Bazedoxifene: A novel selective estrogen receptor modulator for postmenopausal osteoporosis

Climacteric

Volumn 13, Issue 3, 2010, Pages 210-218

  De Villiers, T J ^a  

^a STELLENBOSCH UNIVERSITY   (South Africa)

Author keywords

Bazedoxifene; Bone mineral density; Osteoporosis; Osteoporotic fracture; Postmenopausal; Selective estrogen receptor modulator

Indexed keywords

BAZEDOXIFENE; BISPHOSPHONIC ACID DERIVATIVE; CONJUGATED ESTROGEN; LIPID; PLACEBO; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR;

ABDOMINAL PAIN; ARTHRALGIA; BACKACHE; BONE DENSITY; BONE TURNOVER; BREAST CANCER; BREAST DISEASE; CLINICAL TRIAL; DEEP VEIN THROMBOSIS; DOSE RESPONSE; DRUG EFFICACY; DRUG INDUCED HEADACHE; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; ENDOMETRIUM CANCER; ENDOMETRIUM HYPERPLASIA; ENDOMETRIUM POLYP; FLU LIKE SYNDROME; HORMONE SUBSTITUTION; HOT FLUSH; HUMAN; HYPERTENSION; INFECTION; JAW OSTEONECROSIS; LEG CRAMP; LIPID BLOOD LEVEL; LUNG EMBOLISM; MENOPAUSAL SYNDROME; NONHUMAN; OSTEOLYSIS; PAIN; POSTMENOPAUSE OSTEOPOROSIS; PRIORITY JOURNAL; PROTECTION; REVIEW; VENOUS THROMBOEMBOLISM; VERTEBRA FRACTURE;

CLINICAL TRIALS, PHASE III AS TOPIC; ENDOMETRIUM; FEMALE; FRACTURES, BONE; HUMANS; INDOLES; LIPIDS; MAMMOGRAPHY; OSTEOPOROSIS, POSTMENOPAUSAL; SELECTIVE ESTROGEN RECEPTOR MODULATORS; VENOUS THROMBOEMBOLISM;

EID: 77951836991     PISSN: 13697137     EISSN: 14730804     Source Type: Journal    
DOI: 10.3109/13697130903568542     Document Type: Review

References (48)

1. North American Menopause Society. Management of osteoporosis in postmenopausal women: 2006 position statement of The North American Menopause Society. Menopause 2006;13:340-367
2. Curtis JR, McClure LA, Delzell E, et al. Population-based fracture risk assessment and osteoporosis treatment disparities by race and gender. J Gen Intern Med 2009;24: 956-962
3. Caliri A, De Filippis L, Bagnato GL, Bagnato GF. Osteoporotic fractures: mortality and quality of life. Panminerva Med 2007;49:21-27
4. Desai SS, Duncan BS, Sloan AS. The cost of treating osteoporosis in a managed health care organization. JManag Care Pharm 2003;9:142-149
5. Gold DT. The nonskeletal consequences of osteoporotic fractures. Psychologic and social outcomes. Rheum Dis Clin North Am 2001;27:255-262
6. Salaffi F, Cimmino MA, Malavolta N, et al. The burden of prevalent fractures on health-related quality of life in postmenopausal women with osteoporosis: the IMOF study. J Rheumatol 2007;34:1551-1560
7. MacLean C, Newberry S, Maglione M, et al. Systematic review: comparative effectiveness of treatments to prevent fractures in men and women with low bone density or osteoporosis. Ann Intern Med 2008;148:197-213
8. Komm BS, Lyttle CR. Developing a SERM: stringent preclinical selection criteria leading to an acceptable candidate (WAY-140424) for clinical evaluation. Ann N Y Acad Sci 2001;949:317-326
9. Arun B, Anthony M, Dunn B. The search for the ideal SERM. Expert Opin Pharmacother 2002;3:681-691
10. Gennari L, Merlotti D, Valleggi F, Martini G, Nuti R. Selective estrogen receptor modulators for postmenopausal osteoporosis: current state of development. Drugs Aging 2007;24:361-379
11. Komm BS, Kharode YP, Bodine PV, Harris HA, Miller CP, Lyttle CR. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology 2005;146:3999-4008
12. Peano BJ, Crabtree JS, Komm BS, Winneker RC, Harris HA. Effects of various selective estrogen receptor modulators with or without conjugated estrogens on mouse mammary gland. Endocrinology 2009;150:1897-1903
13. Ronkin S, Clarke L. TSE-424, a novel tissue selective estrogen, reduces biochemical indices of bone metabolism in a dose related fashion. J Bone Miner Res 2001;16(Suppl 1):S413 [abstract SU437]
14. 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)
15. 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
16. 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 active-controlled clinical trial. J Bone Miner Res 2008;23:1923-1934
17. 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
18. Kanis JA, on behalf of the World Health Organization Scientific Group. Assessment of Osteoporosis at the Primary Health Care Level. Technical report. Sheffield, UK: World Health Organization Collaborating Centre for Metabolic Bone Diseases, 2008
19. Kanis JA, Johnell O, Oden A, Johansson H, McCloskey E. FRAX and the assessment of fracture probability in men and women from the UK. Osteoporos Int 2008;19:385-397
20. World Health Organization. Assessment of osteoporosis at the primary health care level. Summary Report of a WHO Scientific Group. Geneva: World Health Organization, 2007. http://www.who.int/chp/topics/rheumatic/en/index. html [serial online]; Accessed March 5, 2009
21. McCloskey E, Johansson H, Oden A, Chines A, Kanis J. Assessment of the effect of bazedoxifene on non-vertebral fracture risk. J Bone Miner Res 2009;24(Suppl 1). Available at: http://www.asbmr.org/Meetings/AnnualMeeting/ Abstract Detail.aspx?aid=6c55b263-692e-4a37-b807-f7a153641564. Accessed October 26, 2009
22. Silverman S, Chines A, Zanchetta JR, et al. Sustained efficacy of bazedoxifene in preventing fractures in postmenopausal women with osteoporosis: results of a 5-year, randomized, placebo-controlled study. J Bone Miner Res 2009;24(Suppl 1). Available at: http://www.asbmr.org/ Meetings/AnnualMeeting/ AbstractDetail.aspx?aid=2643e a2f-c4ab-4eb6-9798-09050bb21b6b. Accessed October 15, 2009
23. de Villiers TJ, Kendler D, Chines A, et al. Safety and tolerability of bazedoxifene in postmenopausal women with osteoporosis: results of a 5-year, randomized, placebo-controlled phase 3 trial. J Bone Miner Res 2009;24(Suppl 1). Available at: http://www.asbmr.org/ Meetings/AnnualMeeting/AbstractDetail.aspx? aid=1dae18 c8-99a0-4757-957b-689b21823623. Accessed October 15, 2009
24. Fleischer AC, Wheeler JE, Yeh IT, Kravitz B, Jensen C, MacDonald B. Sonographic assessment of the endometrium in osteopenic postmenopausal women treated with idoxifene. J Ultrasound Med 1999;18:503-512
25. Goldstein SR, Nanavati N. Adverse events that are associated with the selective estrogen receptor modulator levormeloxifene in an aborted phase III osteoporosis treatment study. Am J Obstet Gynecol 2002;187:521-527
26. 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
27. 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
28. Harvey JA, Holm MK, Ranganath R, Guse PA, Trott EA, Helzner E. The effects of bazedoxifene on mammographic breast density in postmenopausal women with osteoporosis. Menopause 2009;16: 1193-1196
29. Palacios S, Menegoci JC, Kelepouris N, Constantine GD, de Villiers TJ. Endometrial and breast safety of bazedoxifene in postmenopausal women with osteoporosis: findings from a 5-year, randomized, placebo-controlled phase 3 trial. Menopause 2009;16:1263
30. 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. JAMA 1999;282:637-645
31. Grady D, Ettinger B, Moscarelli E, et al. Safety and adverse effects associated with raloxifene: multiple outcomes of raloxifene evaluation. Obstet Gynecol 2004;104: 837-844
32. Adachi JD, Chesnut CH, Brown JP, et al. Safety and tolerability of bazedoxifene in postmenopausal women with osteoporosis: results from a 3-year, randomized, placebo- and active-controlled clinical trial. Poster presented at 35th European Symposium on Calcified Tissues, May 24-28, 2008, Barcelona, Spain
33. 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
34. Komm BS. A new approach to menopausal therapy: the tissue selective estrogen complex. Reprod Sci 2008;15: 984-992
35. 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
36. 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
37. Pickar JH, Yeh I-T, 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
38. 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
39. Pinkerton JV, Utian WH, Constantine GD, Olivier S, Pickar JH. Relief of vasomotor symptoms with the tissueselective estrogen complex containing bazedoxifene/conjugated estrogens: a randomized, controlled trial. Menopause 2009;16:1116-1124
40. Kagan R, Williams RS, Pan K, Mirkin S, Pickar JH. A randomized, placebo- and active-controlled trial of bazedoxifene/ conjugated estrogens for treatment of moderate to severe vulvar/vaginal atrophy in postmenopausal women [published online ahead of print September 25, 2009]. Menopause doi:10.1097/GME. 0b013e3181b7c65f
41. National Osteoporosis Foundation. Clinician's guide to prevention and treatment of osteoporosis. http://www.nof. org/professionals/Clinicians-Guide. htm [serial online]; AccessedOctober 28, 2009
42. Ruggiero SL, Dodson TB, Assael LA, Landesberg R, Marx RE, Mehrotra B. American Association of Oral and Maxillofacial Surgeons position paper on bisphosphonaterelated osteonecrosis of the jaws - 2009 update. J Oral Maxillofac Surg 2009;67:2-12
43. Solomon DH, Rekedal L, Cadarette SM. Osteoporosis treatments and adverse events. Curr Opin Rheumatol 2009;21:363-368
44. Department of Health and Human Services, Public Health Service, Food and Drug Administration. ODS Postmarketing Safety Review. FDA osteonecrosis statement. 2004
45. InternationalOsteoporosis Foundation. Osteonecrosis of the jaw. http://www.iofbonehealth.org/health-professionals/ special-topics/osteonecrosis- of-jaw.html [serial online]; Accessed August 10, 2009
46. 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
47. Martino S, Cauley JA, Barrett-Connor E, et al. Continuing outcomes relevant to Evista: breast cancer incidence in postmenopausal osteoporotic women in a randomized trial of raloxifene. J Natl Cancer Inst 2004;96:1751-1761
48. Kanis JA. Diagnosis of osteoporosis and assessment of fracture risk. Lancet 2002;359: 1929-1936