Conjugated estrogens combined with bazedoxifene: the first approved tissue selective estrogen complex therapy

Abstract

Menopausal therapy with a tissue selective estrogen complex combines estrogens with a selective estrogen receptor modulator, with the goal of blending the desirable effects of estrogens on menopausal symptoms and bone with the tissue selective properties of a selective estrogen receptor modulator. The first tissue selective estrogen complex to receive regulatory approval is a combination of conjugated estrogens (CE) with bazedoxifene (BZA). Clinical trials with CE/BZA in postmenopausal women have shown improvement in vasomotor symptoms, vulvo-vaginal atrophy, and bone mineral density, without stimulation of the endometrium or breast tissue, with a generally favorable safety and tolerability profile. CE/BZA represents a new approach to the management of menopausal symptoms in women with a uterus.

Keywords::

• bazedoxifene
• estrogen
• menopause
• osteoporosis
• vasomotor symptoms

Financial & competing interests disclosure

M Sharifi has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. EM Lewiecki has received institutional grant/research support from Amgen, Merck, Eli Lilly and Pfizer; the author has served on scientific advisory boards for Amgen, Merck, Eli Lilly, Radius Health and AgNovos Healthcare.

No writing assistance was utilized in the production of this manuscript.

Key issues

• Safety concerns with cardiovascular and breast cancer risks have limited the use of estrogen + medroxyprogesterone acetate in postmenopausal women.

• Bazedoxifene (BZA) is a selective estrogen receptor modulator with beneficial effects on the skeleton and neutral effects on the endometrium and breast.

• Tissue-selective estrogen complex is a new class of therapy that combines estrogen(s) with a selective estrogen receptor modulator.

• The combination of conjugated estrogens and BZA is effective in treating menopausal symptoms without stimulation of the endometrium and breast, without an additive effect on venous thromboembolic disease and no evidence of increased risk of stroke coronary heart disease.

• Conjugated estrogens/BZA is the first tissue-selective estrogen complex to receive regulatory approval for the treatment of moderate-to-severe vasomotor symptoms and prevention of osteoporosis in postmenopausal women with a uterus.