Compounds that can be described as selective estrogen receptor modulators (SERMs) have expanded dramatically over the past two decades. The ability of SERMs to act as estrogens in certain tissues while remaining inert or acting as an anti-estrogen in other tissues has opened up opportunities for treating specific estrogen-modulated diseases without accepting the risk of systemic estrogen activity. SERM development has resulted in significant therapeutic advances for breast cancer, osteoporosis and potentially other diseases associated with the menopause. After the publication of the Women's Health Initiative, interest in compound selectivity that reduces menopausal symptoms while protecting bone, breast, uterus and the heart has increased. Future SERMs may also have a therapeutic profile that can be tailored to specific patient populations, including men. This review paper summarizes the characteristics of different SERMs from various pharmacological categories and the feasibility and scope of their use for a large range of disease/health conditions.