The estrogen receptor has been successfully targeted with the anti-est
rogen tamoxifen to treat all stages of breast cancer. Because tamoxife
n is a partial agonist, it exhibits target-site specificity: it acts a
s an anti-estrogen in the breast to inhibit tumor growth, while exhibi
ting estrogenic effects on bones and lipid metabolism. Therefore, tamo
xifen has the added benefit of maintaining bone density and reducing t
he risk of myocardial infarction in postmenopausal women. However, und
esirable side effects of tamoxifen preclude its use as a hormone repla
cement therapy for otherwise healthy women. New anti-estrogens are cur
rently being developed that may prevent osteoporosis, breast and endom
etrial cancer, and reduce the risk of myocardial infarction.