An antiestrogen is a compound that blocks the action of estrogen. Most synthetic antiestrogens have agonistic or antagonistic activity depending on the tissue and the endogenous estrogen mileu. The triphenylethylene derivatives, clomiphene and tamoxifen, are the antiestrogens in greatest clinical use. Their biologic effects, clinical indications, and risks are reviewed. Novel antiestrogens which are beginning to be studied clinically include the benzothiophene derivative, raloxifene and the "pure" antiestrogens such as ICI 182,780. New clinical indications for existing compounds as well as the development of novel antiestrogens may lead to better treatment options for endocrine-dependent conditions.