[SERMs和子宫]。

Annales de medecine interne Pub Date : 2003-03-01
Philippe Touraine
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引用次数: 0

摘要

子宫是卵巢合成的性类固醇的靶器官之一。众所周知,雌激素能刺激子宫内膜细胞增殖,而黄体酮对子宫内膜有抗雌激素分泌作用。在过去的十年中,新的抗雌激素药物对子宫的作用重新引起了人们的兴趣,但不仅仅是为了实现预防或治愈子宫肿瘤的新治疗策略。新的化合物被开发出来,用于其他组织,如乳房,但很快就发现它们是子宫疾病的来源。一个明显的例子是他莫昔芬,它对乳房组织有强大的抗雌激素作用。然而,根据靶组织的不同,人们希望这种表现为拮抗剂或激动剂的化合物对子宫具有抗雌激素作用,相反,对骨骼和血管组织具有激动性雌激素保护作用。这种方法逐渐导致SERMs(选择性雌激素受体调节剂)的发展,这是一种调节雌激素作用的非甾体化合物。这类新药的第一个成员是雷洛昔芬(raloxifen),在法国以品牌Evista上市,它对椎体骨具有雌激素作用,因此被授权用于伴有或不伴有骨折的椎体骨质疏松症患者。因此,雷洛昔芬至少对小梁骨有有益的雌激素作用,而对子宫和乳房有抗雌激素作用。今天的目标是继续开发SERM家族的新化合物,这些化合物在不同的身体组织中具有良好的靶向性和良好的理解,激动和/或拮抗作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[SERMs and uterus].

The uterus is one of the target organs of sexual steroids synthesized in the ovary. Estrogen is known to stimulate cell proliferation in the endometrium while progesterone has an anti-estrogenic secretory effect on this tissue. Renewed interest in the action of new anti-estrogenic agents on the uterus has arisen over the last decade, but not simply in order to achieve new therapeutic strategies for the prevention or cure of uterine tumors. New compounds were developed for their action on other tissues such as the breast, but it rapidly became clear that they were a source of uterine disease. A clear example is tamoxifen which has a powerful anti-estrogenic effect on breast tissue. It was hoped however that this compound, which behaves either like an antagonist or an agonist, depending on the target tissue, could have an anti-estrogenic effect on the uterus and on the contrary an agonistic estrogenic protective effect on bony and vascular tissue. This approach progressively led to the development of SERMs (Selective Estrogen Receptor Modulators), non-steroidal compounds modulating the action of estrogens. The first member of this new pharmaceutical class was raloxifen, marketed in France under the brand name Evista, which has an estrogenic effect on vertebral bone, warranting its authorization for use in patients with vertebral osteoporosis with or without fracture. Raloxifen thus has a beneficial estrogenic effect, at least on trabecular bone, and an anti-estrogenic effect on the uterus and breast. The goal today is to continue the development of new compounds in the SERM family with well targeted, and well understood, agonistic and/or antagonistic actions on different body tissues.

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