1996.
31. Lobo RA. Effects of hormonal replacement on lipids and lipoproteins in postmenopausal women. J Clin Endocrinol Metab 73:925-930, 1991.
32. Brown MS, Goldstein JL. The estradiol-stimulated lipoprotein receptor of rat liver. J Biol Chem 255:10464-10471, 1980.
33. Kauffman RF, Bensch WR, Roudebush RE, Cole HW, Bean JS, Phillips DL, Monroe A, Cullinan GJ, Glasebrook AL, Bryant HU. Hypocholesterolemic activity of raloxifene (LY139481): Pharmacological characterization as a selective estrogen receptor modulator. J Pharmacol Exp Ther 280:146-153, 1997.
34. Bjarnason NH, Haarbo J, Byrjalsen I, Kauffman RF, Chrisiansen K. Raloxifene inhibits aortic accumulation of cholesterol in ovariectomized cholesterol fed rabbits. Circulation (in press), 1997.
35. Zuckerman SH, Bryan-Poole N. Inhibition of LDL oxidation and myeloperoxidase-dependent tyrosyl radical formation by the selective estrogen receptor modulator LY139481 HCl. Atherosclerosis 126:65-75, 1996.
36. Grainger DJ, Witchell CM, Metcalfe JC. Tamoxifen elevates transforming-growth factor-beta and suppresses diet-induced formation of lipid lesions in mouse aorta. Nat Med 1:1067-1073, 1995.
37. Rutqvist LE, Mattson A. Cardiac and thromboembolic morbidity among postmenopausal women with early stage breast cancer in a randomized trial of adjuvant tamoxifen. J Natl Cancer Inst 85:1398-1406, 1993.
38. Fisher B, Constantino JP, Redmond CK, Fisher ER, Wickerham DL, Cronin WM. Endometrial cancer in tamoxifen-treated breast cancer patients: Findings from the National Surgical Adjuvant Breast and Bowel Project. J Natl Cancer Inst 86:527-537, 1994.
39. Bryant HU, Wilson PK, Adrian MD, Cole HW, Phillips DL, Dodge JA, Grese TA, Sluka JP, Glasebrook AL. Selective estrogen receptor modulators: Pharmacological profile in the rat uterus. J Soc Gynecol Invest 3:152A, 1996.
40. Fuchs-Young R, Magee DE, Cole HW, Short L, Glasebrook AL, Rippy MK, Termine JD, Bryant HU. Raloxifene is a tissue specific anti-estrogen that blocks tamoxifen or estrogen-stimulated uterotrophic effects. Endocrinology 136 (Suppl):57, 1995.
41. Grese TA, Sluka JP, Bryant HU, Cole HW, Kim JR, Magee DE, Rowley ER, Sato M. Benzopyran selective estrogen receptor modulators (SERMS): Pharmacological effects and structural correlation with raloxifene. Bioorg Med Chem 6:903-908, 1996.
42. Short LL, Glasebrook AL, Adrian MD, Cole H, Shetler P, Rowley ER, Magee DE, Pell T, Zeng G, Sato M, Bryant HU. Distinct effects of selective estrogen receptor modulators on estrogen dependent and estrogen independent human breast cancer cell proliferation. J Bone Mineral Res 11 (Suppl 1):S482, 1996.
43. Clemens JA, Bennett DR, Black LJ, Jones CD. Effects of a new antiestrogen, keoxifene (LY156758), on growth of carcinogen-induced mammary tumors and on LH and prolactn levels. Life Sci 32:2869-2875, 1983.
44. Fuchs-Young R, Iversen P, Shetler P, Layman N, Hale L, Short L, Magee D, Sluka J, Glasebrook A, Bryant HU, Palkowitz A. Preclinical demonstration of specific and potent inhibition of mammary tumor growth by new selective estrogen receptor modulators. Proceedings of the American Association of Cancer Research 38:573 (1997).
45. Wakeling AE, Dukes M, Bowler J. A potent specific pure antiestrogen with clinical potential. Cancer Res 51:3867-3873, 1991.
46. Anzano MA, Peer CW, Smith JM, Mullen LT, Shrader MW, Logsdon DL, Driver CL, Bown CC, Roberts AB, Sporn MB. Chemoprevention of mammary carcinogenesis in the rat: Combined use of raloxifene and 9-cis-retinoic acid. J Natl Cancer Inst 88:23-25, 1996.
47. Early breast cancer trialists' collaborative group. Systemic treatment of early breast cancer by hormonal, cytotoxic, or immune therapy. Lancet 339:71-85, 1992.
48. Kumar V, Green S, Jin JR, Chambon R. Functional domains of the human estrogen receptor. Cell 51:941-951, 1987.
49. Glasebrook AL, Phillips DL, Sluka JP. Multiple binding sites for the anti-estrogen raloxifene. J Bone Mineral Res 8 (Suppl 1):S268, 1993.
50. Yang NN, Venugopalan M, Glasebrook AL. Identification of an estrogen response element activated by metabolites of 17β-estradiol and raloxifene. Science 273:1222-1225, 1996.
51. Webb P, Lopez GN, Uht RM, Kushner PJ. Tamoxifen activation of the estrogen receptor/AP-1 pathway: Potential origin for the cell specific estrogen-like effects of antiestrogens. Mol Endocrinol 9:443-456, 1995.
52. McDonnell DP, Clemm DL, Hermann T, Goldman ME, Pike JW. Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens. Mol Endocrinol 9:659-669, 1995.
53. Yang NN, Hardikar S, Sato M, Galvin RJS, Glasebrook AL, Bryant HU, Termine JD. Estrogen and raloxifene stimulate transforming Growth Factor-β3 expression in rat bone: A potential mechanism for estrogen- or raloxifene-mediated bone maintenance. Endocrinology 137:2075-2084, 1996.
54. Adrian MD, Cole HW, Shetler PK, Rowley ER, Magee DE, Pell T, Zeng G, Sato M, Bryant HU. Comparative pharmacology of a series of selective estrogen receptor modulators. J Bone Mineral Res 11 (Suppl 1):S447, 1996.
55. Gallagher A, Chambers TJ, Tobias JH. The estrogen antagonist ICI 182,780 reduces cancellous bone volume in female rats. Endocrinology 133:2787-2791, 1993.
56. Lundeen SG, Carver JM, McKean ML, Winneker RC. Characterization of the ovariectomized rat model for the evaluation of estrogen effects on plasma cholesterol levels. Endocrinology 138:1552-1558, 1997.