Paton D M
Emeritus Professor of Pharmacology, University of Auckland, Emeritus Professor of Oral Biology, University of Alberta, Canada.
Drugs Today (Barc). 2014 May;50(5):357-64. doi: 10.1358/dot.2014.50.5.2134451.
Ospemifene is a third-generation selective estrogen receptor modulator (SERM), structurally closely related to toremifene. Clinical studies in postmenopausal women with vulvovaginal atrophy demonstrated that it produced significant improvements in the structure of the vagina and its pH, and significantly reduced dyspareunia, the main complaint of the women treated. Preclinical studies demonstrated that ospemifene, unlike tamoxifen, did not produce DNA adducts, suggesting that it has less carcinogenic potential than tamoxifen. Preclinical and clinical studies showed that ospemifene has an agonist action on bone and reduced the growth of all breast cancer models in animal studies, providing they expressed estrogen receptor-α. Ospemifene had minimal effects on the endometrium of postmenopausal women. Ospemifene 60 mg once a day was approved by the U.S. Food and Drug Administration in February 2013 for women with moderate to severe dyspareunia.
奥司米芬是一种第三代选择性雌激素受体调节剂（SERM），在结构上与托瑞米芬密切相关。针对绝经后外阴阴道萎缩女性的临床研究表明，它能显著改善阴道结构及其pH值，并显著减轻性交困难，这是接受治疗女性的主要诉求。临床前研究表明，与他莫昔芬不同，奥司米芬不会产生DNA加合物，这表明其致癌潜力低于他莫昔芬。临床前和临床研究表明，奥司米芬对骨骼具有激动作用，并且在动物研究中能抑制所有表达雌激素受体α的乳腺癌模型的生长。奥司米芬对绝经后女性的子宫内膜影响极小。2013年2月，美国食品药品监督管理局批准每天一次服用60毫克奥司米芬用于治疗中度至重度性交困难的女性。
