Baker V L, Jaffe R B
Department of Obstetrics, Gynecology and Reproductive Sciences, University of California, San Francisco, USA.
Obstet Gynecol Surv. 1996 Jan;51(1):45-59. doi: 10.1097/00006254-199601000-00021.
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.
抗雌激素是一种能阻断雌激素作用的化合物。大多数合成抗雌激素根据组织和内源性雌激素环境具有激动或拮抗活性。三苯乙烯衍生物氯米芬和他莫昔芬是临床上使用最广泛的抗雌激素。本文综述了它们的生物学效应、临床适应证及风险。开始进行临床研究的新型抗雌激素包括苯并噻吩衍生物雷洛昔芬和“纯”抗雌激素，如ICI 182,780。现有化合物的新临床适应证以及新型抗雌激素的研发可能会为内分泌依赖性疾病带来更好的治疗选择。
