Raloxifene: a selective estrogen receptor modulator

Abstract

Raloxifene is a selective estrogen receptor modulator that produces both estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue. Because of its tissue selectivity, raloxifene may have fewer side effects than are typically observed with estrogen therapy. The most common adverse effects of raloxifene are hot flushes and leg cramps. The drug is also associated with an increased risk of thromboembolic events. The beneficial estrogenic activities of raloxifene include a lowering of total and low-density lipoprotein cholesterol levels and an augmentation of bone mineral density. Raloxifene has been labeled by the U.S. Food and Drug Administration for the prevention of osteoporosis. However, its effects on fracture risk and its ability to protect against cardiovascular disease have yet to be determined. Studies are also being conducted to determine its impact on breast and endometrial cancer reduction.