Selective estrogen receptor modulators: a new category of compounds to extend postmenopausal women's health.
Selective estrogen receptor modulators (SERMs) are a new category of therapeutic agents, which bind with high affinity to estrogen receptors and mimic the effect of estrogens in some tissues but act as estrogen antagonists in others. Tamoxifen, a triphenylethylene derivative, was the first clinically available SERM. It is a potent anti-estrogen in the breast, and its use in breast cancer patients has made it the most widely prescribed antineoplastic drug worldwide. It has estrogen-like activity on bone metabolism, as well as cholesterol reduction. However, its ability to produce proliferation, and polyp formation, and even carcinomas, in the endometrium is well known. A new SERM, raloxifene, a benzothiopene derivative, has a clinical profile similar to tamoxifen's. However, preclinical as well as clinical studies reveal that unlike tamoxifen it is a pure anti-estrogen in the uterus. It has recently been FDA approved for prevention of osteoporosis in postmenopausal women. This report reviews pertinent preclinical and currently available clinical studies about this new SERM and discusses clinical applicability.
Goldstein
S R
SR
Department of Obstetrics and Gynecology, New York University School of Medicine, New York 10016, USA.
D015519:Bone Density / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy / Q000517:prevention & control; D002792:Cholestyramine Resin / Q000494:pharmacology; D016889:Endometrial Neoplasms / Q000517:prevention & control; D004965:Estrogen Antagonists / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D006620:Hip Fractures / Q000517:prevention & control; D020249:Hormone Replacement Therapy / Q000009:adverse effects*; D006801:Humans; D008875:Middle Aged; D015663:Osteoporosis, Postmenopausal / Q000517:prevention & control*; D020849:Raloxifene Hydrochloride / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology* / Q000627:therapeutic use; D013629:Tamoxifen / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D014481:United States; D014486:United States Food and Drug Administration; D014859:Warfarin / Q000494:pharmacology
D004965:Estrogen Antagonists; D020845:Selective Estrogen Receptor Modulators; D013629:Tamoxifen; D002792:Cholestyramine Resin; D020849:Raloxifene Hydrochloride; D014859:Warfarin