Bazedoxifene acetate for the management of postmenopausal osteoporosis

Drugs of Today

Volumn 47, Issue 3, 2011, Pages 187-195

  Palacios, Santiago ^a  

^a Palacios Institute of Women's Health   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

BAZEDOXIFENE; CALCIUM; CONJUGATED ESTROGEN; ESTROGEN; ESTROGEN DERIVATIVE; GESTAGEN; LASOFOXIFENE; PLACEBO; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN; TISSUE SELECTIVE ESTROGEN COMPLEX; UNCLASSIFIED DRUG; VITAMIN D; BONE DENSITY CONSERVATION AGENT; INDOLE DERIVATIVE;

BONE DENSITY; BONE MASS; BREAST CANCER; BREAST CARCINOMA; BREAST METASTASIS; DRUG ACTIVITY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; DRUG STRUCTURE; ENDOMETRIUM CARCINOMA; ENDOMETRIUM HYPERPLASIA; HIGH RISK POPULATION; HORMONAL THERAPY; HOT FLUSH; HUMAN; INCIDENCE; LEG CRAMP; NONHUMAN; OSTEOLYSIS; OSTEOPOROSIS; POSTMENOPAUSE OSTEOPOROSIS; REVIEW; SINGLE DRUG DOSE; UNSPECIFIED SIDE EFFECT; UTERUS BLEEDING; VAGINA ATROPHY; VAGINA BLEEDING; VENOUS THROMBOEMBOLISM; VERTEBRA FRACTURE; CLINICAL TRIAL (TOPIC); FEMALE; MIDDLE AGED;

BONE DENSITY CONSERVATION AGENTS; CLINICAL TRIALS AS TOPIC; FEMALE; HUMANS; INDOLES; MIDDLE AGED; OSTEOPOROSIS, POSTMENOPAUSAL; SELECTIVE ESTROGEN RECEPTOR MODULATORS;

EID: 80051919031     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.2011.47.3.1587026     Document Type: Review

References (37)

1. Kanis, J.A., Johnell, O. Requirements for DXA for the management of osteoporosis in Europe. Osteoporos Int 2005, 16(3): 229-38.
2. Albright, F., Bloomberg, F., Smith, P.H. Postmenopausal osteoporosis. Trans Assoc Am Phys 1940, 55: 298-305.
3. Palacios, S., Sanchez-Borrego, R., Forteza, A. The importance of preventive health care in post-menopausal women. Maturitas 2005, 52(Suppl. 1): S53-60.
4. Harvey, N., Dennison, E., Cooper, C. Osteoporosis: impact on health and economics. Nat Rev Rheumatol 2010, 6(2):99-105.
5. Palacios, S. El ginecólogo en el tratamiento de la osteoporosis. In: Guia Practica de la Osteoporosis en Ginecología. Elsevier: Barcelona 2010, 183-93.
6. Tosteson, A.N., Grove, M.R., Hammond, C.S. et al. Early discontinuation of treatment for osteoporosis. Am J Med 2003, 115(3): 209-16.
7. McCombs, J.S., Thiebaud, P., McLaughlin-Miley, C., Shi, J. Compliance with drug therapies for the treatment and prevention of osteoporosis. Maturitas 2004, 48(3): 271-87.
8. Palacios, S. The future of the new selective estrogen receptor modulators. Menopause Int 2007, 13(1): 27-34.
9. Riggs, B.L., Hartmann, L.C. Selective estrogen-receptor modulators-mechanisms of action and application to clinical practice. N Engl J Med 2003, 348(7): 618-29.
10. Palacios, S. Third generation SERMs: Anything new? Maturitas 2010, 67(2): 101-2.
11. European Public Assessment Report (EPAR): Conbriza. EPAR summary for the public. May 26, 2009. Available at http://www.ema.europa.eu/docs/en-GB/document- library/EPAR---Summary-for-the-public/human/000913/WC500033574.pdf. Accessed March 25, 2011.
12. Committee for Medicinal Produtcs for Human Use. Summary of positive opinion for Fablyn. December 18, 2008. Available at http://www.ema.europa.eu/ docs/en-GB/document-library/Summary-of-opinion---Initial-authorisation/human/ 000977/WC500059847.pdf. Accessed March 25, 2011.
13. Stovall, D.W. Aprela, a single tablet formulation of bazedoxifene and conjugated equine estrogens (Premarin) for the potential treatment of menopausal symptoms. Curr Opin Investig Drugs 2010, 11(4): 464-71.
14. Chang, K.C., Wang, Y., Bodine, P.V., Nagpal, S., Komm, B.S. Gene expression profiling studies of three SERMs and their conjugated estrogen combinations in human breast cancer cells: insights into the unique antagonistic effects of bazedoxifene on conjugated estrogens. J Steroid Biochem Mol Biol 2010, 118(1-2): 117-24.
15. Pinkerton, J.V., Utian, W.H., Constantine, G.D., Olivier, S., Pickar, J.H. Relief of vasomotor symptoms with the tissue-selective estrogen complex containing bazedoxifene/conjugated estrogens: a randomized, controlled trial. Menopause 2009, 16(6): 1116-24.
16. Archer, D.F., Lewis, V., Carr, B.R., Olivier, S., Pickar, J.H. Bazedoxifene/conjugated estrogens (BZA/CE): incidence of uterine bleeding in postmenopausal women. Fertil Steril 2009, 92(3): 1039-44.
17. Lindsay, R., Gallagher, J.C., Kagan, R., Pickar, J.H., Constantine, G. Efficacy of tissue-selective estrogen complex of bazedoxifene/conjugated estrogens for osteoporosis prevention in at-risk postmenopausal women. Fertil Steril 2009, 92(3): 1045-52.
18. Miller, C.P., Collini, M.D., Tran, B.D. et al. Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. J Med Chem 2001, 44(11): 1654-7.
19. Komm, B.S., Kharode, Y.P., Bodine, P.V., Harris, H.A., Miller, C.P., Lyttle, C.R. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology 2005, 146(9): 3999-4008.
20. Peano, B.J., Crabtree, J.S., Komm, B.S., Winneker, R.C., Harris, H.A. Effects of various selective estrogen receptor modulators with or without conjugated estrogens on mouse mammary gland. Endocrinology 2009, 150(4): 1897-903.
21. Ermer, J., McKeand, W., Sullivan, P., Parker, V., Orczyk, G. Bazedoxifene acetate dose proportionality in healthy, postmenopausal women. Clin Pharmacol Ther Clin Pharmacol Ther [Annu Meet Am Soc Clin Pharmacol Ther (ASCPT) (April 2-5, Washington, D.C.) 2003] 2003, 73(2): Abst PII-66.
22. Chandrasekaran, A., McKeand, W.E., Sullivan, P., DeMaio, W., Stoltz, R., Scatina, J. Metabolic disposition of [14C]bazedoxifene in healthy postmenopausal women. Drug Metab Dispos 2009, 37(6): 1219-25.
23. Ronkin, S., Clarke, L., Boudes, P., Constantine, G. TSE-424, a novel selective estrogen, reduces biochemical indices of bone metabolism in a dose related fashion. J Bone Miner Res [23rd Annu Meet Am Soc Bone Miner Res (ASBMR) (Oct 12-16, Phoenix) 2001] 2001, 16(Suppl. 1): Abst SU437.
24. Ronkin, S., Northington, R., Baracat, E., Nunes, M.G., Archer, D.F., Constantine, G., Pickar, J.H. Endometrial effects of bazedoxifene acetate, a novel selective estrogen receptor modulator, in postmenopausal women. Obstet Gynecol 2005, 105(6): 1397-404.
25. Miller, P.D., Chines, A.A., 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(4):525-35.
26. Silverman, S.L., Christiansen, C., Genant, H.K. 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(12): 1923-34.
27. Kanis, J.A., Johansson, H., Oden, A., McCloskey, E.V. Bazedoxifene reduces vertebral and clinical fractures in postmenopausal women at high risk assessed with FRAX. Bone 2009, 44(6): 1049-54.
28. Kanis, J.A. on behalf of the World Health Organization Scientific Group. Assessment of Osteoporosis at the Primary Health Care Level. World Health Organization Collaborating Centre for Metabolic Bone Diseases, University of Sheffield, UK. 2008 Technical report.
29. Kanis, J.A., 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(4): 385-97.
30. 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 [31st Annu Meet Am Soc Bone Miner Res (ASBMR) (Sept 11-15, Denver) 2009] 2009, 24(Suppl. 1): Abst FR0376.
31. Chines, A.A., Zanchetta, J.R., Genant, H.K., Kendler, D.L. et al. Sustained efficacy of bazedoxifene in preventing fractures in postmenopausal women with osteoporosis: Results of a 5-year, randomized, placebo-controlled study. Osteoporos Int [IOF WCO & ECCEO 10 (May 5-8, Florence) 2010] 2010, 21(Suppl. 1): Abst OC17.
32. Christiansen, C., Chesnut, C.H.III, Adachi, J.D. et al. Safety of bazedoxifene in a randomized, double-blind, placebo- and active-controlled phase 3 study of postmenopausal women with osteoporosis. BMC Musculoskelet Disord 2010, 11: 130-40.
33. De Villiers, T.J., Chines, A.A., Palacios, S. et al. Safety and tolerability of bazedoxifene in postmenopausal women with osteoporosis: results of a 5-year, randomized, placebo-controlled phase 3 trial. Osteoporos Int 2011, 22(2): 567-76.
34. 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(3): 197-213.
35. Position Statement: Management of osteoporosis in postmenopausal women: 2010 position statement of The North American Menopause Society. Menopause 2010, 17(1): 25-54.
36. Palacios, S. Efficacy and safety of bazedoxifene, a novel selective estrogen receptor modulator for the prevention and treatment of postmenopausal osteoporosis. Curr Med Res Opin 2010, 26(7): 1553-63.
37. Borgström, F., Ström, O., Kleman, M., McCloskey, E., Johansson, H., Odén, A., Kanis, J.A. Cost-effectiveness of bazedoxifene incorporating the FRAX(R) algorithm in a European perspective. Osteoporos Int 2011, 22(3): 955-65.