Targeted anti-estrogens to treat and prevent diseases in women.
The estrogen receptor has been successfully targeted with the anti-estrogen tamoxifen to treat all stages of breast cancer. Because tamoxifen is a partial agonist, it exhibits target-site specificity: it acts as an anti-estrogen in the breast to inhibit tumor growth, while exhibiting estrogenic effects on bones and lipid metabolism. Therefore, tamoxifen has the added benefit of maintaining bone density and reducing the risk of myocardial infarction in postmenopausal women. However, undesirable side effects of tamoxifen preclude its use as a hormone replacement therapy for otherwise healthy women. New anti-estrogens are currently being developed that may prevent osteoporosis, breast and endometrial cancer, and reduce the risk of myocardial infarction.
Tonetti
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DA
Robert H. Lurie Cancer Center, Northwestern University Medical School, Chicago, IL 60611, USA.
Jordan
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VC
D000818:Animals; D001483:Base Sequence; D001943:Breast Neoplasms / Q000188:drug therapy*; D003327:Coronary Disease / Q000517:prevention & control; D016889:Endometrial Neoplasms / Q000139:chemically induced; D004965:Estrogen Antagonists / Q000009:adverse effects / Q000627:therapeutic use*; D015914:Estrogen Replacement Therapy; D005260:Female; D006801:Humans; D008969:Molecular Sequence Data; D015663:Osteoporosis, Postmenopausal / Q000517:prevention & control; D011960:Receptors, Estrogen / Q000378:metabolism; D013629:Tamoxifen / Q000627:therapeutic use*
D004965:Estrogen Antagonists; D011960:Receptors, Estrogen; D013629:Tamoxifen