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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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Authors and Affiliations

  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Julia A. Balfour & Karen L. Goa

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  1. Julia A. Balfour
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  2. Karen L. Goa
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Correspondence to Julia A. Balfour.

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Balfour, J.A., Goa, K.L. Raloxifene. Drugs Aging 12, 335–341 (1998). https://doi.org/10.2165/00002512-199812040-00006

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  • DOI: https://doi.org/10.2165/00002512-199812040-00006

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