Bazedoxifene: A new selective estrogen receptor modulator for the treatment of postmenopausal osteoporosis

Expert Opinion on Pharmacotherapy

Volumn 10, Issue 8, 2009, Pages 1377-1385

  Kung, Annie W C ^a   Chu, Eva Y W ^a   Xu, Ling ^b  

^a UNIVERSITY OF HONG KONG   (Hong Kong)

^b PEKING UNION MEDICAL COLLEGE HOSPITAL   (China)

Author keywords

Bazedoxifene; Estrogen; Osteoporosis; Selective estrogen receptor modulator

Indexed keywords

BAZEDOXIFENE; BAZEDOXIFENE C 14; CONJUGATED ESTROGEN; ESTROGEN; ESTROGEN RECEPTOR; GESTAGEN; LASOFOXIFENE; MEDROXYPROGESTERONE ACETATE; PARATHYROID HORMONE; PLACEBO; RALOXIFENE; RISEDRONIC ACID; TAMOXIFEN; UNCLASSIFIED DRUG;

AMENORRHEA; BONE DENSITY; BONE METABOLISM; BONE TURNOVER; BREAST; BREAST CARCINOMA; BREAST CYST; CLINICAL TRIAL; CYST; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG EFFICACY; DRUG EXCRETION; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; ENDOMETRIUM CARCINOMA; ENDOMETRIUM HYPERPLASIA; FIBROCYSTIC CYST; HIGH RISK POPULATION; HOT FLUSH; HUMAN; LEG CRAMP; MASTALGIA; MAXIMUM PLASMA CONCENTRATION; MONOTHERAPY; NONHUMAN; OSTEOLYSIS; OSTEOPENIA; POSTMENOPAUSE OSTEOPOROSIS; REVIEW; RISK ASSESSMENT; UTERUS; VASOMOTOR REFLEX; VENOUS THROMBOEMBOLISM; VERTEBRA DISLOCATION;

CLINICAL TRIALS AS TOPIC; HUMANS; INDOLES; OSTEOPOROSIS, POSTMENOPAUSAL; SELECTIVE ESTROGEN RECEPTOR MODULATORS;

EID: 67649690531     PISSN: 14656566     EISSN: None     Source Type: Journal    
DOI: 10.1517/14656560902980228     Document Type: Review

References (27)

1. Prevention and management of osteoporosis. WHO Scientific Group. World Health Organization Technical Report Series 2003;921:1-164
2. Stevenson JC. Justification for the use of HRT in the long-term prevention of osteoporosis. Maturitas 2005;51(2):113-126 (Pubitemid 40726109)
3. Gruber C, Gruber D. Bazedoxifene (Wyeth). Curr Opin Investig Drugs 2004;5(10):1086-1093
4. Patat A, McKeand W, Baird-Bellaire S, et al. Absolute/relative bioavailability of bazedoxifene acetate in healthy postmenopausal women [abstractP43]. Clin Pharmacol Ther 2003;73
5. Ermer J, Kotake A, McKeand W, et al. Clinical pharmacology of a novel tissue selective estrogen (WAY-140424) in postmenopausal women following administration for 30 days [abstractP94]. J Bone Miner Res 2000;17M
6. Chandrasekaran A, Ermer J, McKeand W, et al. Bazedoxifene acetate metabolic disposition in healthy, postmenopausal women [abstractP47]. Clin Pharmacol Ther 2003;73
7. Crabtree JS, Peano BJ, Zhang X, et al. Activity of three selective estrogen receptor modulators on hormone-dependent responses in the mouse uterus and mammary gland. Mol Cell Endocrinol 2008;287(1-2):40-46
8. Komm BS, Kharode YP, Bodine PV, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology 2005;146(9):3999-4008 (Pubitemid 41175771)
9. Komm BS, Kharode YP, Bodine PV, Bex F. Bazedoxifene + conjugated estrogens: a balanced combination to provide optimal "Estrogenic" safety and efficacy [abstractS272]. J Bone Miner Res 2003;18(Suppl 2)
10. 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;949:317-326 (Pubitemid 34059996)
11. Miller CP, Collini MD, Tran BD, et al. Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. J Med Chem 2001;44(11):1654-1657 (Pubitemid 32852172)
12. Smith SY, Minck SY, Jolette J, et al. Bazedoxifene prevents ovariectomy-induced bone loss in the cynomolgus monkey [abstractS174]. J Bone Miner Res 2005;20(Suppl 1)
13. Davies GC, Huster WJ, Lu Y, et al. Adverse events reported by postmenopausal women in controlled trials with raloxifene. Obstet Gynecol 1999;93(4):558-565 (Pubitemid 29147076)
14. Katovich MJ, Simpkins JW, Barney CC. Alpha-adrenergic mediation of the tail skin temperature response to naloxone in morphine-dependent rats. Brain Res 1987;426(1):55-61 (Pubitemid 17158882)
15. Ciriza I, Carrero P, Azcoitia I, et al. Selective estrogen receptor modulators protect hippocampal neurons from kainic acid excitotoxicity: differences with the effect of estradiol. J Neurobiol 2004;61(2):209-221 (Pubitemid 39426147)
16. 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;105(6):1397-1404 (Pubitemid 40734275)
17. van Duren D, Ronkin S, Pickar J, Constantine G. Bazedoxifene combined with conjugated estrogens: a novel alternative to traditional hormone therapies [abstractS88-S89]. Fertil Steril 2006;86(Suppl 1)
18. Itabashi I, Ohta H, Ebede B, Constantine G. A double-blind, placebo-controlled, dose-response study of bazedoxifene in Japanese postmenopausal women with osteoporosis [abstractP79]. J Bone Miner Res 2008;23
19. Boudes P, Ronkin S, Korner P, et al. Effects of bazedoxifene (TSE-424), a novel tissue selective estrogen receptor modulator (SERM), on the incidence of breast pain [abstractS4] Osteoporos Int 2003;14
20. Bachmann G, Crosby U, Feldman RA, et al. Vasomotor effects of bazedoxifene in nonflushing postmenopausal women [abstract P-10]. Menopause 2008;15(6):1212
21. Chesnut CH, Christiansen C, Hoeck HC, et al. Safety and tolerability of bazedoxifene for the prevention of postmenopausal osteoporosis [abstractW387]. J Bone Miner Res 2007;22
22. Miller CP, Christiansen C, Hoeck HC, et al. Efficacy of bazedoxifene for prevention of postmenopausal osteoporosis. Results of a 2-year, phase III, placebo- and active-controlled study [abstract1209]. J Bone Miner Res 2007;22
23. 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(4):525-535
24. Adachi JD, Chesnut CH, Brown JP, et al. Safety and tolerability of bazedoxifene in postmenopausal women with osteoporosis: results from a 3-year, randomized, placebo- and active-controlled clinical trial [abstractW385]. J Bone Miner Res 2007;22
25. 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(12):1923-1934 (Pubitemid 351575033)
26. New Tissue-Selective Estrogen Complex Shows Improvement in Bone Density; 2007 http://www.medscape.com/viewarticle/558305
27. Bayes M, Rabasseda X. Gateways to clinical trials. Methods Find Exp Clin Pharmacol 2008;30(1):67-99