Selective estrogen receptor modulators (SERMS): keys to understanding their function

Selective estrogen receptor modulators (SERMs) are an increasingly important therapeutic modality that are used by clinicians on a daily basis. Unfortunately, clinicians have a limited understanding regarding the underlying mechanism(s) of how SERMs function and their increasingly useful role in the treatment of estrogen-responsive target tissues such as the breast, bone, vagina, uterine endometrium, and brain. This review will provide a basic understanding of our current knowledge of SERM pharmacodynamics and will highlight the clinical applications of Food and Drug Administration-approved SERMs in the treatment of vasomotor symptoms, osteoporosis, genitourinary syndrome of menopause, infertility, and breast cancer and its prevention. SERMs under development and natural phytoestrogens will also be reviewed.