Clinical pharmacology of selective estrogen receptor modulators

Observations of the pharmacology of tamoxifen and related compounds have le ad to the concept of selective estrogen receptor modulators (SERMs). This n ew class of drug displays estrogen agonist or antagonist effects in a tissu e-dependent manner and appears to offer an alternative to hormone replaceme nt therapy for the prevention and treatment of osteoporosis and cardiovascu lar disease in postmenopausal women. Moreover, the estrogen antagonist acti ons of SERMs on breast tissue may also provide a protective effect against breast cancer. Although tamoxifen therapy reduces plasma cholesterol levels and maintains bone density, it is also associated with an increased risk o f endometrial cancer, pulmonary embolism and deep vein thrombosis. This has lead to the development of newer SERMs which will hopefully lack these adv erse effects of tamoxifen. These compounds promise a new era of disease pre vention in the aging woman and their therapeutic potential is currently bei ng evaluated in large-scale clinical trials.