225
Views
28
CrossRef citations to date
0
Altmetric
Drug Evaluations

Ospemifene use in postmenopausal women

, MD PhD, , MD, , MD & , MD
Pages 839-849 | Published online: 25 May 2009

Bibliography

  • Lund KJ. Menopause and the menopausal transition. Med Clin North Am 2008;92(5):1253-71
  • Nelson HD. Menopause. Lancet 2008;371(9614):760-70
  • Melton LJ 3rd, Chrischilles EA, Cooper C, et al. Perspective: how many women have osteoporosis? J Bone Miner Res 1992;7:1005-10
  • Riggs BL, Melton LJ 3rd. The prevention and treatment of osteoporosis. N Engl J Med 1992;327(9):620-7
  • Riggs BL, Khosla S, Melton LJ III. Sex steroids and the construction and conservation of the adult skeleton. Endo Rev 2002;23:279-302
  • Reginster JY, Burlet N. Osteoporosis: a still increasing prevalence. Bone 2006;38:S4-9
  • Riggs BL, Khosla S, Melton LJ 3rd. A unitary model of involutional osteoporosis: estrogen deficiency causes both type I and type II osteoporosis in postmenopausal women and contributes to bone loss in aging men. J Bone Miner Res 1998;13:763-73
  • Patten RD, Karas RH. Estrogen replacement and cardiomyocyte protection. Trends Cardiovasc Med 2006;16(3):69-75
  • ESHRE Capri Workshop Group. Hormones and cardiovascular health in women. Hum Reprod Update 2006;12(5):483-97
  • Gustafsson JA. Estrogen receptor beta: a new dimension in estrogen mechanism of action. J Endocrinol 1999;163(3):379-83
  • Bord S, Horner A, Beavan S, et al. Estrogen receptors alpha and beta are differentially expressed in developing human bone. J Clin Endocrinol Metab 2001;86(5):2309-14
  • Grady D, Rubin SM, Petitti DB, et al. Hormone therapy to prevent disease and prolong life in postmenopausal women. Ann Intern Med 1992;117:1016-37
  • Chlebowski RT, Wactawski-Wende J, Ritenbaugh C, et al. Women's Health Initiative Investigators. Estrogen plus progestin and colorectal cancer in postmenopausal women. N Engl J Med 2004;350:991-1004
  • Practice Committee of American Society for Reproductive Medicine. Estrogen and progestogen therapy in postmenopausal women. Fertil Steril 2008;90(5 Suppl ):S88-102
  • Grodstein F, Manson JE, Colditz GA, et al. A prospective, observational study of postmenopausal hormone therapy and primary prevention of cardiovascular disease. Ann Intern Med 2000;133:933-41
  • Manson JE, Hsia J, Johnson KC, et al. Women's Health Initiative Investigators. Estrogen plus progestin and the risk of coronary heart disease. N Engl J Med 2003;349:523-34
  • Rossouw JE, Prentice RL, Manson JE, et al. Postmenopausal hormone therapy and risk of cardiovascular disease by age and years since menopause. JAMA 2007;297:1465-77
  • Vassilopoulou-Sellin R. Breast cancer and hormonal replacement therapy. Ann NY Acad Sci 2003;997:341-50
  • HRT: What are women (and their doctors) to do? [editorial]. Lancet 2004;364:2069-70
  • Barlow DH. The medical management of menopause: to treat or not to treat? Ann NY Acad Sci 2008;1127:134-9
  • Jenkins MR, Sikon AL. Update on nonhormonal approaches to menopausal management. Cleve Clin J Med 2008;75(Suppl 4):S17-24
  • Sambrook P, Cooper C. Osteoporosis. Lancet 2006;367:2010-8
  • Rabenda V, Mertens R, Fabri V, et al. Adherence to bisphosphonates therapy and hip fracture risk in osteoporotic women. Osteoporos Int 2008;19:811-8
  • Cho CH, Nuttall ME. Therapeutic potential of oestrogen receptor ligands in development for osteoporosis. Emerg Drugs 2001;6:137-54
  • Nilsson S, Koehler KF. Oestrogen receptors and selective oestrogen receptor modulators: molecular and cellular pharmacology. Basic Clin Pharmacol Toxicol 2005;96:15-25
  • Gennari L, Merlotti D, De Paola V, Nuti R. Raloxifene in breast cancer prevention. Expert Opin Drug Saf 2008b;7:259-70
  • Riggs BL, Hartmann LC. Selective estrogen-receptor modulators-mechanisms of action and application to clinical practice. N Engl J Med 2003;348:618-29
  • Gennari L, Merlotti D, Valleggi F, et al. Selective estrogen receptor modulators for postmenopausal osteoporosis: current state of development. Drugs Aging 2007;24:361-79
  • Delmas PD, Bjarnason NH, Mitlak BH, et al. Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women. N Engl J Med 1997;337:1641-7
  • Lufkin EG, Whitaker MD, Nickelsen T, et al. Treatment of established postmenopausal osteoporosis with raloxifene: a randomized trial. J Bone Miner Res 1998;13:1747-54
  • Ettinger B, Black DM, Mitlak BH, et al. Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: results from a 3-year randomized clinical trial. Multiple Outcomes of Raloxifene Evaluation (MORE) Investigators. JAMA 1999;282:637-45. (erratum JAMA. 1999;282:2124)
  • Bryant HU, Glasebrook AL, Yang NN, Sato M. A pharmacological review of raloxifene. J Bone Miner Metab 1996;14:1-9
  • Weinstein RS, Parfitt AM, Marcus R, et al. Effects of raloxifene, hormone replacement therapy, and placebo on bone turnover in postmenopausal women. Osteoporos Int 2003;14:814-22
  • Prestwood KM, Gunness M, Muchmore DB, et al. A comparison of the effects of raloxifene and estrogen on bone in postmenopausal women. J Clin Endocrinol Metab 2000;85:2197-202
  • Morello KC, Wurz GT, DeGregorio MW. SERMs: current status and future trends. Crit Rev Oncol Hematol 2002;43:63-76
  • Gennari L. Ospemifene hormos. Curr Opin Investig Drugs 2004;5(4):448-55
  • Bachman GA, Komi J, Hanley RM. A New SERM, Ophena (Ospemifene), effectively treats vulvovaginal atrophy in postmenopausal women: Results from a Pivotal Phase 3 Study. The Endocrine Society's 90th Annual Meeting, San Francisco, June 15-18, 2008, P2-513
  • Willson TM, Norris JD, Wagner BL, et al. Dissection of the molecular mechanism of action of GW5638, a novel estrogen receptor ligand, provides insights into the role of estrogen receptor in bone. Endocrinology 1997;138(9):3901-11
  • Qiang Q, Zhengt H, Dahlund J, et al. Selective estrogenic effects of a novel triphenylethylene compound, FC1271a, on bone, cholesterol levels and reproductive tissues in intact and ovariectomized rats. Endocrinology 2000;141(2):809-20
  • Qu Q, Harkonen PL, Vaananen HK. Comparative effects of estrogen and antiestrogens on differentiation of osteoblasts in mouse bone marrow culture. J Cell Biochem 1999;73(4):500-7
  • Degregorio MW, Wurz GT, Taras TL, et al. Pharmacokinetics of (deaminohydroxy)toremifene in humans: a new, selective estrogen-receptor modulator. Eur J Clin Pharmacol 2000;56(6-7):469-75
  • Wiebe VJ, Benz CC, Shemano I, et al. Pharmacokinetics of toremifene and its metabolites in patients with advanced breast cancer. Cancer Chemother Pharmacol 1990;25(4):247-51
  • Bryson S, Cornelissen K, Anttila M. Absorption, metabolism and excretion of (3H)-ospemifene following a single oral dose to postmenopausal women. Clin Pharmacol Ther 2005;77:82 [abstract]
  • Taras TL, Wurz GT, DeGregorio MW. In vitro and in vivo biologic effects of ospemifene (FC-1271a) in breast cancer. J Steroid Biochem Mol Biol 2001;77(4-5):271-9
  • Kallio A, Guo T, Lamminen E, et al. Estrogen and the selective estrogen receptor modulator (SERM) protection against cell death in estrogen receptor alpha and beta expressing U2OS cells. Mol Cell Endocrinol 2008;289(1-2):38-48
  • Parikka V, Lehenkari P, Harkonen PL, et al. The effect of two selective estrogens raloxifene and FC1271a on osteoclast survival and resorption in vitro. Bone 1998;23:S5-S552
  • Michael H, Härkönen PL, Kangas L, et al. Differential effects of selective oestrogen receptor modulators (SERMs) tamoxifen, ospemifene and raloxifene on human osteoclasts in vitro. Br J Pharmacol 2007;151(3):384-95
  • Hellmann-blumberg U, Taras TL, Wurz GT, et al. Genotoxic effects of the novel mixed antiestrogen FC-1271a in comparison to tamoxifen and toremifene. Breast Cancer Res Treat 2000;60(1):63-70
  • Namba R, Young LJ, Maglione JE, et al. Selective estrogen receptor modulators inhibit growth and progression of premalignant lesions in a mouse model of ductal carcinoma in situ. Breast Cancer Res 2005;7(6):R881-9
  • Wurz GT, Read KC, Marchisano-Karpman C, et al. Ospemifene inhibits the growth of dimethylbenzanthracene-induced mammary tumors in Sencar mice. J Steroid Biochem Mol Biol 2005;97(3):230-40
  • Wurz GT, Hellmann-Blumberg U, DeGregorio MW. Pharmacologic effects of ospemifene in rhesus macaques: a pilot study. Basic Clin Pharmacol Toxicol 2008;102(6):552-8
  • Ylikorkala O, Cacciatore B, Halonen K, et al. Effects of ospemifene, a novel SERM, on vascular markers and function in healthy, postmenopausal women. Menopause 2003;10(5):440-7
  • Rutanen EM, Heikkinen J, Halonen K, et al. Effects of ospemifene, a novel SERM, on hormones, genital tract, climacteric symptoms, and quality of life in postmenopausal women: a double-blind, randomized trial. Menopause 2003;10(5):433-9
  • Voipio SK, Komi J, Halonen K, et al. Effects of ospemifene (FC-1271a) on uterine endometrium, vaginal maturation index, and hormonal status in healthy postmenopausal women. Maturitas 2002;43(3):207-14
  • Komi J, Lankinen KS, DeGregorio M, et al. Effects of ospemifene and raloxifene on biochemical markers of bone turnover in postmenopausal women. J Bone Miner Metab 2006;24(4):314-8
  • Komi J, Heikkinen J, Rutanen EM, et al. Effects of ospemifene, a novel SERM, on biochemical markers of bone turnover in healthy postmenopausal women. Gynecol Endocrinol 2004;18(3):152-8
  • Komi J, Lankinen KS, Harkonen P, et al. Effects of ospemifene and raloxifene on hormonal status, lipids, genital tract, and tolerability in postmenopausal women. Menopause 2005;12(2):202-9
  • Available from: http//www.clinical trials.gov; A service of the US National Institute of Health developed by the National Library of Medicine. Trial identifiers: NCT00566982 and NCT00729469
  • Bernstein L, Deapen D, Cerhan JR, et al. Tamoxifen therapy for breast cancer and endometrial cancer risk. J Natl Cancer Inst 1999;91(19):1654-62
  • Morello K, Wurz GT, DeGregorio MW. Pharmacokinetics of selective estrogen receptor modulators. Clin Pharmacokinet 2003;42(4):361-72
  • Gennari L, Merlotti D, De Paola V, et al. Bazedoxifene for the prevention of postmenopausal osteoporosis. Ther Clin Risk Manag 2008;4(6):1-14
  • Taylor HS. Designing the ideal selective estrogen receptor modulator-an achievable goal? Menopause 2009 [Epub ahead of print]
  • NDA 22-242, Lasofoxifene Tartrate (Proposed trade name: FABLYN), Pfizer, Inc, Proposed Indication: ‘FABLYN is a selective estrogen receptor modulator indicated for treatment of osteoporosis in postmenopausal women at increased risk of fracture’. Background Document for Meeting of Advisory Committee for Reproductive Health Drugs (September 8, 2008); Prepared by Division of Reproductive and Urologic Products Office of New Drugs Center for Drug Evaluation and Research Food and Drug Administration August 15, 2008. Available from: http://www.fda.gov/ohrms/dockets/ac/08/briefing/2008-4381b1-01-FDA.pdf. [Last accessed 4 March 2009]

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.