Selective Estrogen Receptor Modulators (SERMs): State of the Art

Abstract

The function of selective estrogen receptor modulators (SERMs) is to produce specific positive effects on certain target tissues with estrogen receptors and negative or neutral effects on other tissues with estrogen receptors but in which no action is required. Relevant articles in English are published between 1980 and 2018, which have been identified through the PubMed database (search string “selective estrogen receptor modulator or SERM”). Tamoxifen is a drug used in the treatment of hormone-dependent breast cancer and in primary prevention in women at high risk of developing the disease. Raloxifene is the first SERM approved to prevent and treat osteoporosis. Raloxifene is also as effective as tamoxifen in reducing the risk of breast cancer in postmenopausal women. Bazedoxifene has been shown to be effective in reducing vertebral and, in a high-risk group, non-vertebral fractures. Ospemifene is the first SERM for the treatment of dyspareunia in the USA and for patients with vulvovaginal atrophy who are not eligible for estrogen therapy in Europe. SERMs have a specific action different from that of estrogens. They all have a unique tissue-specific effect that make them different from each other and therefore have different applications.