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Review
. 2016 Aug;10(4):787-91.
doi: 10.4184/asj.2016.10.4.787. Epub 2016 Aug 16.

Selective Estrogen Receptor Modulators

Affiliations
Review

Selective Estrogen Receptor Modulators

Ki-Chan An. Asian Spine J. 2016 Aug.

Abstract

Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue. After tamoxifen, raloxifene, lasofoxifene and bazedoxifene SERMs have been developed and used for treatment. The clinically decisive difference among these drugs (i.e., the key difference) is their endometrial safety. Compared to bisphosphonate drug formulations for osteoporosis, SERMs are to be used primarily in postmenopausal women of younger age and are particularly recommended if there is a family history of invasive breast cancer, as their use greatly reduces the incidence of this type of cancer in women. Among the above mentioned SERMs, raloxifene has been widely used in prevention and treatment of postmenopausal osteoporosis and vertebral compression fractures, and clinical studies are now underway to test the comparative advantages of raloxifene with those of bazedoxifene, a more recently developed SERM. Research on a number of adverse side effects of SERM agents is being performed to determine the long-term safety of this class of compouds for treatment of osteoporosis.

Keywords: Osteoporosis; Selective estrogen receptor modulators.

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Conflict of interest statement

No potential conflict of interest relevant to this article was reported.

References

    1. Johnson SR. Menopause and hormone replacement therapy. Med Clin North Am. 1998;82:297–320. - PubMed
    1. Archer DF. The gynecologic effects of lasofoxifene, an estrogen agonist/antagonist, in postmenopausal women. Menopause. 2011;18:6–7. - PubMed
    1. Silverman SL, Chines AA, Kendler DL, et al. Sustained efficacy and safety of bazedoxifene in preventing fractures in postmenopausal women with osteoporosis: results of a 5-year, randomized, placebocontrolled study. Osteoporos Int. 2012;23:351–363. - PubMed
    1. Nelson ER, Wardell SE, McDonnell DP. The molecular mechanisms underlying the pharmacological actions of estrogens, SERMs and oxysterols: implications for the treatment and prevention of osteoporosis. Bone. 2013;53:42–50. - PMC - PubMed
    1. Paterni I, Granchi C, Katzenellenbogen JA, Minutolo F. Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential. Steroids. 2014;90:13–29. - PMC - PubMed