Cited by 39Menopause: Health Impacts and TreatmentsBone health and osteoporosis researchEstrogen and related hormone effects

Bazedoxifene for the prevention of postmenopausal osteoporosis

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Gennari, Luigi·2008·Therapeutics and Clinical Risk Management

Abstract

Bazedoxifene for the prevention of postmenopausal osteoporosis Luigi Gennari, Daniela Merlotti, Vincenzo De Paola, Giuseppe Martini, Ranuccio NutiDepartment of Internal Medicine, Endocrine-Metabolic Sciences and Biochemistry, University of Siena, Policlinico Le Scotte 53100-Siena, ItalyAbstract: Bazedoxifene acetate is a novel, chemically distinct selective estrogen receptor modulator (SERM) that has been specifically developed after a stringent preclinical screening in order to obtain favorable effects on the skeleton and lipid metabolism with the additional improvement of a neutral effect on hot flushes and without stimulating the uterus or the breast. In both preclinical and clinical studies this SERM was shown to maintain BMD, prevent fractures, and reduce total cholesterol. Moreover, bazedoxifene also showed an improved uterine profile and demonstrated estrogen antagonistic activity on the endometrium. Importantly, this latter capacity has led to the development of a novel class of menopausal therapy called tissue selective estrogen complex (TSEC), in which bazedoxifene is combined with conjugated estrogen. The rationale for selecting bazedoxifene as the SERM in this TSEC combination is that it may offset estrogen stimulation of endometrial and breast tissue, without the necessity of using a progestin in women with an intact uterus, without aggravating menopausal vasomotor symptoms, but with an additive effect on bone. Preliminary data from phase 3 clinical trials appear to confirm this hypothesis, showing a greater effect of bazedoxifene on BMD with respect to raloxifene, coupled with efficacy on menopausal vasomotor symptoms not achieved by SERM alone. These properties and the safety profile of this combination, if confirmed long-term in ongoing phase 3 trials, might significantly affect the way women and physicians approach menopause and its related disorders.Keywords: bazedoxifene, SERM, estrogen, postmenopausal osteoporosis, treatment

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  • Conjugated estrogens/bazedoxifene increased total hip BMD, with a treatment difference of 1.21% at 12 months.

    “Treatment with conjugated estrogens/bazedoxifene also increased total hip BMD. The treatment difference in total hip BMD at 12 months was 1.21 % [87–90].”

    From Clinician’s Guide to Prevention and Treatment of Osteoporosis (2014) · cites this paper as [87]

    The section on clinical studies of bazedoxifene with estrogen reports increased BMD with bazedoxifene/conjugated estrogens after two years and says similar results were observed for hip BMD. It does not report a 1.21% treatment difference for total hip BMD at 12 months. Page numbers were not available in our copy. (LLM, conf=0.86)

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  • Conjugated estrogens/bazedoxifene significantly increased mean lumbar spine BMD (treatment difference 1.51%) at 12 months compared to placebo in women who had been postmenopausal between 1 and 5 years.

    “Use of this combination drug significantly increased mean lumbar spine BMD (treatment difference, 1.51 %), at 12 months compared to placebo in women who had been postmenopausal between 1 and 5 years.”

    From Clinician’s Guide to Prevention and Treatment of Osteoporosis (2014) · cites this paper as [87]

    In “Clinical studies of bazedoxifene acetate in combination with estrogen” (page unavailable), the SMART-1 substudy reports greater lumbar spine BMD with bazedoxifene/conjugated estrogens than placebo after two years, including women within five years of menopause. It does not report the claimed 1.51% treatment difference at 12 months for that combination; the passage mentioning a significant 12-month increase concerns bazedoxifene alone. (LLM, conf=0.88)

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Research works printed but not linked: 1

  1. Bergmann Koury C 2007 TSECs may offer new option for menopausal symptom treatment, osteoporosis prevention Review of Endocrinology 45 6

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Authors
Gennari, L.
Affiliations
University of Siena (IT)
Corresponding author
Gennari, Luigi
Venue
Therapeutics and Clinical Risk Management
Published
2008-12
Volume
Volume 4
Issue
6
Pages
1229-1242
ISSN
  • 1176-6336 (ISSN-L)
  • 1178-203X
OpenAlex
W1895595364
Cited by
39
References
66
Citations by year
2026: 2 · 2025: 2 · 2024: 4 · 2023: 2 · 2022: 2 · 2021: 5 · 2020: 4 · 2017: 3 · 2015: 2 · 2014: 1 · 2013: 1 · 2012: 2
FWCI
2.18
Type
journal article
Language
en
Open access
Locations
  • Therapeutics and Clinical Risk Management (publishedVersion, cc-by-nc)
  • PubMed Central (publishedVersion)
  • PubMed (publishedVersion)
  • Use Siena air (University of Siena) (submittedVersion, cc-by-nc)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
  • Dove Medical Press (Taylor and Francis Group) (submittedVersion, cc-by-nc)
Topics
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Menopause: Health Impacts and Treatments
  • Health Sciences › Medicine › Orthopedics and Sports Medicine › Bone health and osteoporosis research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
Keywords
bazedoxifene, postmenopausal osteoporosis, selective estrogen receptor modulators, tissue-selective estrogen complex, conjugated estrogens, bone mineral density, fracture prevention, menopausal vasomotor symptoms, endometrial protection, raloxifene, lipid metabolism, hot flashes

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