Osteoporosis.  2015 Aug;13(1):1-14. 10.0000/ost.2015.13.1.1.

Selective Estrogen Receptor Modulators: A Review of Action Mechanism and Clinical Data

• Kim SS

• KMID: 2314151
• DOI: http://doi.org/10.0000/ost.2015.13.1.1

Abstract

Selective estrogen receptor modulators (SERMs) are a diverse group of synthetic non-steroidal compounds that have various levels of estrogen receptor (ER) agonist or antagonist activity depending on the target tissue. This feature of SERMs could be explained by the differential expression of two ER isoforms (ERalpha or ERbeta), the differential ER conformational change and the differential coregulatory proteins (coactivator or corepressor) in a selected tissue. Based on their efficacy and safety, SERMs have been used for the prevention and treatment of breast cancer (tamoxifene and toremifene), prevention and treatment of osteoporosis (relaoxifene and bazedoxifene), treatment for dyspareunia related to vulvovaginal atrophy (ospemifene) and treatment for vasomotor symptoms associated with menopause (tissue selective estrogen complex; TSEC). Many of the available SERMs are well-known for their anti-estrogenic effects in breast and for their estrogenic effects in bone. The effect on the endometrium have played a key role in differentiate SERMs in clinical practice. The effect of SERMs in the vagina also shows clear distinction among different SERMs. This review summarizes their action mechanism and describes their clinical findings in different target tissues. In the osteoporosis treatment, SERMs such as raloxifene and bazedoxifene is a safe and effective option for women who cannot tolerate or are unwilling to take bisphosphonates and may be appropriate for younger woman with the age of < or =70 years old who expect to remain on therapy for many years and are concerned about the long-term safety of bisphosphonates.

Keyword

Agonist; Antagonist; Estrogen receptor; Osteoporosis; Selective estrogen receptor modulator

MeSH Terms

Atrophy
Breast
Breast Neoplasms
Diphosphonates
Dyspareunia
Endometrium
Estrogens
Female
Humans
Menopause
Osteoporosis
Protein Isoforms
Raloxifene Hydrochloride
Selective Estrogen Receptor Modulators*
Vagina
Diphosphonates
Estrogens
Protein Isoforms
Selective Estrogen Receptor Modulators