, Volume 71, Issue 16, pp 2193-2212
Date: 24 Sep 2012

Bazedoxifene

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Abstract

Bazedoxifene (Conbriza®, Viviant®) is the first third-generation selective estrogen receptor modulator (SERM) and it is approved for the treatment of postmenopausal osteoporosis in the EU and Japan. Bazedoxifene contains an indole-based core binding domain that binds with high affinity to estrogen receptors and exhibits favourable effects on bone and lipid profiles, with no clinically relevant endometrial or breast stimulation. Oral bazedoxifene once daily reduced the incidence of new vertebral fractures in patients with postmenopausal osteoporosis in a large, well designed trial of 3 years’ duration; both bazedoxifene and raloxifene were significantly more effective than placebo. Neither bazedoxifene nor raloxifene reduced the incidence of nonvertebral fractures in the overall study population; however, bazedoxifene, but not raloxifene, reduced the rate of nonvertebral fractures in high-risk patients. Moreover, data from patients who continued to receive the drug during a 2-year extension phase of this trial indicate that bazedoxifene continues to provide protection against new vertebral fractures for up to 5 years. Bazedoxifene also increases bone mineral density and reduces the levels of bone turnover markers. Bazedoxifene was generally well tolerated and did not detrimentally affect the reproductive tract or breast tissue in clinical trials, thereby demonstrating a favourable risk-benefit profile. A pharmacoeconomic analysis conducted from an EU perspective predicted bazedoxifene to be cost effective in some EU countries.Therefore, bazedoxifene presents another useful option for the treatment of post-menopausal osteoporosis, especially in those at high risk for osteoporotic fracture.

An Erratum for this chapter can be found at http://dx.doi.org/10.2165/11631020-000000000-00000
Various sections of the manuscript reviewed by: S.L. Silverman, Division of Medicine and Rheumatology, Cedars-Sinai Medical Center, Beverly Hills, Los Angeles, CA, USA; S.L. Bonnick, Clinical Research Center of North Texas, Denton, TX, USA; M.L. Brandi, Department of Internal Medicine, University of Florence, Florence, Italy; J.A. Kanis, WHO Collaborating Centre for Metabolic Bone Diseases, University of Sheffield Medical School, Sheffield, UK; D.F. Archer, Department of Obstetrics & Gynecology, Eastern Virginia Medical School, Norfolk, VA, USA.

Data Selection

Sources: Medical literature (including published and unpublished data) on ‘bazedoxifene’ was identified by searching databases since 1996 (including MEDLINE and EMBASE and in-house AdisBase), bibliographies from published literature, clinical trial registries/databases and websites (including those of regional regulatory agencies and the manufacturer). Additional information (including contributory unpublished data) was also requested from the company developing the drug.
Search strategy: MEDLINE, EMBASE and AdisBase search terms were ‘bazedoxifene’ and (‘postmenopausal osteoporosis’ or ‘postmenopause osteoporosis’). Searches were last updated on 15 July 2011.
Selection: Studies in patients with postmenopausal osteoporosis who received bazedoxifene. Inclusion of studies was based mainly on the methods section of the trials. When available, large, well controlled trials with appropriate statistical methodology were preferred. Relevant pharmacodynamic and pharmacokinetic data are also included.
Index terms: Bazedoxifene, postmenopausal osteoporosis, pharmacodynamics, pharmacokinetics, therapeutic use, tolerability, pharmacoeconomics.
An erratum to this article is available at http://dx.doi.org/10.2165/11631020-000000000-00000.