Bazedoxifene for the treatment of osteoporosis

References

• Osteoporosis prevention, diagnosis, and therapy NIH Consensus. Development Panel on Osteoporosis Prevention, Diagnosis, and Therapy. JAMA. 2001 Feb 14;285(6):785–795.
   Google Scholar
• Demontiero O, Vidal C, Duque G. Aging and bone loss: new insights for the clinician. Ther Adv Musculoskelet Dis. 2012. 4. Apr(2):61–76.
   Google Scholar
• Khosla S, Riggs BL. Pathophysiology of age-related bone loss and osteoporosis. Endocrinol Metab Clin North Am. 2005 Dec;34(4):1015–30, xi.
   PubMed Web of Science ®Google Scholar
• Khosla S, Atkinson EJ, Melton LJ 3rd, et al. Effects of age and estrogen status on serum parathyroid hormone levels and biochemical markers of bone turnover in women: a population-based study. J Clin Endocrinol Metab. 1997 May;82(5):1522–1527.
   PubMed Web of Science ®Google Scholar
• Wright NC, Looker AC, Saag KG, et al. The recent prevalence of osteoporosis and low bone mass in the United States based on bone mineral density at the femoral neck or lumbar spine. J Bone Miner Res. 2014 Nov;29(11):2520–2526.
   PubMed Web of Science ®Google Scholar
• Reginster JY, Burlet N. Osteoporosis: a still increasing prevalence. Bone. 2006 Feb;38(2 Suppl 1):S4–S9.
   PubMed Web of Science ®Google Scholar
• Watts NB, Bilezikian JP, Camacho PM, et al. american association of clinical endocrinologists medical guidelines for clinical practice for the diagnosis and treatment of postmenopausal osteoporosis. Endocr Pract. 2010;16(Suppl 3):1–37. Nov-Dec
   PubMedGoogle Scholar
• Dm B, Nk A, Palermo L, et al. Prevalent vertebral deformities predict hip fractures and new vertebral deformities but not wrist fractures. Study of Osteoporotic fractures research group. J Bone Miner Res. 1999 May;14(5):821–828.
   PubMed Web of Science ®Google Scholar
• Melton LJ 3rd, Atkinson EJ, Cooper C, et al. Vertebral fractures predict subsequent fractures. Osteoporos Int. 1999;10(3):214–221.
   PubMed Web of Science ®Google Scholar
• Ross PD, Davis JW, Epstein RS, et al. Pre-existing fractures and bone mass predict vertebral fracture incidence in women. Ann Intern Med. 1991 Jun 1;114(11):919–923.
   PubMed Web of Science ®Google Scholar
• Kendler DL, Bauer DC, Davison KS, et al. Vertebral fractures: clinical importance and management. Am J Med. 2016 Feb;129(2):221e1–10.
   Web of Science ®Google Scholar
• Cooper C, Campion G, Melton LJ 3rd. Hip fractures in the elderly: a world-wide projection. Osteoporos Int. 1992 Nov;2(6):285–289.
   PubMed Web of Science ®Google Scholar
• Svedbom A, Hernlund E, Ivergard M, et al. Osteoporosis in the European Union: a compendium of country-specific reports. Arch Osteoporos. 2013;8:137.
   PubMed Web of Science ®Google Scholar
• Briot K. Fracture Liaison services. Curr Opin Rheumatol. 2017 Jul;29(4):416–421.
   PubMed Web of Science ®Google Scholar
• Makras P, Panagoulia M, Mari A, et al. Evaluation of the first fracture liaison service in the Greek healthcare setting. Arch Osteoporos. 2017;Dec;12(1):3.
   PubMed Web of Science ®Google Scholar
• Kanis JA, McCloskey EV, Johansson H, et al. European guidance for the diagnosis and management of osteoporosis in postmenopausal women. Osteoporos Int. 2013 Jan;24(1):23–57.
   PubMed Web of Science ®Google Scholar
• Maximov PY, Lee TM, Jordan VC. The discovery and development of selective estrogen receptor modulators (SERMs) for clinical practice. Curr Clin Pharmacol. 2013 May;8(2):135–155.
   PubMedGoogle Scholar
• Papapoulos S, Makras P. Selection of antiresorptive or anabolic treatments for postmenopausal osteoporosis. Nat Clin Pract Endocrinol Metab. 2008 Sep;4(9):514–523.
   PubMedGoogle Scholar
• Makras P, Vaiopoulos G, Lyritis GP. Greek National Medicine A. 2011 guidelines for the diagnosis and treatment of osteoporosis in Greece. J Musculoskelet Neuronal Interact. 2012 Mar;12(1):38–42.
   PubMed Web of Science ®Google Scholar
• Shirley M. Abaloparatide: first global approval. Drugs. 2017 Aug;77(12):1363–1368.
   PubMed Web of Science ®Google Scholar
• Kulak Junior J, Kulak CA, Taylor HS. SERMs in the prevention and treatment of postmenopausal osteoporosis: an update. Arq Bras Endocrinol Metabol. 2010 Mar;54(2):200–205.
   PubMedGoogle Scholar
• Hollick RJ, Reid DM. Role of bisphosphonates in the management of postmenopausal osteoporosis: an update on recent safety anxieties. Menopause Int. 2011 Jun;17(2):66–72.
   PubMedGoogle Scholar
• Kamel HK. Update on osteoporosis management in long-term care: focus on bisphosphonates. J Am Med Dir Assoc. 2007 Sep;8(7):434–440.
   PubMed Web of Science ®Google Scholar
• Makras P, Hamdy NA, Zwinderman AH, et al. Bisphosphonate dose and incidence of fractures in postmenopausal osteoporosis. Bone. 2009 May;44(5):766–771.
   PubMed Web of Science ®Google Scholar
• Rizzoli R, Burlet N, Cahall D, et al. Osteonecrosis of the jaw and bisphosphonate treatment for osteoporosis. Bone. 2008 May;42(5):841–847.
   PubMed Web of Science ®Google Scholar
• Khosla S, Burr D, Cauley J, et al. Bisphosphonate-associated osteonecrosis of the jaw: report of a task force of the American society for bone and mineral research. J Bone Miner Res. 2007 Oct;22(10):1479–1491.
   PubMed Web of Science ®Google Scholar
• Shane E, Burr D, Abrahamsen B, et al. Atypical subtrochanteric and diaphyseal femoral fractures: second report of a task force of the American society for bone and mineral research. J Bone Miner Res. 2014 Jan;29(1):1–23.
   PubMed Web of Science ®Google Scholar
• Shane E, Burr D, Ebeling PR, et al. Atypical subtrochanteric and diaphyseal femoral fractures: report of a task force of the American society for bone and mineral research. J Bone Miner Res. 2010 Nov;25(11):2267–2294.
   PubMed Web of Science ®Google Scholar
• Whitaker M, Guo J, Kehoe T, et al. Bisphosphonates for osteoporosis–where do we go from here? N Engl J Med. 2012 May 31;366(22):2048–2051.
   PubMed Web of Science ®Google Scholar
• Kim DH, Rogers JR, Fulchino LA, et al. Bisphosphonates and risk of cardiovascular events: a meta-analysis. PLoS One. 2015;10(4):e0122646.
   PubMed Web of Science ®Google Scholar
• Anastasilakis AD, Toulis KA, Polyzos SA, et al. Long-term treatment of osteoporosis: safety and efficacy appraisal of denosumab. Ther Clin Risk Manag. 2012;8:295–306.
   PubMed Web of Science ®Google Scholar
• Anastasilakis AD, Polyzos SA, Makras P. THERAPY OF ENDOCRINE DISEASE: denosumab vs bisphosphonates for the treatment of postmenopausal osteoporosis. Eur J Endocrinol. 2018 Jul;179(1):R31–R45.
   PubMed Web of Science ®Google Scholar
• Bone HG, Bolognese MA, Yuen CK, et al. Effects of denosumab treatment and discontinuation on bone mineral density and bone turnover markers in postmenopausal women with low bone mass. J Clin Endocrinol Metab. 2011 Apr;96(4):972–980.
   PubMed Web of Science ®Google Scholar
• 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 Apr;23(4):525–535.
   PubMed Web of Science ®Google Scholar
• Anastasilakis AD, Polyzos SA, Makras P, et al. Clinical Features of 24 patients with rebound-associated vertebral fractures after denosumab discontinuation: systematic review and additional cases. J Bone Miner Res. 2017 Jun;32(6):1291–1296.
   PubMed Web of Science ®Google Scholar
• Cummings SR, Ferrari S, Eastell R, et al. Vertebral fractures after discontinuation of Denosumab: A Post Hoc Analysis of the randomized placebo-controlled FREEDOM trial and its extension. J Bone Miner Res. 2018 Feb;33(2):190–198.
   PubMed Web of Science ®Google Scholar
• Anastasilakis AD, Yavropoulou MP, Makras P, et al. Increased osteoclastogenesis in patients with vertebral fractures following discontinuation of denosumab treatment. Eur J Endocrinol. 2017 Jun;176(6):677–683.
   PubMed Web of Science ®Google Scholar
• Tsourdi E, Langdahl B, Cohen-Solal M, et al. Discontinuation of Denosumab therapy for osteoporosis: A systematic review and position statement by ECTS. Bone. 2017;105:11–17.
   PubMed Web of Science ®Google Scholar
• Eastell R, Nickelsen T, Marin F, et al. Sequential treatment of severe postmenopausal osteoporosis after teriparatide: final results of the randomized, controlled European Study of Forsteo (EUROFORS). J Bone Miner Res. 2009 Apr;24(4):726–736.
   PubMed Web of Science ®Google Scholar
• Leder BZ, Neer RM, Wyland JJ, et al. Effects of teriparatide treatment and discontinuation in postmenopausal women and eugonadal men with osteoporosis. J Clin Endocrinol Metab. 2009 Aug;94(8):2915–2921.
   PubMed Web of Science ®Google Scholar
• Rossouw JE, Anderson GL, Prentice RL, et al. Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the women’s Health Initiative randomized controlled trial. Jama. 2002 Jul 17;288(3):321–333.
   PubMed Web of Science ®Google Scholar
• 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 Aug 18;282(7):637–645.
   PubMed Web of Science ®Google Scholar
• Delmas PD, Ensrud KE, Adachi JD, et al. 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 Aug;87(8):3609–3617.
   PubMed Web of Science ®Google Scholar
• 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 Jun;105(6):1397–1404.
   PubMed Web of Science ®Google Scholar
• 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 Dec;23(12):1923–1934.
   PubMed Web of Science ®Google Scholar
• Silverman SL, Chines AA, Kendler DL, et al. Sustained efficacy and safety of bazedoxifene in preventing fractures in postmenopausal women with osteoporosis: results of a 5-year, randomized, placebo-controlled study. Osteoporos Int. 2012 Jan;23(1):351–363.
   PubMed Web of Science ®Google Scholar
• Darba J, Perez-Alvarez N, Kaskens L, et al. Cost-effectiveness of bazedoxifene versus raloxifene in the treatment of postmenopausal women in Spain. Clinicoecon Outcomes Res. 2013;5:327–336.
   PubMedGoogle Scholar
• Robinson SP, Koch R, Jordan VC. In vitro estrogenic actions in rat and human cells of hydroxylated derivatives of D16726 (zindoxifene), an agent with known antimammary cancer activity in vivo. Cancer Res. 1988 Feb 15; 48(4):784–787.
   PubMed Web of Science ®Google Scholar
• Komm BS, Kharode YP, Bodine PV, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology. 2005 Sep;146(9):3999–4008.
   PubMed Web of Science ®Google Scholar
• Miller CP, Collini MD, Tran BD, et al. Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. J Med Chem. 2001 May 24;44(11):1654–1657.
   PubMed Web of Science ®Google Scholar
• 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 Dec;949:317–326.
   PubMed Web of Science ®Google Scholar
• Kung AW, Chu EY, Xu L. Bazedoxifene: a new selective estrogen receptor modulator for the treatment of postmenopausal osteoporosis. Expert Opin Pharmacother. 2009 Jun;10(8):1377–1385.
   PubMed Web of Science ®Google Scholar
• Peano BJ, Crabtree JS, Komm BS, et al. Effects of various selective estrogen receptor modulators with or without conjugated estrogens on mouse mammary gland. Endocrinology. 2009 Apr;150(4):1897–1903.
   PubMed Web of Science ®Google Scholar
• Chandrasekaran A, McKeand WE, Sullivan P, et al. Metabolic disposition of [14C]bazedoxifene in healthy postmenopausal women. Drug Metab Dispos. 2009 Jun;37(6):1219–1225.
   PubMed Web of Science ®Google Scholar
• Shen L, Ahmad S, Park S, et al. In vitro metabolism, permeability, and efflux of bazedoxifene in humans. Drug Metab Dispos. 2010 Sep;38(9):1471–1479.
   PubMed Web of Science ®Google Scholar
• Pharmacokinetics MW, Proportionality D. Bioavailability of Bazedoxifene in healthy postmenopausal women. Clin Ther. 2017 Sep;39(9):1769–1779.
   PubMed Web of Science ®Google Scholar
• McKeand WE, Orczyk GP, Ermer JC, et al. A double-blind, randomized, ascending, multiple-dose study of bazedoxifene in healthy postmenopausal women. Clin Pharmacol Drug Dev. 2014 Jul;3(4):262–269.
   PubMed Web of Science ®Google Scholar
• Morello KC, Wurz GT, DeGregorio MW. Pharmacokinetics of selective estrogen receptor modulators. Clin Pharmacokinet. 2003;42(4):361–372.
   PubMed Web of Science ®Google Scholar
• McKeand W, Baird-Bellaire S, Ermer J, et al. Safety of Bazedoxifene in hepatically impaired and healthy postmenopausal women. Clin Pharmacol Drug Dev. 2018 May;7(4):365–372.
   PubMed Web of Science ®Google Scholar
• McKeand W, Ermer J, Korth-Bradley J. Assessment of the effects of age and renal function on Pharmacokinetics of Bazedoxifene in postmenopausal women. Clin Pharmacol Drug Dev. 2018 Nov;7(8):920–926.
   PubMed Web of Science ®Google Scholar
• Bachmann G, Crosby U, Feldman RA, et al. Effects of bazedoxifene in nonflushing postmenopausal women: a randomized phase 2 trial. Menopause. 2011 May;18(5):508–514.
   PubMed Web of Science ®Google Scholar
• Palacios S, Silverman SL, de Villiers TJ, et al. A 7-year randomized, placebo-controlled trial assessing the long-term efficacy and safety of bazedoxifene in postmenopausal women with osteoporosis: effects on bone density and fracture. Menopause. 2015 Aug;22(8):806–813.
   PubMed Web of Science ®Google Scholar
• Peng L, Luo Q, Lu H. Efficacy and safety of bazedoxifene in postmenopausal women with osteoporosis: A systematic review and meta-analysis. Medicine (Baltimore). 2017 Dec;96(49):e8659.
   PubMed Web of Science ®Google Scholar
• Christiansen C, Chesnut CH 3rd, Adachi JD, 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 Jun 22;11:130.
   PubMed Web of Science ®Google Scholar
• 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 Nov-Dec;16(6):1109–1115.
   PubMed Web of Science ®Google Scholar
• de Villiers TJ, Chines AA, 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 Feb;22(2):567–576.
   PubMed Web of Science ®Google Scholar
• 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 Dec 1;96(23):1751–1761.
   PubMedGoogle Scholar
• Martino S, Disch D, Dowsett SA, et al. Safety assessment of raloxifene over eight years in a clinical trial setting. Curr Med Res Opin. 2005 Sep;21(9):1441–1452.
   PubMed Web of Science ®Google Scholar
• Cummings SR, Ensrud K, Delmas PD, et al. Lasofoxifene in postmenopausal women with osteoporosis. N Engl J Med. 2010 Feb 25;362(8):686–696.
   PubMed Web of Science ®Google Scholar
• 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 Sep 16;90(18):1371–1388.
   PubMed Web of Science ®Google Scholar
• Kaufman JM, Palacios S, Silverman S, et al. An evaluation of the Fracture Risk Assessment Tool (FRAX(R)) as an indicator of treatment efficacy: the effects of bazedoxifene and raloxifene on vertebral, nonvertebral, and all clinical fractures as a function of baseline fracture risk assessed by FRAX(R). Osteoporos Int. 2013 Oct;24(10):2561–2569.
   PubMed Web of Science ®Google Scholar
• Pickar JH, Yeh IT, Bachmann G, et al. Endometrial effects of a tissue selective estrogen complex containing bazedoxifene/conjugated estrogens as a menopausal therapy. Fertil Steril. 2009 Sep;92(3):1018–1024.
   PubMed Web of Science ®Google Scholar
• Pinkerton JV, Abraham L, Bushmakin AG, et al. Evaluation of the efficacy and safety of bazedoxifene/conjugated estrogens for secondary outcomes including vasomotor symptoms in postmenopausal women by years since menopause in the Selective estrogens, Menopause and Response to Therapy (SMART) trials. J Womens Health (Larchmt). 2014 Jan;23(1):18–28.
   PubMed Web of Science ®Google Scholar
• Mirkin S, Komm BS, Pan K, et al. Effects of bazedoxifene/conjugated estrogens on endometrial safety and bone in postmenopausal women. Climacteric. 2013 Jun;16(3):338–346.
   PubMed Web of Science ®Google Scholar
• Kagan R, Williams RS, Pan K, et al. A randomized, placebo- and active-controlled trial of bazedoxifene/conjugated estrogens for treatment of moderate to severe vulvar/vaginal atrophy in postmenopausal women. Menopause. 2010 Mar;17(2):281–289.
   PubMed Web of Science ®Google Scholar
• Pinkerton JV, Harvey JA, Pan K, et al. Breast effects of bazedoxifene-conjugated estrogens: a randomized controlled trial. Obstet Gynecol. 2013 May;121(5):959–968.
   PubMed Web of Science ®Google Scholar
• Pinkerton JV, Harvey JA, Lindsay R, et al. Effects of bazedoxifene/conjugated estrogens on the endometrium and bone: a randomized trial. J Clin Endocrinol Metab. 2014 Feb;99(2):E189–E98.
   PubMed Web of Science ®Google Scholar
• Pinkerton JV, Archer DF, Utian WH, et al. Bazedoxifene effects on the reproductive tract in postmenopausal women at risk for osteoporosis. Menopause. 2009 Nov-Dec;16(6):1102–1108.
   PubMed Web of Science ®Google Scholar
• Goldberg T, Fidler B. Conjugated Estrogens/Bazedoxifene (Duavee): A novel agent for the treatment of moderate-to-severe vasomotor symptoms associated with menopause and the prevention of postmenopausal Osteoporosis. P T. 2015 Mar;40(3):178–182.
   PubMedGoogle Scholar
• Beck TJ, Fuerst T, Gaither KW, et al. The effects of bazedoxifene on bone structural strength evaluated by hip structure analysis. Bone. 2015;77:115–119.
   PubMed Web of Science ®Google Scholar
• Ott SM, Oleksik A, Lu Y, et al. Bone histomorphometric and biochemical marker results of a 2-year placebo-controlled trial of raloxifene in postmenopausal women. J Bone Miner Res. 2002 Feb;17(2):341–348.
   PubMed Web of Science ®Google Scholar
• Ellis AG, Reginster JY, Luo X, et al. Indirect comparison of bazedoxifene vs oral bisphosphonates for the prevention of vertebral fractures in postmenopausal osteoporotic women. Curr Med Res Opin. 2014 Aug;30(8):1617–1626.
   PubMed Web of Science ®Google Scholar
• Ellis AG, Reginster JY, Luo X, et al. Bazedoxifene versus oral bisphosphonates for the prevention of nonvertebral fractures in postmenopausal women with osteoporosis at higher risk of fracture: a network meta-analysis. Value Health. 2014 Jun;17(4):424–432.
   PubMed Web of Science ®Google Scholar
• Palacios S, Williams R, Mirkin S, et al. Efficacy and tolerability of bazedoxifene in Mexican women with osteoporosis: a subgroup analysis of a randomized phase 3 trial. Menopause. 2016 Jul;23(7):771–777.
   PubMed Web of Science ®Google Scholar
• Bueno JAH, Arias L, Yu CR, et al. Efficacy and safety of bazedoxifene in postmenopausal Latino women with osteoporosis. Menopause. 2017 Sep;24(9):1033–1039.
   PubMed Web of Science ®Google Scholar
• Xu L, Tsai KS, Kim GS, et al. Efficacy and safety of bazedoxifene in postmenopausal Asian women. Osteoporos Int. 2011 Feb;22(2):559–565.
   PubMed Web of Science ®Google Scholar
• Itabashi A, Yoh K, Chines AA, et al. Effects of bazedoxifene on bone mineral density, bone turnover, and safety in postmenopausal Japanese women with osteoporosis. J Bone Miner Res. 2011 Mar;26(3):519–529.
   PubMed Web of Science ®Google Scholar
• Adami S, San Martin J, Munoz-Torres M, et al. Effect of raloxifene after recombinant teriparatide [hPTH(1-34)] treatment in postmenopausal women with osteoporosis. Osteoporos Int. 2008 Jan;19(1):87–94.
   PubMed Web of Science ®Google Scholar