摘要
非甾体抗雌激素他莫昔芬(tamoxifen,TAM)用于乳腺癌的抗激素治疗具有确定的价值,但他莫昔芬类药物对某些组织有雌激素样作用,即其部分激动活性,导致一些非理想的作用,如子宫内膜增生和增加子宫内膜癌的发病率。近年来国外开发了一类新的抗雌激素,因不具有部分激动活性,在治疗雌激素依赖性疾病中具有优越性。在合成的一系列此类化合物中,AstraZeneca公司的Fulvestrant(ICI 182780),因其与雌激素受体(ER)有高亲和力和高活性,被选中做进一步临床评价。本文对Fulvestrant的药理作用机理、临床前研究和临床研究结果以及其临床应用前景等做一综述。
Clinical experience with the nonsteroidal antiestrogen tamoxifen hasestablished unequivocally the value of antiestrogen therapy in the treatment ofpatients with breast carcinoma. But tamoxifen-like drugs have estrogen-like actionson certain tissues and their intrinsic partial-agonist effects may have undesiredconsequences, such as increased endometrial proliferation, a slightly increased riskof endometrial carcinoma. A new class of specific antiestrogen without any agonisteffects may have advantages over tamoxifen in the treatment of patients withestrogen dependent disease. The search for such a drug revealed a number ofcompounds with the appropriate effect, of which fulvestrant (ICI l82780,AstraZeneca) was selected for clinical evaluation because of its greater potencyand affinity for the estrogen receptor (ER). In this paper, we reviewed the mode ofaction of fulvestrant, preclinical data, clinical data and clinical uses.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2002年第2期156-158,共3页
The Chinese Journal of Clinical Pharmacology
