Raloxifene

Abstract

Raloxifene, a bezothiophene binds as a selective estrogen receptor modulator that binds to estrogen receptors inducing several tissue specific effects. As a SERM Raloxifene mimics the activity of estrogen in some specific tissues while inhibiting it in others. Raloxifene is structurally, chemically, and in its tissue specific action different from tamoxifen. Raloxifene shows estrogen agonistic effects on bone and lipids, but fails to show estrogenic effects on uterus and breast. Raloxifen is absorbed rapidly after oral intake, and is highly bound to plasma proteins. After first-pass metabolism plasma elimination half-life of the compound in humans is 27.7 hours. Raloxifene is registered for the treatment of osteoporosis. The following information provides a summary of the known effects of Raloxifene in bone and lipid metabolism, endometrium and breast.