Abstract
For the postmenopausal and/or ovariectomized woman, osteoporosis is part of an estrogen deficiency syndrome that also increases risk for coronary heart disease. Hormone replacement therapy directly addresses this syndrome from etiological and pathophysiological grounds, but has poor compliance because of potential side effects and risk/benefit ratio. We describe in this issue a non-steroidal molecule, Raloxifene, that acts as a selective estrogen receptor modulator (SERM). Thus, raloxifene is, at the same time and in the same treated subject, an estrogen receptor agonist that stops bone loss and lowers cholesterol and an estrogen receptor antagonist that represses the adverse effects of estrogen on uterine endometrium and breast tissue. This compound is therefore an excellent candidate for the prevention and treatment of postmenopausal osteoporosis and the estrogen deficiency syndrome.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Riggs BL: Overview of osteoporosis. West J Med 154: 63–77, 1991
Gordon T, Kannel WB, Hjortland MC et al.: Menopause and coronary heart disease: The Framingham Study. Ann Intern Med 89: 157–161, 1978
Matthews KA, Meilahn E, Kuller LH et al.: Menopause and risk factors for coronary heart disease: N Eng J Med 321: 641–646, 1989
Lindsay R: The effect of estrogens in the prevention and treatment of osteoporosis. In: Munro H (ed.) Nutrition in the elderly, Nestle Nutrition Workshop Series, New York: Raven, 29: 161–167, 1992
Stampfer MJ, Colditz GA, Willet WC et al.: Postmenopausal estrogen therapy and cardiovascular disease: Ten year follow-up from the nurses' health study. N Engl J Med 325: 756–762, 1991
Veseyy MP: Exogenous hormones in the aetiology of cancer in women. J Roy Soc Med 77: 542–549, 1984
Dupont WD, Page DL: Menopausal estrogen replacement therapy and breast cancer. Arch Intern Med 151: 67–72, 1991
Love RR, Cameron L, Connell BL et al.: Symptoms associated with tamoxifen treatment in postmenopausal women. Arch Intern Med 151: 1842–1847, 1991
Black LJ, Jones CD, Falcone F: antagonism of estrogen with a new benzothiaphene derived antiestrogen. Life Sci 32: 1031–1036, 1983
Clemens JA, Bennett DR, Black LJ et al.: Effects of new antiestrogen, keoxyfene LY156758, on growth of carcinogen-induced mammary tumors and on leutinizing hormone and prolactin levels. Life Sci 32: 2869–2876, 1983
Gottardis MM, Jordan VC: Antitumor actions of keoxyfene and tamoxifen in the N-nitrosomethylurea induced rat mammary carcinoma model. Cancer Res 47: 4020–4024, 1987
Osborne CK, Hubbs K, Clark GM: Effects of estrogens and antiestrogens on growth of human breast cancer cells in athymic nude mice. Cancer Res 45: 584–590, 1985
Black LJ, Sato M, Rowley ER et al.: Raloxifene (LY139481 HCl) prevents bone loss and reduces serum cholesterol without causing uterine hyptrophy in ovariectomized rats. J Clin Invest 93: 63–69, 1994
Draper MW, Flowers DE, Huster WJ et al.: Effects of raloxifene (LY139481 HCl) on biochemical markers of bone and lipid metabolism in healthy postmenopausal women. In: Christiansen C, Riis B (eds.) Proceedings 4th international symposium on osteoporosis and consensus development conference. Aalborg: Handelstrykkerict Aalborg APS, pp. 119–121, 1993
Glasebrook AL, Phillips DL, Sluka JP: Multiple binding sites for the antiestrogen raloxifene. J Bone Miner Res 8 (Suppl 1): S268, 1993
Yang NN, Hardikar S, Kim J et al.: Raloxifene, an anti-estrogen, stimulates the effects of estrogen on inhibiting bone resorption through regulating TGF β-3 expression in bone. J Bone Miner Res 8 (Suppl 1): S118, 1993
Author information
Authors and Affiliations
About this article
Cite this article
Termine, J.D. Therapy for postmenopausal osteoporosis based on fundamental disease etiology and pathophysiology. J Bone Miner Metab 12 (Suppl 2), S25–S28 (1994). https://doi.org/10.1007/BF02383391
Issue Date:
DOI: https://doi.org/10.1007/BF02383391