Endometrial Effects of Bazedoxifene Acetate, a Novel Selective Estrogen Receptor Modulator, in Postmenopausal Women

Ronkin, Sheila; Northington, Robert; Baracat, Edmund Chada; Nunes, Márcia Gaspar; Archer, David F.; Constantine, Ginger D.; Pickar, James H.

doi:10.1097/01.aog.0000163253.27610.b9

Cited by 106 publications

(64 citation statements)

References 20 publications

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“…Based on endometrial protective properties of BZA observed in preclinical and clinical evaluations (11)(12)(13), it was hypothesized that a TSEC composed of BZA/CE would provide effective relief of menopausal symptoms with a high level of endometrial safety and a favorable tolerability profile. Findings from this phase III trial indicate that TSECs composed of BZA/CE at dose combinations of BZA 20 and 40 mg with CE 0.45 and 0.625 mg are associated with an amenorrhea profile similar to that observed with placebo, suggesting that BZA/CE may offer a favorable tolerability profile.…”

Section: Figurementioning

confidence: 99%

“…Preclinical studies (11,12) also showed that BZA inhibits 17b-E 2 -induced proliferation of MCF-7 human breast cancer cells in a dose-dependent manner. Daily doses of 2.5, 5.0, 10, 20, 30, and 40 mg BZA in a phase II study (13) were generally well tolerated and were not associated with endometrial stimulation compared with placebo. Further, BZA 30 and 40 mg were associated with significantly smaller mean increases in endometrial thickness and significant decreases in uterine bleeding compared with placebo (P<.05) (13), suggesting estrogen antagonist activity in the endometrium.…”

mentioning

confidence: 98%

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Bazedoxifene/conjugated estrogens (BZA/CE): incidence of uterine bleeding in postmenopausal women

Archer

Lewis

Carr

et al. 2009

Fertility and Sterility

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116

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Section: Figurementioning

confidence: 99%

mentioning

confidence: 98%

Bazedoxifene/conjugated estrogens (BZA/CE): incidence of uterine bleeding in postmenopausal women

Archer

Lewis

Carr

et al. 2009

Fertility and Sterility

Self Cite

116

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“…A recent report of a 2 year study revealed that BMD of the lumbar spine and hip were significantly greater with bazodoxifene than with placebo for all the various doses. There was reduced bone turnover and prevention of bone loss similar to raloxifene [51]. The significant differences were apparent at 6 months with bazodoxifene versus placebo and were maintained up to the 24th month.…”

Section: Serms Under Developmentmentioning

confidence: 84%

SERMs and SERMs with estrogen for postmenopausal osteoporosis

Bolognese

2010

Rev Endocr Metab Disord

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Bone loss with aging places postmenopausal women at a higher risk for osteoporosis and its consequences such as fractures, pain, disability, and increased morbidity and mortality. Approximately 200 million patients worldwide are affected. The Third National Health and Nutrition Examination Survey (NHANES III) estimated that up to 18% of US women aged 50 and older have osteoporosis and up to 50% have osteopenia. Greater than 2 million osteoporotic related fractures occurred in the United States with direct healthcare costs exceeding $17 billion. Hormone Replacement Therapy (HRT) was a popular option for postmenopausal women before the Women's Health Initiative (WHI). Several agents are available in the U.S., including bisphosphonates, hormone therapy, calcitonin, parathyroid hormone and the selective estrogen receptor modulator (SERM) raloxifene. There are concerns about long term safety and compliance. Therefore, other agents are under investigation. SERMs are a diverse group of agents that bind to the estrogen receptor and each SERM appears to have a unique set of clinical responses, which are not always consistent with the typical responses seen with other SERMs. This article will discuss the SERMs approved in the United States, tamoxifene and raloxifene, and investigational SERMs. The ideal SERM would include the beneficial effects of estrogen in bone, heart and the central nervous system, with neutral or antagonistic effects in tissues where estrogen effects are undesirable(breast and endometrium). A new target in treating postmenopausal osteoporosis is the tissue estrogen complex or the pairing of a SERM with a conjugated estrogen known as a tissue selective estrogen complex (TSEC). This novel approach is currently being evaluated with bazodoxifene which could yield the beneficial effects of estrogens and SERMS, while potentially being more tolerable and safer than either therapy alone.

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“…No difference in endometrial thickness was found in a randomized clinical trial of approximately 500 women with an intact uterus [6]. No difference in endometrial thickness was found between bazedoxifene and placebo.…”

Section: Phase 2 Studiesmentioning

confidence: 88%

New therapies for osteoporosis: Zoledronic acid, bazedoxifene, and denosumab

Silverman

2009

Curr Osteoporos Rep

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Intravenous (IV) zoledronic acid, a new once-yearly bisphosphonate therapy, is approved by the US Food and Drug Administration for treatment of postmenopausal osteoporosis, glucocorticoid-induced osteoporosis, and osteoporosis in men. IV zoledronic acid significantly reduced the risk of vertebral, nonvertebral, and hip fractures in postmenopausal women and decreased risk of clinical fracture and clinical vertebral fracture in men and women with hip fracture. Two promising new therapies are in late clinical development. Denosumab is a monoclonal receptor activator of nuclear factor- kappaB ligand (RANKL) antibody given by subcutaneous injection every 6 months that has been shown to significantly reduce risk of vertebral-, nonvertebral-, and hip fracture in postmenopausal women. Bazedoxifene, an estrogen agonist/antagonist, has significantly reduced the risk of vertebral fracture in postmenopausal women; a post hoc analysis showed reduction in risk of nonvertebral fracture in high-risk women.

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Endometrial Effects of Bazedoxifene Acetate, a Novel Selective Estrogen Receptor Modulator, in Postmenopausal Women

Cited by 106 publications

References 20 publications

Bazedoxifene/conjugated estrogens (BZA/CE): incidence of uterine bleeding in postmenopausal women

Bazedoxifene/conjugated estrogens (BZA/CE): incidence of uterine bleeding in postmenopausal women

SERMs and SERMs with estrogen for postmenopausal osteoporosis

New therapies for osteoporosis: Zoledronic acid, bazedoxifene, and denosumab

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