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选择性雌激素受体调节剂:进展与未来展望。

SERMs: progress and future perspectives.

机构信息

Department of Obstetrics and Gynecology, Columbia University Medical Center, New York, NY 10032, USA.

出版信息

Maturitas. 2010 Oct;67(2):129-38. doi: 10.1016/j.maturitas.2010.05.009. Epub 2010 Jun 26.

DOI:10.1016/j.maturitas.2010.05.009
PMID:20580502
Abstract

Selective estrogen receptor modulators (SERMs) interact with estrogen receptors as agonists or antagonists depending on the target tissue. Currently available SERMs are used to treat and prevent breast cancer and osteoporosis, to treat ovulatory dysfunction in women, and for contraception. Because current therapies do not adequately treat menopausal symptoms, the search continues for the optimal SERM for postmenopausal women, which would relieve hot flushes, treat vaginal atrophy, and prevent fractures, while protecting the endometrium, breast, and cardiovascular system. Future use of SERMs may also include their use in a tissue selective estrogen complex (TSEC), a therapy that combines a SERM with estrogen(s), designed to deliver the efficacy of each component with improved overall tolerability for the treatment of postmenopausal women. The future of SERMs may also include their use in men for the treatment of osteoporosis and various syndromes associated with secondary hypogonadism and possibly prostate cancer. Continued research should allow the full potential of SERMs to be uncovered.

摘要

选择性雌激素受体调节剂(SERMs)根据靶组织与雌激素受体相互作用为激动剂或拮抗剂。目前可用的 SERMs 用于治疗和预防乳腺癌和骨质疏松症,治疗女性排卵功能障碍,并用于避孕。由于目前的治疗方法不能充分治疗更年期症状,因此仍在寻找用于绝经后妇女的最佳 SERM,该药物将缓解热潮红,治疗阴道萎缩,并预防骨折,同时保护子宫内膜、乳房和心血管系统。SERMs 的未来用途还可能包括将其用于组织选择性雌激素复合物(TSEC)中,这种治疗方法将 SERM 与雌激素(estrogen)结合使用,旨在提高每种成分的疗效,同时提高整体耐受性,用于治疗绝经后妇女。SERMs 的未来用途还可能包括将其用于男性治疗骨质疏松症和各种与继发性性腺功能减退症相关的综合征,以及可能的前列腺癌。持续的研究应能发掘 SERMs 的全部潜力。

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