Pharmacokinetics of raloxifene and its clinical application

European Journal of Obstetrics and Gynecology and Reproductive Biology

Volumn 85, Issue 1, 1999, Pages 23-29

  Hochner Celnikier, Drorith ^a  

^a HADASSAH HEBREW UNIVERSITY MEDICAL CENTER   (Israel)

Author keywords

Coronary heart disease; HRT; Osteoporosis; Raloxifene; SERMs

Indexed keywords

ESTROGEN RECEPTOR; RALOXIFENE;

ADULT; AGED; BREAST CANCER; CARDIOVASCULAR DISEASE; COGNITION; CONFERENCE PAPER; DRUG CLEARANCE; DRUG DESIGN; DRUG RECEPTOR BINDING; ESTROGEN ACTIVITY; FEMALE; HORMONE SUBSTITUTION; HUMAN; HUMAN TISSUE; LIPID METABOLISM; ORAL DRUG ADMINISTRATION; OSTEOPOROSIS; POSTMENOPAUSE; PRIORITY JOURNAL; RISK FACTOR;

EID: 0033062743     PISSN: 03012115     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0301-2115(98)00278-4     Document Type: Conference Paper

References (59)

1. Kannel W.B., Hjortland M.C., McNamara P.M., Gordon T. Menopause and the risk of cardiovascular disease: the Framingham study. Ann Intern Med. 85:1976;447-482.
2. Parrish H.M., Carr L.A., Hall D.G.et al. Time interval from castration in premenopausal women to development of excessive coronary atherosclerosis. Am J Obstet Gynecol. 99:1967;155-162.
3. Aitken J.M., Hart D.M., Anderson J.B.et al. Osteoperosis after oophorectomy for non-malignant disease in premenopausal women. Br Med J. 2:1973;325-328.
4. Richeson L.S., Wahner H.W., Melton L.J. (I)et al. Relative contributions of aging and estrogen deficiency to postmenopausal bone loss. New Eng J Med. 311:1984;1273-1275.
5. American College of Physicians. Guidelines for counseling postmenopausal women about preventive hormone therapy. Ann Intern Med 1992;12:1038-41.
6. Lomax L., Schonbaum E. Postmenopausal hot flushes and their management. Pharmacol Ther. 57:1993;347-358.
7. Grady D., Rubin S.M., Petitti D.B.et al. Hormone therapy to prevent disease and prolong life in postmenopausal women. Ann Intern Med. 117:1992;1016-1037.
8. Lindsay R. Hormone replacement therapy for prevention and treatment of osteoporosis (abstract). Am J Med. 95(Suppl 5A):1993;37-39.
9. Wolf P.H., Madans J.H., Finucane F.F., Higgins M., Kleinman J.C. Reduction of cardiovascular disease-related mortality among postmenopausal women who use hormones: evidence from a national cohort. Am J Obstet Gynecol. 164:1991;489-494.
10. Harris S.T., Genant H.K., Baylink D.J.et al. The effects of estrone (Ogen) on spinal bone density of postmenopausal women. Arch Intern Med. 151:1991;1980-1984.
11. Stampfer M.J., Colditz G.A., Willett W.C.et al. Postmenopausal estrogen therapy and cardiovascular disease. New Eng J Med. 325:1991;756-762.
12. Lobo R.A. Effects of hormonal replacement on lipids and lipoproteins in postmenopausal women. J Clin Endocrinol Metab. 73:1991;925-930.
13. Barrett-Connor E., Bush T.L. Estrogen and coronary heart disease in women. J Am Med Assoc. 265:1991;1861-1867.
14. Tang M.X., Jacobs D., Stern Y.et al. Effect of oestrogen during me nopause on risk and age of onset of Alzheimer's disease. Lancet. 348:1996;429-432.
15. Kawas C., Resnick S., Morrison A.et al. A prospective study of estrogen replacement therapy and the risk of developing Alzheimer's disease: the Baltimore longitudinal study of aging. Neurology. 48:1997;1517-1521.
16. Paganini-Hill A., Henderson V.W. Estrogen deficiency and risk of Alzheimer's disease in women. Am J Epidemiol. 140:1994;256-261.
17. Resnick S.M., Metter E.J., Zonderman A.B. Estrogen replacement therapy and longitudinal decline in visual memory. Neurology. 49:1997;1491-1497.
18. Felson D.T., Zhang Y., Hannan M.T., Kiel D.P., Wilson P.W.F., Andersen J.J. The effect of postmenopausal estrogen therapy on bone density in elderly women. New Eng Med J. 329:1993;1141-1146.
19. Hammond C.B. Women's concerns with hormone replacement therapy - compliance issues. Fertil Steril. 62:1994;1575-1605.
20. Ravnikar V.A. Compliance with hormone replacement therapy: Are women receiving the full impact of hormone replacement therapy preventative health benefits? Women's Health Issues. 2:1992;75-82.
21. Golditz G.A., Hankinson S.E., Hunter D.J.et al. The use of estrogens and progestins and the risk of breast cancer in postmenopausal women. New Eng J Med. 332:1995;1589-1593.
22. Collaborative Group on Hormonal Factors in Breast Cancer. Breast cancer and hormone replacement therapy: collaborative reanalysis of data from 51 epidemiological studies of 52 705 women with breast cancer and 108 411 women without breast cancer. Lancet 1997;350:1047-59.
23. Yang N.N., Venugopalan M., Hardikar S., Glasebrook A. Identification of an estrogen response activated by metabolites of 17β-estradiol and raloxifene. Science. 273:1996;1222-1225.
24. Jordan V.C. Tamoxifen: the herald of a new era of therapeutics. J Natl Concer Inst. 89:1997;747-749.
25. Breast cancer prevention trial shows major benefit, some risk [press release]. Bethesda, MD: National Cancer Institute April 6, 1998.
26. Jordan V.C. Tamoxifen and endometrial cancer. Lancet. 2:1989;117-120.
27. Fornander T., Cedermark B., Mattsson A.et al. Adjuvant tamoxifen in early breast concer: Occurrence of new primary cancers. Lancet. i:1989;117-120.
28. Delmas P.D., Bjarnason N.H., Mitlak B.H.et al. Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women. New Engl J Med. 337:1997;1641-1647.
29. Walsh B.W., Lewis H.K., Robert A.et al. Effects of raloxifene on serum lipids and coagulation factors in healthy postmenopausal women. J Am Med Assoc. 279:1998;1445-1451.
30. Jordan V.C., Glusman J.E., Eckert S.et al. Incident primary breast cancers are reduced by raloxifene: integrated data from multicenter, double-blind, randomized trials in ~12 000 women. Abstract. ASCO. 17:1998;466.
31. Cummings S.R., Norton L., Eckert S.et al. Raloxifene reduces the risk of breast cancer and may decrease the risk of endometrial cancer in postmenopausal women. Two year findings from the multiple outcomes of raloxifene evaluation (more) trial. Abstract. ASCO. 17:1998;3.
32. Glasebrook A.L., Phillips D.L., Sluka J.P. Multiple binding sites for the anti-estrogen raloxifene (abstract). J Bone Miner Res. 8(Suppl I):1993;S268.
33. Brown M.S., Goldstein J.L. The estradiol-stimulated lipoprotein receptor of rat liver. J Biol Chem. 255:1980;10464-10471.
34. Szego C., Roberts S. Steroid action and interactions in uterine metabolism. Recent Prog Horm Res. 8:1953;419-468.
35. Kumar V., Green S., Jin J.R., Chambon R. Functional domains of the human estrogen receptor. Cell. 51:1987;941-951.
36. Webb P., Lopez G.N., Uht R.M., Kushner P.J. Tamoxifen activation of the estrogen receptor/AP-1 pathway: Potential origin for the cell specific estrogen-like effects of antiestrogens. Mol Endocrinol. 9:1995;443-456.
37. McDonnell D.P., Clemm D.L., Hermann T., Goldman M.E., Pike J.W. Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens. Mol Endocrinol. 9:1995;659-669.
38. Yang N.N., Hardikar S., Sato M.et al. Estrogen and raloxifene stimulate transforming Growth Factor β3 expression in rat bone: A potential mechanism for estrogen- or raloxifene-mediated bone maintainance. Endocrinology. 137:1996;2075-2084.
39. Data on File, Lilly Research Laboratories.
40. Riggs B.L. Overview of osteoporosis. West J Med. 154:1991;63-77.
41. Hosking D.J., McClung M.R., Ravn P.et al. Alendronate in the prevention of osteoporosis: EPIC study's two-year results (abstract). J Bone Miner Res. 11(Suppl I):1996;S133.
42. Adami S., Passeri M., Ortolani S.et al. Effects of oral alendronate and intranasal calcitonin on bone mass and biochemical markers of bone turnover in postmenopausal women with osteoporosis. Bone. 17:1995;383-390.
43. Harris S.T., Watts N.B., Jackson R.D.et al. Four year study of intermittent cyclic etidronate treatment of postmenopausal osteoporosis: three years of blinded therapy followed by one year of open therapy. Am J Med. 95:1993;557-567.
44. Grey A.B., Stapleton J.P., Evans M.C., Tatnell M.A., Ames R.W., Reid I.R. The effect of the antiestrogen tamoxifen on bone mineral density in normal late postmenopausal women. Am J Med. 99:1995;636-641.
45. Powles T.J., Hickish T., Kanis J.A., 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. 14:1996;78-84.
46. Vital Statistics of the United States, 1994. National Center for Health Statistics 1997; Vol 2, A. Washington, DC: Public Health Service.
47. Lerner D.J., Kannel W.B. Patterns in coronary heart disease - morbidity and mortality in the sexes; A 26-year follow-up of the Framingham population. Am Heart J. 111:1986;383-390.
48. Bryant H.U., Dodge J.A., Sato M., Glasebrook A.L. Comparative pharmacological profiles for a spectrum of estrogen receptor active agents in ovariectomized rats. Osteoporosis Int. 6(Suppl I):1996;233.
49. Kauffman R.F., Bensch W.R., Roudebush R.E.et al. Hypocholesterolemic activity of raloxifene (LY139481): Pharmacological characterization as a selective estrogen receptor modulator. J Pharmacol Exp Ther. 280:1997;146-153.
50. Draper M.W., Flowers D.E., Huster W.J.et al. A controlled trial of raloxifene (LY139481) HCl: Impact on bone turnover and serum lipid profile in healthy postmenopausal women. J Bone Min Res. 11:1996;835-842.
51. Bjarnason N.H., Haarbo J., Byrjalsen I., Kauffman R.F., Christiansen K. Raloxifene inhibits aortic accumulation of cholesterol in ovariectomized cholesterol-fed rabbits. Circulation. 96:1997;1964-1969.
52. Zukerman S.H., Bryan-Poole N. Inhibition of LDL oxidation and myeloperoxidase-dependent tyrosyl radical formation by the selective estrogen receptor modulator LY139481 HCl. Atherosclerosis. 126:1996;65-75.
53. Black L.J., Sato M., Rowley E.R.et al. Raloxifene (LY139481 HCl) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin Invest. 93:1994;63-69.
54. Fisher B., Constantino J.P., Redmond C.K., Fisher E.R., Wickerham D.L., Cronin W.M. Endometrial cancer in tamoxifen-treated breast cancer patients: Findings from the National Surgical Adjuvant Breast and Bowel Project. J Natl Cancer Inst. 86:1994;527-537.
55. Short L.L., Glasebrook A.L., Adrian M.D.et al. 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):1996;S482.
56. Clemens J.A., Bennett D.R., Black L.J., Jones C.D. Effects of a new antiestrogen, keoxifene (LY 156758), on growth of carcinogen-induced mammary tumors and on LH and prolactin levels. Life Sci. 32:1983;3869-3875.
57. Anzano M.A., Peer C.W., Smith J.M.et al. Chemoprevention of mammary carcinogenesis in the rat: Combined use of raloxifene and 9-cis-retinoic acid. J Natl Cancer Inst. 88:1996;23-25.
58. Wakeling A.E., Dukes M., Bowler J. A potent specific pure antiestrogen with clinical potential. Cancer Res. 51:1991;3867-3873.
59. Early breast cancer trialists' collaborative group. Systemic treatment of early breast cancer by hormonal, cytotoxic, or immune therapy. Lancet 1992;339:1-15 and 71-85.