Selective estrogen receptor modulators in clinical practice: a safety overview

Bibliography

• Riggs BL, Hartmann LC. Selective estrogen-receptor modulators – mechanisms of action and application to clinical practice. N Engl J Med 2003;348:618-29
   PubMed Web of Science ®Google Scholar
• Jordan VC, Collins MM, Rowsby L, Prestwich G. A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. J Endocrinol 1977;75:305-16
   PubMed Web of Science ®Google Scholar
• Osborne CK, Boldt DH, Clark GM, Trent JM. Effects of tamoxifen on human breast cancer cell cycle kinetics: accumulation of cells in early G1 phase. Cancer Res 1983;43:3583-5
   PubMed Web of Science ®Google Scholar
• Nolvadex [package insert]. AstraZeneca Pharmaceuticals LP; Wilmington, DE: 2007
   Google Scholar
• Fisher B, Costantino JP, Redmond CK, et al. 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;86:527-37
   PubMed Web of Science ®Google Scholar
• 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;281:2189-97
   PubMed Web of Science ®Google Scholar
• 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;337:1641-7
   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;282:637-45
   PubMed Web of Science ®Google Scholar
• Evista [package insert]. Eli Lilly and Co; Indianapolis, IN: 2011
   Google Scholar
• Harvey HA, Kimura M, Hajba A. Toremifene: an evaluation of its safety profile. Breast 2006;15:142-57
   PubMed Web of Science ®Google Scholar
• Michael H, Harkonen PL, Kangas L, et al. Differential effects of selective oestrogen receptor modulators (SERMs) tamoxifen, ospemifene and raloxifene on human osteoclasts in vitro. Br J Pharmacol 2007;151:384-95
   PubMed Web of Science ®Google Scholar
• Brzozowski AM, Pike AC, Dauter Z, et al. Molecular basis of agonism and antagonism in the oestrogen receptor. Nature 1997;389:753-8
   PubMed Web of Science ®Google Scholar
• Karlsson S, Iatropoulos MJ, Williams GM, et al. The proliferation in uterine compartments of intact rats of two different strains exposed to high doses of tamoxifen or toremifene. Toxicol Pathol 1998;26:759-68
   PubMed Web of Science ®Google Scholar
• Chatterjee M, Harris AL. Enhancement of Adriamycin cytotoxicity in a multidrug resistant Chinese hamster ovary (CHO) subline, CHO-Adrr, by toremifene and its modulation by alpha 1 acid glycoprotein. Eur J Cancer 1990;26:432-6
   PubMed Web of Science ®Google Scholar
• Fareston [package insert]. ProStrakan Inc; Bridgewater, NJ: 2012
   Google Scholar
• Komm BS, Kharode YP, Bodine PV, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology 2005;146:3999-4008
   PubMed Web of Science ®Google Scholar
• Lewis-Wambi JS, Kim H, Curpan R, et al. The selective estrogen receptor modulator bazedoxifene inhibits hormone-independent breast cancer cell growth and down-regulates estrogen receptor alpha and cyclin D1. Mol Pharmacol 2011;80:610-20
   PubMed Web of Science ®Google Scholar
• Rosati RL, Da Silva JP, Cameron KO, et al. Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene. J Med Chem 1998;41:2928-31
   PubMed Web of Science ®Google Scholar
• European Medicines Agency. Assessment report for fablyn. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/000977/WC500020096.pdf [Last accessed 23 January 2014]
   Google Scholar
• Qu Q, Zheng H, Dahllund J, et al. Selective estrogenic effects of a novel triphenylethylene compound, FC1271a, on bone, cholesterol level, and reproductive tissues in intact and ovariectomized rats. Endocrinology 2000;141:809-20
   PubMed Web of Science ®Google Scholar
• Osphena [package insert]. Shionogi Inc; Florham Park, NJ: 2013
   Google Scholar
• European Medicines Agency. CHMP summary of positive opinion for senshio. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/Summary_of_opinion_-_Initial_authorisation/human/002780/WC500177633.pdf [Last accessed 15 January 2015]
   Google Scholar
• Howell A, Osborne CK, Morris C, Wakeling AE. ICI 182,780 (Faslodex): development of a novel, "pure" antiestrogen. Cancer 2000;89:817-25
   PubMed Web of Science ®Google Scholar
• Dauvois S, White R, Parker MG. The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling. J Cell Sci 1993;106(Pt 4):1377-88
   PubMed Web of Science ®Google Scholar
• Wardell SE, Marks JR, McDonnell DP. The turnover of estrogen receptor alpha by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy. Biochem Pharmacol 2011;82:122-30
   PubMed Web of Science ®Google Scholar
• European Medicines Agency. Summary of product characteristics: faslodex. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000540/WC500021174.pdf [Last accessed 23 January 2014]
   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;90:1371-88
   PubMed Web of Science ®Google Scholar
• Cuzick J, Forbes J, Edwards R, et al. First results from the International Breast Cancer Intervention Study (IBIS-I): a randomised prevention trial. Lancet 2002;360:817-24
   PubMed Web of Science ®Google Scholar
• Barrett-Connor E, Mosca L, Collins P, et al. Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women. N Engl J Med 2006;355:125-37
   PubMed Web of Science ®Google Scholar
• Christiansen C, Chesnut CHIII, 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;11:130
   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;22:567-76
   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;23:525-35
   PubMed Web of Science ®Google Scholar
• LaCroix AZ, Powles T, Osborne CK, et al. Breast cancer incidence in the randomized PEARL trial of lasofoxifene in postmenopausal osteoporotic women. J Natl Cancer Inst 2010;102:1706-15
   PubMed Web of Science ®Google Scholar
• Simon JA, Lin VH, Radovich C, Bachmann GA. One-year long-term safety extension study of ospemifene for the treatment of vulvar and vaginal atrophy in postmenopausal women with a uterus. Menopause 2013;20:418-27
   PubMed Web of Science ®Google Scholar
• Portman DJ, Bachmann GA, Simon JA. Ospemifene, a novel selective estrogen receptor modulator for treating dyspareunia associated with postmenopausal vulvar and vaginal atrophy. Menopause 2013;20:623-30
   PubMed Web of Science ®Google 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;21:1441-52
   PubMed Web of Science ®Google Scholar
• Pyrhonen S, Valavaara R, Modig H, et al. Comparison of toremifene and tamoxifen in post-menopausal patients with advanced breast cancer: a randomized double-blind, the ’nordic’ phase III study. Br J Cancer 1997;76:270-7
   PubMed Web of Science ®Google Scholar
• Gershanovich M, Garin A, Baltina D, et al. A phase III comparison of two toremifene doses to tamoxifen in postmenopausal women with advanced breast cancer. Eastern European Study Group. Breast Cancer Res Treat 1997;45:251-62
   PubMed Web of Science ®Google Scholar
• Hayes DF, Van Zyl JA, Hacking A, et al. Randomized comparison of tamoxifen and two separate doses of toremifene in postmenopausal patients with metastatic breast cancer. J Clin Oncol 1995;13:2556-66
   PubMed Web of Science ®Google Scholar
• Pagani O, Gelber S, Price K, et al. Toremifene and tamoxifen are equally effective for early-stage breast cancer: first results of International Breast Cancer Study Group Trials 12-93 and 14-93. Ann Oncol 2004;15:1749-59
   PubMed Web of Science ®Google Scholar
• Palacios S, de Villiers TJ, Nardone FC, et al. Assessment of the safety of long-term bazedoxifene treatment on the reproductive tract in postmenopausal women with osteoporosis: results of a 7-year, randomized, placebo-controlled, phase 3 study. Maturitas 2013;76:81-7
   PubMed Web of Science ®Google Scholar
• Bachmann GA, Komi JO. Ospemifene effectively treats vulvovaginal atrophy in postmenopausal women: results from a pivotal phase 3 study. Menopause 2010;17:480-6
   PubMed Web of Science ®Google Scholar
• Morales L, Neven P, Timmerman D, et al. Prospective assessment of the endometrium in postmenopausal breast cancer patients treated with fulvestrant. Breast Cancer Res Treat 2009;117:77-81
   PubMed Web of Science ®Google Scholar
• Soltamox [package insert]. Savient Pharmaceuticals, Inc; East Brunswick, NJ: 2005
   Google Scholar
• Cuzick J, Forbes JF, Sestak I, et al. Long-term results of tamoxifen prophylaxis for breast cancer – 96-month follow-up of the randomized IBIS-I trial. J Natl Cancer Inst 2007;99:272-82
   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;96:1751-61
   PubMed Web of Science ®Google Scholar
• Vogel VG, Costantino JP, Wickerham DL, et al. 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;295:2727-41
   PubMed Web of Science ®Google Scholar
• Chi F, Wu R, Zeng Y, et al. Effects of toremifene versus tamoxifen on breast cancer patients: a meta-analysis. Breast Cancer 2013;20:111-22
   PubMed Web of Science ®Google Scholar
• Vogel CL, Johnston MA, Capers C, Braccia D. Toremifene for breast cancer: a review of 20 years of data. Clin Breast Cancer 2014;14:1-9
   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;23:1923-34
   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;23:351-63
   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;16:1109-15
   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;16:1102-8
   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;362:686-96
   PubMed Web of Science ®Google Scholar
• Goldstein SR, Neven P, Cummings S, et al. Postmenopausal Evaluation and Risk Reduction With Lasofoxifene (PEARL) trial: 5-year gynecological outcomes. Menopause 2011;18:17-22
   PubMed Web of Science ®Google Scholar
• Ensrud K, LaCroix A, Thompson JR, et al. Lasofoxifene and cardiovascular events in postmenopausal women with osteoporosis: five-year results from the Postmenopausal Evaluation and Risk Reduction with Lasofoxifene (PEARL) trial. Circulation 2010;122:1716-24
   PubMed Web of Science ®Google Scholar
• Fong K, Causer P, Atri M, et al. Transvaginal US and hysterosonography in postmenopausal women with breast cancer receiving tamoxifen: correlation with hysteroscopy and pathologic study. Radiographics 2003;23:137-50
   PubMed Web of Science ®Google Scholar
• Robertson JF, Osborne CK, Howell A, et al. Fulvestrant versus anastrozole for the treatment of advanced breast carcinoma in postmenopausal women: a prospective combined analysis of two multicenter trials. Cancer 2003;98:229-38
   PubMed Web of Science ®Google Scholar
• Howell A, Robertson JF, Abram P, et al. Comparison of fulvestrant versus tamoxifen for the treatment of advanced breast cancer in postmenopausal women previously untreated with endocrine therapy: a multinational, double-blind, randomized trial. J Clin Oncol 2004;22:1605-13
   PubMed Web of Science ®Google Scholar
• Di Leo A, Jerusalem G, Petruzelka L, et al. Results of the CONFIRM phase III trial comparing fulvestrant 250 mg with fulvestrant 500 mg in postmenopausal women with estrogen receptor-positive advanced breast cancer. J Clin Oncol 2010;28:4594-600
   PubMed Web of Science ®Google Scholar
• Duvernoy CS, Kulkarni PM, Dowsett SA, Keech CA. Vascular events in the Multiple Outcomes of Raloxifene Evaluation (MORE) trial: incidence, patient characteristics, and effect of raloxifene. Menopause 2005;12:444-52
   PubMed Web of Science ®Google Scholar
• Walsh BW, Kuller LH, Wild RA, et al. Effects of raloxifene on serum lipids and coagulation factors in healthy postmenopausal women. JAMA 1998;279:1445-51
   PubMed Web of Science ®Google Scholar
• Euser AM, Zoccali C, Jager KJ, Dekker FW. Cohort studies: prospective versus retrospective. Nephron Clin Pract 2009;113:c214-17
   PubMed Web of Science ®Google Scholar
• European Medicine Agency. Summary of product characteristics. Conbriza. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000913/WC500033577.pdf [Last accessed 19 December 2013]
   Google Scholar
• Palacios S, Silverman SL, de Villiers TJ, et al. A 7-year, randomized, placebo-controlled trial to assess the long-term efficacy and safety of bazedoxifene in postmenopausal women with osteoporosis: effects on bone density and fracture. Menopause 2015. [Epub ahead of print]
   Google Scholar
• Study evaluating bazedoxifene acetate in osteoporosis in postmenopausal women NCT00205777. ClinicalTrials.gov Available from: http://www.clinicaltrials.gov/ct2/show/study/NCT00205777?term=3068A1-301&rank=2&sect=X30156 [Last accessed 20 November 2014]
   Google Scholar