The effects of bazedoxifene in the ovariectomized aged cynomolgus monkey

Journal of Bone and Mineral Metabolism

Volumn 33, Issue 2, 2015, Pages 161-172

  Smith, Susan Y ^a   Jolette, Jacquelin ^a   Chouinard, Luc ^a   Komm, Barry S ^b  

^a CHARLES RIVER LABORATORIES   (United States)

^b PFIZER INC   (United States)

Author keywords

Bazedoxifene; Osteoporosis; Prevention; Selective estrogen receptor modulator; Treatment

Indexed keywords

BAZEDOXIFENE; INDOLE DERIVATIVE; SELECTIVE ESTROGEN RECEPTOR MODULATOR;

ANIMAL; BONE DENSITY; BONE REMODELING; DRUG EFFECTS; DRUG SCREENING; FEMALE; FEMUR; HUMAN; LUMBAR VERTEBRA; MACACA FASCICULARIS; METABOLISM; OSTEOLYSIS; OSTEOPOROSIS, POSTMENOPAUSAL; OVARIECTOMY; PHOTON ABSORPTIOMETRY; PROCEDURES;

ABSORPTIOMETRY, PHOTON; ANIMALS; BONE DENSITY; BONE REMODELING; BONE RESORPTION; DRUG EVALUATION, PRECLINICAL; FEMALE; FEMUR; HUMANS; INDOLES; LUMBAR VERTEBRAE; MACACA FASCICULARIS; OSTEOPOROSIS, POSTMENOPAUSAL; OVARIECTOMY; SELECTIVE ESTROGEN RECEPTOR MODULATORS;

EID: 84895933265     PISSN: 09148779     EISSN: 14355604     Source Type: Journal    
DOI: 10.1007/s00774-014-0580-z     Document Type: Article

References (43)

1. Fast Facts on Osteoporosis. National Osteoporosis Foundation. http://www.nof.org/node/40. Accessed 28 Feb 2014
2. Burge R, Dawson-Hughes B, Solomon DH, Wong JB, King A, Tosteson A (2007) Incidence and economic burden of osteoporosis-related fractures in the United States, 2005–2025. J Bone Miner Res 22:465–475
3. Atik OS, Gunal I, Korkusuz F (2006) Burden of osteoporosis. Clin Orthop Relat Res 443:19–24
4. Ioannidis G, Papaioannou A, Hopman WM, Akhtar-Danesh N, Anastassiades T, Pickard L, Kennedy CC, Prior JC, Olszynski WP, Davison KS, Goltzman D, Thabane L, Gafni A, Papadimitropoulos EA, Brown JP, Josse RG, Hanley DA, Adachi JD (2009) Relation between fractures and mortality: results from the Canadian Multicentre Osteoporosis Study. CMAJ 181:265–271
5. Salaffi F, Cimmino MA, Malavolta N, Carotti M, Di ML, Scendoni P, Grassi W (2007) The burden of prevalent fractures on health-related quality of life in postmenopausal women with osteoporosis: the IMOF study. J Rheumatol 34:1551–1560
6. Management of osteoporosis in postmenopausal women (2010) 2010 position statement of The North American Menopause Society. Menopause 17:25–54
7. Deroo BJ, Korach KS (2006) Estrogen receptors and human disease. J Clin Invest 116:561–570
8. Komm BS, Lyttle CR (2001) Developing a SERM: stringent preclinical selection criteria leading to an acceptable candidate (WAY-140424) for clinical evaluation. Ann N Y Acad Sci 949:317–326
9. Komm BS, Kharode YP, Bodine PV, Harris HA, Miller CP, Lyttle CR (2005) Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology 146:3999–4008
10. Miller CP, Collini MD, Tran BD, Harris HA, Kharode YP, Marzolf JT, Moran RA, Henderson RA, Bender RH, Unwalla RJ, Greenberger LM, Yardley JP, Abou-Gharbia MA, Lyttle CR, Komm BS (2001) Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. J Med Chem 44:1654–1657
11. Lewis-Wambi JS, Kim H, Curpan R, Grigg R, Sarker MA, Jordan VC (2011) The selective estrogen receptor modulator bazedoxifene inhibits hormone-independent breast cancer cell growth and down-regulates estrogen receptor alpha and cyclin D1. Mol Pharmacol 80:610–620
12. Archer DF (2004) Role of the nonhuman primate for research related to women’s health. ILAR J 45:212–219
13. Bellino FL, Wise PM (2003) Nonhuman primate models of menopause workshop. Biol Reprod 68:10–18
14. Brommage R (2001) Perspectives on using nonhuman primates to understand the etiology and treatment of postmenopausal osteoporosis. J Musculoskelet Neuronal Interact 1:307–325
15. Smith SY, Jolette J, Turner CH (2009) Skeletal health: primate model of postmenopausal osteoporosis. Am J Primatol 71:752–765
16. Ronkin S, Northington R, Baracat E, Nunes MG, Archer DF, Constantine G, Pickar JH (2005) Endometrial effects of bazedoxifene acetate, a novel selective estrogen receptor modulator, in postmenopausal women. Obstet Gynecol 105:1397–1404
17. Guidelines for preclinical and clinical evaluation of agents used in the prevention or treatment of postmenopausal osteoporosis. Division of Metabolic and Endocrine Drug Products; Food and Drug Administration. http://www.fda.gov. Accessed 28 Feb 2014
18. Lundon K, Grynpas M (1993) The long-term effect of ovariectomy on the quality and quantity of cortical bone in the young cynomolgus monkey: a comparison of density fractionation and histomorphometric techniques. Bone 14:389–395
19. Turner CH, Burr DB (1993) Basic biomechanical measurements of bone: a tutorial. Bone 14:595–608
20. Parfitt AM, Drezner MK, Glorieux FH, Kanis JA, Malluche H, Meunier PJ, Ott SM, Recker RR (1987) Bone histomorphometry: standardization of nomenclature, symbols, and units. Report of the ASBMR Histomorphometry Nomenclature Committee. J Bone Miner Res 2:595–610
21. Hotchkiss CE, Stavisky R, Nowak J, Brommage R, Lees CJ, Kaplan J (2001) Levormeloxifene prevents increased bone turnover and vertebral bone loss following ovariectomy in cynomolgus monkeys. Bone 29:7–15
22. Mashiba T, Turner CH, Hirano T, Forwood MR, Johnston CC, Burr DB (2001) Effects of suppressed bone turnover by bisphosphonates on microdamage accumulation and biomechanical properties in clinically relevant skeletal sites in beagles. Bone 28:524–531
23. Allen MR, Iwata K, Phipps R, Burr DB (2006) Alterations in canine vertebral bone turnover, microdamage accumulation, and biomechanical properties following 1-year treatment with clinical treatment doses of risedronate or alendronate. Bone 39:872–879
24. Mashiba T, Hirano T, Turner CH, Forwood MR, Johnston CC, Burr DB (2000) Suppressed bone turnover by bisphosphonates increases microdamage accumulation and reduces some biomechanical properties in dog rib. J Bone Miner Res 15:613–620
25. Seeman E (2008) Structural basis of growth-related gain and age-related loss of bone strength. Rheumatology (Oxford) 47 Suppl 4:iv2–iv8
26. Lewiecki EM, Watts NB (2008) Assessing response to osteoporosis therapy. Osteoporos Int 19:1363–1368
27. Lees CJ, Register TC, Turner CH, Wang T, Stancill M, Jerome CP (2002) Effects of raloxifene on bone density, biomarkers, and histomorphometric and biomechanical measures in ovariectomized cynomolgus monkeys. Menopause 9:320–328
28. Ott SM, Oleksik A, Lu Y, Harper K, Lips P (2002) Bone histomorphometric and biochemical marker results of a 2-year placebo-controlled trial of raloxifene in postmenopausal women. J Bone Miner Res 17:341–348
29. Stepan JJ, Alenfeld F, Boivin G, Feyen JH, Lakatos P (2003) Mechanisms of action of antiresorptive therapies of postmenopausal osteoporosis. Endocr Regul 37:225–238
30. Fontana A, Delmas PD (2003) Selective estrogen receptors modulators in the prevention and treatment of postmenopausal osteoporosis. Endocrinol Metab Clin North Am 32:219–232
31. Allen MR, Iwata K, Sato M, Burr DB (2006) Raloxifene enhances vertebral mechanical properties independent of bone density. Bone 39:1130–1135
32. Allen MR, Hogan HA, Hobbs WA, Koivuniemi AS, Koivuniemi MC, Burr DB (2007) Raloxifene enhances material-level mechanical properties of femoral cortical and trabecular bone. Endocrinology 148:3908–3913
33. Lees C, Shen V, Brommage R (2007) Effects of lasofoxifene on bone in surgically postmenopausal cynomolgus monkeys. Menopause 14:97–105
34. Vrablik M, Fait T, Kovar J, Poledne R, Ceska R (2008) Oral but not transdermal estrogen replacement therapy changes the composition of plasma lipoproteins. Metabolism 57:1088–1092
35. Clarkson TB, Anthony MS, Jerome CP (1998) Lack of effect of raloxifene on coronary artery atherosclerosis of postmenopausal monkeys. J Clin Endocrinol Metab 83:721–726
36. Christiansen C, Chesnut CH III, Adachi JD, Brown JP, Fernandes CE, Kung AW, Palacios S, Levine AB, Chines AA, Constantine GD (2010) Safety of bazedoxifene in a randomized, double-blind, placebo- and active-controlled Phase 3 study of postmenopausal women with osteoporosis. BMC Musculoskelet Disord 11:130
37. Pickar JH, MacNeil T, Ohleth K (2010) SERMs: progress and future perspectives. Maturitas 67:129–138
38. Pinkerton JV, Goldstein SR (2010) Endometrial safety: a key hurdle for selective estrogen receptor modulators in development. Menopause 17:642–653
39. Cummings SR, Eckert S, Krueger KA, Grady D, Powles TJ, Cauley JA, Norton L, Nickelsen T, Bjarnason NH, Morrow M, Lippman ME, Black D, Glusman JE, Costa A, Jordan VC (1999) The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. Multiple Outcomes of Raloxifene Evaluation. JAMA 281:2189–2197
40. Pinkerton JV, Archer DF, Utian WH, Menegoci JC, Levine AB, Chines AA, Constantine GD (2009) Bazedoxifene effects on the reproductive tract in postmenopausal women at risk for osteoporosis. Menopause 16:1102–1108
41. Archer DF, Pinkerton JV, Utian WH, Menegoci JC, de Villiers TJ, Yuen CK, Levine AB, Chines AA, Constantine GD (2009) Bazedoxifene, a selective estrogen receptor modulator: effects on the endometrium, ovaries, and breast from a randomized controlled trial in osteoporotic postmenopausal women. Menopause 16:1109–1115
42. Miller PD, Chines AA, Christiansen C, Hoeck HC, Kendler DL, Lewiecki EM, Woodson G, Levine AB, Constantine G, Delmas PD (2008) 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 23:525–535
43. Silverman SL, Christiansen C, Genant HK, Vukicevic S, Zanchetta JR, de Villiers TJ, Constantine GD, Chines AA (2008) 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 23:1923–1934