Current understanding of selective estrogen receptor modulators

Abstract

Despite the variety of selective estrogen receptor modulators of different classes of compounds and their active use for the treatment of hormone-dependent breast cancer, climacteric conditions, and polycystic ovary syndrome, as well as for ovulation stimulation and for prevention and treatment of postmenopausal osteoporosis and vertebral fractures, there are a number of serious side effects, such as thromboembolic disorders, uterine cancer and endometrial cancer. Among the selective estrogen receptor modulators used in clinical practice, it is worth noting: Raloxifene, for the prevention and treatment of postmenopausal osteoporosis and vertebral fractures; Tamoxifen, for the treatment of breast cancer; Toremifene, for the treatment of metastatic breast cancer in postmenopausal women; Lasofoxifene, for the treatment of osteoporosis; Bazedoxifene, for the treatment and prevention of postmenopausal osteoporosis; Clomiphene, for the treatment of anovulatory infertility; Ospemifene, for the treatment of moderate to severe dyspareunia associated with postmenopausal syndrome. An ongoing search for an effective and safe selective estrogen receptor modulator for the treatment of endometriosis is currently underway.