Raloxifen

Abstract

Raloxifene belongs to the group of selective estrogen receptor modulators (SERMs). It interacts with both estrogen receptor α and β, but the postreceptor responses differ from those of estrogens: Raloxifene exerts tissue specific responses that differ from estrogens. The drug increases bone mass by 2-3% and inhibits the risk of subsequent vertebral fractures by 30-50%. Raloxifene reduces the risk of breast cancer by 76% after treatment for four years and builds an atrophic endometrium without any bleedings. Furthermore, the risk of endometrial cancer is not incresased. The drug exerts positive effects on plasma lipids, but the effects of these changes on subsequent risk of myocardial infarction and cardiovascular death are still unknown. The main side effects are leg cramps, increases in hot flushes and peripherale oedema. Like estrogen, the drug increases the relative risk for venous thrombosis by a factor three.