Approaching the ideal selective estrogen receptor modulator for prevention and treatment of postmenopausal osteoporosis

Formulary

Volumn 45, Issue 2, 2010, Pages 52-61

  Taylor, Hugh S ^a  

^a YALE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALENDRONIC ACID; ARZOXIFENE; BAZEDOXIFENE; CALCITONIN; CENTCHROMAN; CONJUGATED ESTROGEN; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; IBANDRONIC ACID; IDOXIFENE; LASOFOXIFENE; LOW DENSITY LIPOPROTEIN CHOLESTEROL; LSN 2120310; OSPEMIFENE; PARATHYROID HORMONE[1-34]; PLACEBO; RAD 1901; RALOXIFENE; RISEDRONIC ACID; SALCATONIN; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN; UNCLASSIFIED DRUG; Y 134; ZOLEDRONIC ACID;

BONE DENSITY; BONE REMODELING; BONE TURNOVER; BREAST CANCER; CANCER RISK; CHOLESTEROL BLOOD LEVEL; CLAVICLE FRACTURE; CLINICAL EVALUATION; CLINICAL TRIAL; COST EFFECTIVENESS ANALYSIS; DEEP VEIN THROMBOSIS; DRUG EFFICACY; DRUG SELECTIVITY; DRUG TOLERABILITY; DRUG WITHDRAWAL; DUAL ENERGY X RAY ABSORPTIOMETRY; ENDOMETRIAL DISEASE; ENDOMETRIUM CANCER; ENDOMETRIUM POLYP; EUROPEAN UNION; FOOD AND DRUG ADMINISTRATION; FRACTURE; GYNECOLOGIC DISEASE; HEALTH CARE COST; HIP FRACTURE; HOT FLUSH; HUMAN; HUMERUS FRACTURE; ISCHEMIC HEART DISEASE; JAW OSTEONECROSIS; LEG CRAMP; LEG FRACTURE; LIPID ANALYSIS; LOW DRUG DOSE; LUMBAR SPINE; OSTEOPENIA; PELVIS FRACTURE; POST HOC ANALYSIS; POSTMENOPAUSE OSTEOPOROSIS; PRACTICE GUIDELINE; PREVALENCE; REVIEW; RISK BENEFIT ANALYSIS; STROKE; UNITED STATES; VAGINA ATROPHY; VAGINA BLEEDING; VENOUS THROMBOEMBOLISM; VERTEBRA FRACTURE; WRIST FRACTURE;

EID: 77954780711     PISSN: 1082801X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (83)

1. Dennison E, Cooper C. Epidemiology of osteoporotic fractures. Horm Res. 2000;54 (Suppl 1):58-63.
2. Looker AC, Orwoll ES, Johnston CC, Jr, et al. Prevalence of low femoral bone density in older U.S. adults from NHANES III. J Bone Miner Res. 1997;12:1761-1768.
3. Desai SS, Duncan BS, Sloan AS. The cost of treating osteoporosis in a managed health care organization. J Manag Care Pharm. 2003;9:142-149.
4. Burge R, Dawson-Hughes B, Solomon DH, Wong JB, King A, Tosteson A. Incidence and economic burden of osteoporosis-related fractures in the United States, 2005-2025. J Bone Miner Res. 2007;22:465-475.
5. Center JR, Nguyen TV, Schneider D, Sambrook PN, Eisman JA. Mortality after all major types of osteoporotic fracture in men and women: an observational study. Lancet. 1999;353:878-882.
6. Kanis JA, Oden A, Johansson H, Borgström F, Ström O, McCloskey E. FRAX and its applications to clinical practice. Bone. 2009;44:734-743.
7. North American Menopause Society. Management of osteoporosis in postmenopausal women: 2006 position statement of The North American Menopause Society. Menopause. 2006;13:340-367.
8. Riggs BL, Hartmann LC. Selective estrogenreceptor modulators - mechanisms of action and application to clinical practice. N Engl J Med. 2003;348:618-629.
9. Taylor HS. Designing the ideal selective estrogen receptor modulator - an achievable goal? Menopause. 2009;16:609-615
10. Love RR, Mazess RB, Barden HS, et al. Effects of tamoxifen on bone mineral density in postmenopausal women with breast cancer. N Engl J Med. 1992;326:852-856.
11. Christodoulakos GE, Lambrinoudaki IV, Botsis DC. The cardiovascular effects of selective estrogen receptor modulators. Ann NY Acad Sci. 2006;1092:374-384.
12. Rutqvist LE, Mattsson A. Cardiac and thromboembolic morbidity among postmenopausal women with early-stage breast cancer in a randomized trial of adjuvant tamoxifen. The Stockholm Breast Cancer Study Group. J Natl Cancer Inst. 1993;85:1398-1406.
13. Fisher B, Costantino 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 (NSABP) B-14. J Natl Cancer Inst. 1994;86:527-537. (Pubitemid 24111008)
14. Cohen I. Endometrial pathologies associated with postmenopausal tamoxifen treatment. Gynecol Oncol. 2004;94:256-266.
15. Fisher B, Costantino JP, Wickerham DL, et al. Tamoxifen for prevention of breast cancer: report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study. J Natl Cancer Inst. 1998;90:1371-1388.
16. Love RR, Cameron L, Connell BL, Leventhal H. Symptoms associated with tamoxifen treatment in postmenopausal women. Arch Intern Med. 1991;151:1842-1847.
17. Dignam JJ, Fisher B. Occurrence of stroke with tamoxifen in NSABP B-24. Lancet. 2000;355:848-849.
18. 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;337:1641-1647.
19. 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;282:637-645.
20. Delmas PD, Ensrud KE, Adachi JD, et al; Multiple Outcomes of Raloxifene Evaluation Investigators. Efficacy of raloxifene on vertebral fracture risk reduction in postmenopausal women with osteoporosis: four-year results from a randomized clinical trial. J Clin Endocrinol Metab. 2002;87:3609-3617.
21. Delmas PD, Genant HK, Crans GG, et al. Severity of prevalent vertebral fractures and the risk of subsequent vertebral and nonvertebral fractures: results from the MORE trial. Bone. 2003;33:522-532.
22. Siris ES, Harris ST, Eastell R, et al; Continuing Outcomes Relevant to Evista (CORE) Investigators. Skeletal effects of raloxifene after 8 years: results from the continuing outcomes relevant to Evista (CORE) study. J Bone Miner Res. 2005;20:1514-1524.
23. Barrett-Connor E, Mosca L, Collins P, et al; Raloxifene Use for the Heart (RUTH) Trial Investigators. Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women. N Engl J Med. 2006;355:125-137.
24. Vogel VG, Costantino JP, Wickerham DL, et al; National Surgical Adjuvant Breast and Bowel Project (NSABP). Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial. JAMA. 2006;295:2727-2741.
25. Cummings SR, Eckert S, Krueger KA, et al. 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.
26. Glusman JE, Huster WJ, Paul S. Raloxifene effects on vasomotor and other climacteric symptoms in postmenopausal women. Prim Care Update Ob Gyns. 1998;5:166.
27. Davies GC, Huster WJ, Lu Y, Plouffe L Jr, Lakshmanan M. Adverse events reported by postmenopausal women in controlled trials with raloxifene. Obstet Gynecol. 1999;93:558-565.
28. Mosca L, Grady D, Barrett-Connor E, et al. Effect of raloxifene on stroke and venous thromboembolism according to subgroups in postmenopausal women at increased risk of coronary heart disease. Stroke. 2009;40:147-155.
29. Ronkin S, Clarke L. TSE-424, a novel tissue selective estrogen, reduces biochemical indices of bone metabolism in a dose related fashion [abstract SU437]. J Bone Miner Res. 2001;16(Suppl 1):S413.
30. Boudes P, Ronkin S, Korner P, Baracat E, Constantine G. Effects of bazedoxifene (TSE-424), a novel tissue selective estrogen receptor modulator (SERM), on the incidence of breast pain [abstract OC39]. Osteoporos Int. 2003;14(Suppl 7):S14.
31. Ronkin S, Northington R, Baracat E, et al. Endometrial effects of bazedoxifene acetate, a novel selective estrogen receptor modulator, in postmenopausal women. Obstet Gynecol. 2005;105:1397-1404. (Pubitemid 40734275)
32. Miller PD, Chines AA, Christiansen C, et al. Effects of bazedoxifene on BMD and bone turnover in postmenopausal women: 2-yr results of a randomized, double-blind, placebo-, and active-controlled study. J Bone Miner Res. 2008;23:525-535.
33. Silverman SL, Christiansen C, Genant HK, et al. Efficacy of bazedoxifene in reducing new vertebral fracture risk in postmenopausal women with osteoporosis: results from a 3-year, randomized, placebo- and activecontrolled clinical trial. J Bone Miner Res. 2008;23:1923-1934.
34. Kanis JA, Johansson H, Oden A, McCloskey EV. Bazedoxifene reduces vertebral and clinical fractures in postmenopausal women at high risk assessed with FRAX. Bone. 2009;44:1049-1054.
35. McCloskey EV, Johansson H, Oden A, et al. Ten-year fracture probability identifies women who will benefit from clodronate therapy-additional results from a double-blind, placebo-controlled randomised study. Osteoporos Int. 2009;20:811-817.
36. Pinkerton JV, Archer DF, Utian WH, et al. Bazedoxifene effects on the reproductive tract in postmenopausal women at risk for osteoporosis. Menopause. 2009;16:1102-1108.
37. Archer DF, Pinkerton JV, Utian WH, et al. Bazedoxifene, a selective estrogen receptor modulator: effects on the endometrium, ovaries, and breast from a randomized controlled trial in osteoporotic postmenopausal women. Menopause. 2009;16:1109-1115.
38. Lindsay R, Gallagher JC, Kagan R, Pickar JH, Constantine G. Efficacy of tissue-selective estrogen complex of bazedoxifene/conjugated estrogens for osteoporosis prevention in at-risk postmenopausal women. Fertil Steril. 2009;92:1045-1052.
39. Lobo RA, Pinkerton JV, Gass ML, et al. Evaluation of bazedoxifene/ conjugated estrogens for the treatment of menopausal symptoms and effects on metabolic parameters and overall safety profile. Fertil Steril. 2009;92:1025-1038.
40. Pickar JH, Yeh IT, Bachmann G, Speroff L. Endometrial effects of a tissue selective estrogen complex containing bazedoxifene/conjugated estrogens as a menopausal therapy. Fertil Steril. 2009;92:1018-1024.
41. Archer DF, Lewis V, Carr BR, Olivier S, Pickar JH. Bazedoxifene/ conjugated estrogens (BZA/CE): incidence of uterine bleeding in postmenopausal women. Fertil Steril. 2009;92:1039-1044.
42. Komm BS. A new approach to menopausal therapy: the tissue selective estrogen complex. Reprod Sci. 2008;15:984-992.
43. Kharode Y, Bodine PV, Miller CP, Lyttle CR, Komm BS. The pairing of a selective estrogen receptor modulator, bazedoxifene, with conjugated estrogens as a new paradigm for the treatment of menopausal symptoms and osteoporosis prevention. Endocrinology. 2008;149:6084-6091.
44. McClung MR, Siris E, Cummings S, et al. Prevention of bone loss in postmenopausal women treated with lasofoxifene compared with raloxifene. Menopause. 2006;13:377-386.
45. Cummings SR, Eastell R, Ensrud K, et al. The effects of lasofoxifene on fractures and breast cancer: 3-year results from the PEARL trial [abstract 1288]. J Bone Miner Res. 2008;23(Suppl 1):S81.
46. Eastell R, Reid DM, Vukicevic S, et al. The effects of lasofoxifene on bone turnover markers: the PEARL trial. [abstract 1287]. J Bone Miner Res. 2008;23(Suppl 1):S81.
47. Bachmann G, Gass M, Kagan R, Moffett A, Barcomb L, Symons J. Lasofoxifene (laso), a next generation selective estrogen response modulator (SERM), improves dyspareunia in postmenopausal women with vaginal atrophy (VA) [abstract ED1]. Menopause. 2005;12:238.
48. Gass M, Portman D, Bachmann G, Moffett A, Symons J. Clinical signs of vaginal atrophy are improved by the SERM, lasofoxifene [abstract P-68]. Menopause. 2004;11:670.
49. Bachmann G, Gass M, Moffett A, Portman D, Symons J. Lasofoxifene improves symptoms associated with vaginal atrophy [abstract P-63]. Menopause. 2004;11:669.
50. Pfizer Inc. FABLYN (lasofoxifene tartrate) 0.5 mg Tablets. NDA 22-242. Reproductive Health Drugs Advisory Committee Briefing Document, 08 September 2008. Available at: http://www.fda.gov/ohrms/dockets/ac/08/briefing/2008-4381b1- 02-Pfizer.pdf. Accessed January 6, 2010.
51. 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;24:314-318.
52. Komi J, Heikkinen J, Rutanen EM, Halonen K, Lammintausta R, Ylikorkala O. Effects of ospemifene, a novel SERM, on biochemical markers of bone turnover in healthy postmenopausal women. Gynecol Endocrinol. 2004;18:152-158.
53. Voipio SK, Komi J, Kangas L, Halonen K, DeGregorio MW, Erkkola RU. Effects of ospemifene (FC-1271a) on uterine endometrium, vaginal maturation index, and hormonal status in healthy postmenopausal women. Maturitas. 2002;43:207-214.
54. Rutanen EM, Heikkinen J, Halonen K, Komi J, Lammintausta R, Ylikorkala O. 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;10:433-439.
55. Komi J, Lankinen KS, Hörkönen P, et al. Effects of ospemifene and raloxifene on hormonal status, lipids, genital tract, and tolerability in postmenopausal women. Menopause. 2005;12:202-209.
56. Munster PN. Arzoxifene: the development and clinical outcome of an ideal SERM. Expert Opin Investig Drugs. 2006;15:317-326.
57. Fabian CJ, Kimler BF, Anderson J, et al. Breast cancer chemoprevention phase I evaluation of biomarker modulation by arzoxifene, a third generation selective estrogen receptor modulator. Clin Cancer Res. 2004;10:5403-5417.
58. Munster PN, Buzdar A, Dhingra K, et al. Phase I study of a third-generation selective estrogen receptor modulator, LY353381. HCL, in metastatic breast cancer. J Clin Oncol. 2001;19:2002-2009.
59. Baselga J, Llombart-Cussac A, Bellet M, et al. Randomized, double-blind, multicenter trial comparing two doses of arzoxifene (LY353381) in hormone-sensitive advanced or metastatic breast cancer patients. Ann Oncol. 2003;14:1383-1390.
60. Buzdar A, O'Shaughnessy JA, Booser DJ, et al. Phase II, randomized, double-blind study of two dose levels of arzoxifene in patients with locally advanced or metastatic breast cancer. J Clin Oncol. 2003;21:1007-1014.
61. Deshmane V, Krishnamurthy S, Melemed AS, Peterson P, Buzdar AU. Phase III double-blind trial of arzoxifene compared with tamoxifen for locally advanced or metastatic breast cancer. J Clin Oncol. 2007;25:4967-4973.
62. Bolognese M, Krege JH, Utian WH, et al. Effects of arzoxifene on bone mineral density and endometrium in postmenopausal women with normal or low bone mass. J Clin Endocrinol Metab. 2009;94:2284-2289.
63. Eli Lilly and Company. Lilly reports on outcome of phase III study of arzoxifene. Based on preliminary phase III GJAD study results, Lilly concludes arzoxifene's clinical profile does not support regulatory submission [press release]. Available at: http://news.prnewswire.com/ViewContent.aspx?ACCT= 109&STORY=/www/story/08-18-2009/0005079632&EDATE=. Accessed January 6, 2010.
64. Wells GA, Cranney A, Peterson J, et al. Alendronate for the primary and secondary prevention of osteoporotic fractures in postmenopausal women. Cochrane Database Syst Rev. 2008;(1):CD001155.
65. Wells G, Cranney A, Peterson J, et al. Risedronate for the primary and secondary prevention of osteoporotic fractures in postmenopausal women. Cochrane Database Syst Rev. 2008;(1):CD004523.
66. Chesnut III CH, Skag A, Christiansen C, et al; Oral Ibandronate Osteoporosis Vertebral Fracture Trial in North America and Europe (BONE). Effects of oral ibandronate administered daily or intermittently on fracture risk in postmenopausal osteoporosis. J Bone Miner Res. 2004;19:1241-1249.
67. Black DM, Delmas PD, Eastell R, et al; HORIZON Pivotal Fracture Trial. Onceyearly zoledronic acid for treatment of postmenopausal osteoporosis. N Engl J Med. 2007;356:1809-1822.
68. Bobba RS, Beattie K, Parkinson B, Kumbhare D, Adachi JD. Tolerability of different dosing regimens of bisphosphonates for the treatment of osteoporosis and malignant bone disease. Drug Saf. 2006;29:1133-1152.
69. Strampel W, Emkey R, Civitelli R. Safety considerations with bisphosphonates for the treatment of osteoporosis. Drug Saf. 2007;30:755-763.
70. Schneider JP. Bisphosphonates and lowimpact femoral fractures: current evidence on alendronate-fracture risk. Geriatrics. 2009;64:18-23.
71. Solomon DH, Rekedal L, Cadarette SM. Osteoporosis treatments and adverse events. Curr Opin Rheumatol. 2009;21:363-368.
72. Ruggiero SL, Mehrotra B, Rosenberg TJ, Engroff SL. Osteonecrosis of the jaws associated with the use of bisphosphonates: a review of 63 cases. J Oral Maxillofac Surg. 2004;62:527-534.
73. Hulley S, Grady D, Bush T, et al. Heart and Estrogen/progestin Replacement Study (HERS) Research Group. Randomized trial of estrogen plus progestin for secondary prevention of coronary heart disease in postmenopausal women. JAMA. 1998;280:605-613.
74. Rossouw JE, Anderson GL, Prentice RL, et al; Writing Group for the Women's Health Initiative Investigators. Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the Women's Health Initiative randomized controlled trial. JAMA. 2002;288:321-333.
75. Vickers MR, MacLennan AH, Lawton B, et al; WISDOM group. Main morbidities recorded in the women's international study of long duration oestrogen after menopause (WISDOM): a randomised controlled trial of hormone replacement therapy in postmenopausal women. BMJ. 2007;335:239.
76. Utian WH, Archer DF, Bachmann GA, et al; North American Menopause Society. Estrogen and progestogen use in postmenopausal women: July 2008 position statement of The North American Menopause Society. Menopause. 2008;15:584-602.
77. Miller PD. Anti-resorptives in the management of osteoporosis. Best Pract Res Clin Endocrinol Metab. 2008;22:849-868.
78. Cole Z, Dennison E, Cooper C. Update on the treatment of post-menopausal osteoporosis. Br Med Bull. 2008;86:129-143.
79. National Osteoporosis Foundation. Clinician's guide to prevention and treatment of osteoporosis. Available at: http://www.nof.org/professionals/ Clinicians-Guide.htm. Accessed January 7, 2010.
80. Tosteson AN, Burge RT, Marshall DA, Lindsay R. Therapies for treatment of osteoporosis in US women: cost-effectiveness and budget impact considerations. Am J Manag Care. 2008;14:605-615.
81. Kanis JA, Borgström F, Johnell O, Oden A, Sykes D, Jönsson B. Cost-effectiveness of raloxifene in the UK: an economic evaluation based on the MORE study. Osteoporos Int. 2005;16:15-25.
82. Borgström F, Johnell O, Kanis JA, Oden A, Sykes D, Jönsson B. Cost effectiveness of raloxifene in the treatment of osteoporosis in Sweden: an economic evaluation based on the MORE study. Pharmacoeconomics. 2004;22:1153-1165.
83. Strom O, BorgströmF, McCloskey E, Oden A, Johansson H, Kanis J. Cost-effectiveness of bazedoxifene in the US incorporating the FRAX-algorithm. J Bone Miner Res. 2009;24(Suppl 1). Available at: http://www.asbmr.org/Meet ings/AnnualMeet ing/Abstract Detail .aspx?a id=b1416cf8-4c60-4fa9-a0c6- 3b18f4b8719f. Accessed January 7, 2010.