Raloxifene

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Abstract
▴ Raloxifene is a selective estrogen receptor modulator which mimics the effects of estrogens on bone and blood lipid levels without stimulatory effects on the breast or uterus. ▴ Raloxifene inhibits estrogen-dependent proliferation of human breast cancer cells in vitro and development of induced mammary tumours in rats in vivo. ▴ Raloxifene inhibits bone resorption induced by estrogen deficiency in murine and human studies and lowers serum cholesterol levels. In clinical studies in postmenopausal women, raloxifene 60 mg/day for 2 years significantly increased bone mineral density compared with placebo. ▴ In comparative clinical studies, raloxifene 60 mg/day had more modest effects than conjugated estrogens 0.625 mg/day on bone resorption and formation parameters and appeared to be less effective in increasing bone mineral density. ▴ In older postmenopausal women with existing bone fractures, raloxifene 60 or 120 mg/day for 1 year produced modest increases in bone mineral density. ▴ The most common treatment-related adverse events in raloxifene recipients were hot flushes and leg cramps. The risk of venous thromboembolic events is increased during raloxifene therapy. In contrast with conjugated estrogens 0.625 mg/day, raloxifene 200 or 600 mg/day for 8 weeks or 150 mg/day for 1 year did not produce endometrial proliferation.

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