Profile of bazedoxifene/conjugated estrogens for the treatment of estrogen deficiency symptoms and osteoporosis in women at risk of fracture

Maurizio Rossini,1 Stefano Lello,2 Ignazio Sblendorio,3 Ombretta Viapiana,1 Elena Fracassi,1 Silvano Adami,1 Davide Gatti11Department of Medicine, Rheumatology Unit, University of Verona, Italy; 2Endocrinological Gynecology, Pathophysiology of Menopause and Osteoporosis, Dermopathic Institute of Imm...

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Main Authors: Rossini M, Lello S, Sblendorio I, Viapiana O, Fracassi E, Adami S, Gatti D
Format: Article
Language:English
Published: Dove Medical Press 2013-07-01
Series:Drug Design, Development and Therapy
Online Access:http://www.dovepress.com/profile-of-bazedoxifeneconjugated-estrogens-for-the-treatment-of-estro-a13733
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author Rossini M
Lello S
Sblendorio I
Viapiana O
Fracassi E
Adami S
Gatti D
author_facet Rossini M
Lello S
Sblendorio I
Viapiana O
Fracassi E
Adami S
Gatti D
author_sort Rossini M
collection DOAJ
description Maurizio Rossini,1 Stefano Lello,2 Ignazio Sblendorio,3 Ombretta Viapiana,1 Elena Fracassi,1 Silvano Adami,1 Davide Gatti11Department of Medicine, Rheumatology Unit, University of Verona, Italy; 2Endocrinological Gynecology, Pathophysiology of Menopause and Osteoporosis, Dermopathic Institute of Immacolata, Roma, Italy; 3Medical Coach Italia Center, Bari, ItalyAbstract: Decreasing levels of estrogens during menopause are associated with reduced bone density and an increased risk of osteoporosis. Many women also experience bothersome vasomotor and vaginal symptoms during the menopausal transition. Results of systematic reviews and meta-analyses of randomized controlled trials have shown that both systemic estrogen therapy or hormone therapy (estrogen combined with a progestin) are useful to prevent bone loss, and they are the most effective treatment for such climacteric symptoms as hot flushes, sweating, vaginal dryness, and dyspareunia. Unfortunately, estrogen therapy and hormone therapy increase the risk of endometrial and breast cancer, respectively. The selective estrogen receptor modulators (SERMs) result in positive estrogenic effects on bone, with no negative effects on the endometrium and breast but do not provide relief from postmenopausal symptoms. The combination of a SERM with estrogen as a tissue selective estrogen complex (TSEC) is a new strategy for the prevention of bone loss and the treatment of climacteric symptoms. This combination is particularly interesting from a clinical point of view, taking into account that estrogen alone did not increase breast cancer risk by the Women's Health Initiative. TSEC is hypothesized to provide the benefits of estrogen-alone therapy, with an improved tolerability profile because the SERM component can make possible the elimination of progestin. The objective of this review was to critically evaluate the evidence from the reports published to date on the use of bazedoxifene (a third-generation SERM) in combination with conjugated estrogens in postmenopausal women. The conclusion is that effectively, the combination of bazedoxifene and conjugated estrogens may be a promising alternative to hormone therapy for the prevention of osteoporosis and the treatment of postmenopausal symptoms in non-hysterectomized postmenopausal women.Keywords: tissue selective estrogen complex, menopause, bone mineral density, bone turnover markers, climacteric symptoms
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spelling doaj.art-364053c9b36d4bb4892ba7c709299b7a2022-12-22T02:43:36ZengDove Medical PressDrug Design, Development and Therapy1177-88812013-07-012013default601610Profile of bazedoxifene/conjugated estrogens for the treatment of estrogen deficiency symptoms and osteoporosis in women at risk of fractureRossini MLello SSblendorio IViapiana OFracassi EAdami SGatti DMaurizio Rossini,1 Stefano Lello,2 Ignazio Sblendorio,3 Ombretta Viapiana,1 Elena Fracassi,1 Silvano Adami,1 Davide Gatti11Department of Medicine, Rheumatology Unit, University of Verona, Italy; 2Endocrinological Gynecology, Pathophysiology of Menopause and Osteoporosis, Dermopathic Institute of Immacolata, Roma, Italy; 3Medical Coach Italia Center, Bari, ItalyAbstract: Decreasing levels of estrogens during menopause are associated with reduced bone density and an increased risk of osteoporosis. Many women also experience bothersome vasomotor and vaginal symptoms during the menopausal transition. Results of systematic reviews and meta-analyses of randomized controlled trials have shown that both systemic estrogen therapy or hormone therapy (estrogen combined with a progestin) are useful to prevent bone loss, and they are the most effective treatment for such climacteric symptoms as hot flushes, sweating, vaginal dryness, and dyspareunia. Unfortunately, estrogen therapy and hormone therapy increase the risk of endometrial and breast cancer, respectively. The selective estrogen receptor modulators (SERMs) result in positive estrogenic effects on bone, with no negative effects on the endometrium and breast but do not provide relief from postmenopausal symptoms. The combination of a SERM with estrogen as a tissue selective estrogen complex (TSEC) is a new strategy for the prevention of bone loss and the treatment of climacteric symptoms. This combination is particularly interesting from a clinical point of view, taking into account that estrogen alone did not increase breast cancer risk by the Women's Health Initiative. TSEC is hypothesized to provide the benefits of estrogen-alone therapy, with an improved tolerability profile because the SERM component can make possible the elimination of progestin. The objective of this review was to critically evaluate the evidence from the reports published to date on the use of bazedoxifene (a third-generation SERM) in combination with conjugated estrogens in postmenopausal women. The conclusion is that effectively, the combination of bazedoxifene and conjugated estrogens may be a promising alternative to hormone therapy for the prevention of osteoporosis and the treatment of postmenopausal symptoms in non-hysterectomized postmenopausal women.Keywords: tissue selective estrogen complex, menopause, bone mineral density, bone turnover markers, climacteric symptomshttp://www.dovepress.com/profile-of-bazedoxifeneconjugated-estrogens-for-the-treatment-of-estro-a13733
spellingShingle Rossini M
Lello S
Sblendorio I
Viapiana O
Fracassi E
Adami S
Gatti D
Profile of bazedoxifene/conjugated estrogens for the treatment of estrogen deficiency symptoms and osteoporosis in women at risk of fracture
Drug Design, Development and Therapy
title Profile of bazedoxifene/conjugated estrogens for the treatment of estrogen deficiency symptoms and osteoporosis in women at risk of fracture
title_full Profile of bazedoxifene/conjugated estrogens for the treatment of estrogen deficiency symptoms and osteoporosis in women at risk of fracture
title_fullStr Profile of bazedoxifene/conjugated estrogens for the treatment of estrogen deficiency symptoms and osteoporosis in women at risk of fracture
title_full_unstemmed Profile of bazedoxifene/conjugated estrogens for the treatment of estrogen deficiency symptoms and osteoporosis in women at risk of fracture
title_short Profile of bazedoxifene/conjugated estrogens for the treatment of estrogen deficiency symptoms and osteoporosis in women at risk of fracture
title_sort profile of bazedoxifene conjugated estrogens for the treatment of estrogen deficiency symptoms and osteoporosis in women at risk of fracture
url http://www.dovepress.com/profile-of-bazedoxifeneconjugated-estrogens-for-the-treatment-of-estro-a13733
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