a Department of Obstetrics and Gynecology, Division of Midlife Health , University of Virginia Health System , Charlottesville , VA , USA.
Climacteric. 2019 Apr;22(2):140-147. doi: 10.1080/13697137.2019.1568403.
Selective estrogen receptor modulators (SERMs) are synthetic non-steroidal agents which have variable estrogen agonist and antagonist activities in different target tissues. Tamoxifen is an anti-estrogen in the breast used for treatment and prevention of breast cancer, with estrogen agonist activity in the uterus. Raloxifene prevents and treats osteoporosis and prevents breast cancer, and can be safely combined with vaginal but not systemic estrogen. The tissue selective estrogen complex combines conjugated equine estrogens (CEE) with the SERM bazedoxifene (BZA). The five Selective Estrogen Menopause and Response to Therapy studies, with up to 2 years of data, demonstrated that CEE/BZA 0.45 mg/BZA 20 mg improved vasomotor symptoms and vulvovaginal atrophy, prevented bone loss, and was neutral on breast tenderness, breast density, with breast cancer incidence similar to placebo. Protection against estrogen-induced endometrial hyperplasia and cancer was found, with similar amenorrhea rates to placebo. Ospemifene is approved to treat dyspareunia, with potential benefits on bone and the breast, while lasofoxifene is being developed to treat resistant estrogen receptor-positive breast cancer in women. Estetrol is an estrogen synthesized exclusively during pregnancy by the human fetal liver and initially considered a weak estrogen, but it appears to have dual weak estrogenic/anti-estrogenic features.
选择性雌激素受体调节剂 (SERMs) 是合成的非甾体类药物，在不同的靶组织中具有可变的雌激素激动剂和拮抗剂活性。他莫昔芬是一种用于治疗和预防乳腺癌的乳房抗雌激素药物，在子宫中有雌激素激动剂活性。雷洛昔芬可预防和治疗骨质疏松症并预防乳腺癌，并且可以与阴道雌激素安全联合使用，但不能与全身雌激素联合使用。组织选择性雌激素复合物将结合雌激素（CEE）与 SERM 巴多昔芬（BZA）结合在一起。五项选择性雌激素绝经和治疗反应研究，最长达 2 年的数据表明，CEE/BZA 0.45mg/BZA 20mg 改善了血管舒缩症状和阴道萎缩，预防了骨质流失，并且对乳房触痛、乳房密度呈中性，乳腺癌发病率与安慰剂相似。发现对雌激素引起的子宫内膜增生和癌症有保护作用，与安慰剂的闭经率相似。奥昔孕诺芬被批准用于治疗性交困难，可能对骨骼和乳房有益，而拉索昔芬正在开发中，用于治疗女性对雌激素受体阳性乳腺癌的耐药性。雌三醇是一种仅在妊娠期间由人胎儿肝脏合成的雌激素，最初被认为是一种弱雌激素，但它似乎具有双重弱雌激素/抗雌激素特性。
