Tissue-selective estrogen complex bazedoxifene and conjugated estrogens for the treatment of menopausal vasomotor symptoms

Drugs

Volumn 71, Issue 13, 2011, Pages 1649-1657

  Stovall, Dale W ^a   Tanner Kurtz, Kirby ^a   Pinkerton, Joann V ^a  

^a UNIVERSITY OF VIRGINIA HEALTH SYSTEM   (United States)

Author keywords

Bazedoxifene; Conjugated estrogens; Conjugated estrogensbazedoxifene; Hot flashes; Menopausal syndrome; Menopause; Selective estrogen receptor modulators.

Indexed keywords

BAZEDOXIFENE; CONJUGATED ESTROGEN; ETHINYLESTRADIOL; GESTAGEN; HIGH DENSITY LIPOPROTEIN; LOW DENSITY LIPOPROTEIN; MEDROXYPROGESTERONE ACETATE; PLACEBO; RALOXIFENE;

AMENORRHEA; BONE DENSITY; BREAST CANCER; CANCER RISK; CELL PROLIFERATION; DISEASE ASSOCIATION; ENDOMETRIUM HYPERPLASIA; ESTROGEN BLOOD LEVEL; GALLBLADDER DISEASE; HEART INFARCTION; HOT FLUSH; HUMAN; HYSTERECTOMY; LUNG EMBOLISM; MENOPAUSAL SYNDROME; NIGHT SWEAT; OSTEOPOROSIS; OVARY CYST; OVARY FOLLICLE; QUALITY OF LIFE; REVIEW; SLEEP DEPRIVATION; STROKE; TRANSIENT ISCHEMIC ATTACK; VAGINA ATROPHY; VASOMOTOR DISORDER; VENOUS THROMBOEMBOLISM;

ADULT; DRUG THERAPY, COMBINATION; ESTROGENS, CONJUGATED (USP); FEMALE; HOT FLASHES; HUMANS; INDOLES; MENOPAUSE; MIDDLE AGED; OSTEOPOROSIS, POSTMENOPAUSAL; RANDOMIZED CONTROLLED TRIALS AS TOPIC; SELECTIVE ESTROGEN RECEPTOR MODULATORS; VASOMOTOR SYSTEM;

EID: 80052617751     PISSN: 00126667     EISSN: 11791950     Source Type: Journal    
DOI: 10.2165/11592820-000000000-00000     Document Type: Review

References (40)

1. Morabia A, Costanza MC. International variability in ages at menarche, first livebirth, and menopause. World Health Organization Collaborative Study of Neoplasia and Steroid Contraceptives. Am J Epidemiol 1998; 148: 1195-205 (Pubitemid 29018283)
2. US Census Bureau.Annual estimates of the population by sex and five-year age groups for the United States: April 1, 2000 to July 1, 2007 (NC-EST2007-01) [online]. Available from URL: http://www.census.gov [Accessed 2011 Mar 01]
3. McKinlay SM, Brambilla DJ, Posner JG. The normal menopause transition. Maturitas 1992; 14: 103-15
4. National Institutes of Health. State of science conference statement on management of menopause-related symptoms, 2005 [online]. Available from URL: http://consensus. nih.gov/[Accessed 2011Mar 01]
5. Col NF, Guthrie JR, Politi M, et al. Duration of vasomotor symptoms in middle-aged women: a longitudinal study. Menopause 2009; 16 (3): 453-7
6. Guthrie JR, Dennerstein L, Taffe JR, et al. Health careseeking for menopausal problems. Climacteric 2003; 6: 112-7
7. Avis ND, Stellato R, Crawford S, et al. Is there a menopausal syndrome? Menopausal status and symptoms across racial/ethnic groups. Soc Sci Med 2001; 52: 345-56
8. Bobula JD. Vasomotor symptoms and quality of life in postmenopausal women [abstract]. Value Health 2003; 6: 707
9. Guidance for Industry. Estrogen and estrogen/progestin drug products to treat vasomotor symptoms and vulvar and vaginal atrophy symptoms: recommendations for clinical evaluation. Silver Spring (MD): U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research, 2003
10. Santoro N. Symptoms of menopause: hot flushes. Clin Obstet Gynecol 2008; 51 (3): 539-48
11. Kronenberg F. Hot flashes: epidemiology and physiology. Ann NY Acad Sci 1990; 592: 52-86 (Pubitemid 20273207)
12. Freedman RR, Norton D, Woodward S, et al. Core body temperature and circadian rhythm of hot flashes in menopausal women. J Clin Endocrinol Metab 1995; 80: 2354-8
13. Freedman RR, Krell W. Reduced thermoregulatory null zone in postmenopausal women with hot flashes. Am J Obstet Gynecol 1999; 181: 66-71
14. Freedman RR, Woodward S, Sabharwal SC. Alpha2-adrenergic mechanism in menopausal hot flushes. Obstet Gynecol 1990; 76: 573-8 (Pubitemid 20322054)
15. Freedman RR. Biochemical, metabolic, and vascular mechanisms in menopausal hot flashes. Fertil Steril 1998; 70: 332-7 (Pubitemid 28361490)
16. Berendsen HH. The role of serotonin in hot flushes. Maturitas 2000; 36: 155-64
17. Bhavnani GR. Estrogens and menopause: pharmacology of conjugated equine estrogens and their potential role in the prevention of neurodegenerative diseases such as Alzheimer's. J Steroid Biochem Mol Biol 2003; 85 (2-5): 473-82
18. Jackson RD, Wactawski-Wende J, LaCroiz AZ, et al. Effects of conjugated equine estrogen on risk of fractures and BMD in postmenopausal women with hysterectomy: results from the Women's Health Initiative randomized trial. J Bone Miner Res 2006; 216: 817-28 (Pubitemid 43787988)
19. Maclennan AH, Broadbent JL, Lester S, et al. Oral oestrogen and combined oestrogen/progestogen therapy versus placebo for hot flushes. Cochrane Database Syst Rev 2004; 4: CD002978
20. Smith DC, Prentice R, Thompson DJ, et al. Association of exogenous estrogen and endometrial carcinoma. N Engl J Med 1975; 293: 1164-7
21. Anderson GL, Judd HL, Kaunitz AM, et al. Effects of estrogen plus progestin on gynecologic cancers and associated diagnostic procedures: the Women's Health Initiative randomized trial. JAMA 2003; 290: 1739-48 (Pubitemid 37430624)
22. Rossouw JE, Anderson GL, Prentice RL, et al. Risks and benefits of estrogen plus progestin in healthy menopausal women: principal results from the Women's Health Initiative randomized controlled trial. JAMA 2002; 288: 321-33 (Pubitemid 34761611)
23. Lukes AJ. Evolving issues in the clinical and managed care settings on the management of menopause following the Women's Health Initiative. Manage Care Pharm 2008; 14 (3): 7-13
24. Katzenellenbogen BS, Choi IH, Delage-Mouroux R, et al. Molecular mechanisms of estrogen action: selective ligands and receptor pharmacology. J Steroid Biochem Mol Biol 2000; 74: 279-85 (Pubitemid 32126240)
25. Silverman SL. New selective estrogen receptor modulators (SERMs) in development. Curr Osteoporosis Rep 2010; 8: 151-3
26. Kian TM, Rogatsky I, Tzagarakis-Foster C, et al. Estradiol and selective estrogen receptor modulators differentially regulate target genes with estrogen receptors alpha and beta. Mol Cell Biol 2004; 15: 1262-72 (Pubitemid 38316233)
27. Komm BS, Lyttle CR. Developing a SERM: Stringent preclinical selection criteria leading to an acceptable candidate (WAY-140424) for clinical evaluation. Ann NY Acad Sci 2001; 949: 317-26 (Pubitemid 34059996)
28. Komm BS, Kharode YP, Bodine PV, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology 2005; 146: 3999-4008 (Pubitemid 41175771)
29. 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 (Pubitemid 351501893)
30. 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
31. Ronkin S, Northington R, Baracat E, et al. Endometrial effects of bazedoxifen acetate, a novel selective estrogen receptor modulator, in postmenopausal women. Obstet Gynecol 2005; 105: 1397-404 (Pubitemid 40734275)
32. Van Duren D, Ronkin S, Pickar J, et al. Bazedoxifene combined with conjugated estrogens: a novel alternative to traditional hormone therapies. Fertil Steril 2006; 86: S88-9
33. 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; 92: 1018-24
34. Lobo RA, Pinkerton JV, Gass MLS, 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: 1025-38
35. Archer DE, Lewis V, Carr BR, et al. Bazedoxifene/conjugated estrogens (BZA/CE): incidence of uterine bleeding in postmenopausal women. Fertil Steril 2009; 92: 1039-44
36. Lindsay R, Gallagher JC, Kagan R, et al. Efficacy of tissueselective estrogen complex of bazedoxifene/conjugated estrogens for osteoporosis prevention in at-risk postmenopausal women. Fertil Steril 2009; 93: 1045-52
37. Pinkerton JV, Utian WH, Constantine GD, et al. Relief of vasomotor symptoms with the tissue-selective estrogen complex containing bazedoxifene/conjugated estrogens: a randomized, controlled trial. Menopause 2009; 16: 1116-24
38. Utian WH, Yu H, Bobula J, et al. Bazedoxifene/conjugated estrogens and quality of life in postmenopausal women. Maturitas 2009; 63: 329-35
39. 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; 17 (2): 281-9
40. Bachmann G, Bobula J, Mirkin S. Effects of bazedoxifene/conjugated estrogens on quality of life in postmenopausal women with symptoms of vulvar/vaginal atrophy. Climacteric 2010; 13 (2): 132-40