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雷洛昔芬:一种雌激素受体选择性调节剂

[Raloxifene: a selective modulator of estrogen receptors].

作者信息

van den Brûle F A, Kalbus M F, Gaspard U J

机构信息

Service de Gynécologie, CHU Liège.

出版信息

J Gynecol Obstet Biol Reprod (Paris). 1999 Dec;28(8):788-99.

Abstract

It has been demonstrated that postmenopausal hypoestrogenia induces numerous complications including osteoporosis and increased risk of cardiovascular disease. Oral or transdermal administration of estrogens can reduce these risks, but induces adverse effects. Recently, raloxifene, a new molecule from the benzothiophene family, has been demonstrated to prevent postmenopausal bone loss. It does not induce endometrial stimulation, and recent studies show that it could reduce breast cancer incidence. Its mode of action, consisting of mixed agonist and antagonistic estrogenic actions on different organs and systems, allows to classify it into the selective estrogen receptor modulator (SERM) family. In this review article, we will describe the characteristics of the molecule, its mode of action and the potential indications of its clinical use.

摘要

已证实绝经后雌激素缺乏会引发多种并发症,包括骨质疏松和心血管疾病风险增加。口服或经皮给予雌激素可降低这些风险,但会引发不良反应。最近,雷洛昔芬,一种来自苯并噻吩家族的新分子,已被证明可预防绝经后骨质流失。它不会引起子宫内膜刺激,并且最近的研究表明它可以降低乳腺癌发病率。其作用模式包括对不同器官和系统的混合激动剂和拮抗雌激素作用,使其可归类为选择性雌激素受体调节剂(SERM)家族。在这篇综述文章中,我们将描述该分子的特性、其作用模式及其临床应用的潜在适应症。

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