Cano A, Hermenegildo C
Department of Pediatrics, Obstetrics and Gynecology, Facultad de Medicina, Valencia, Spain.
Hum Reprod Update. 2000 May-Jun;6(3):244-54. doi: 10.1093/humupd/6.3.244.
The ideal selective oestrogen receptor modulator (SERM) would retain an oestrogen-like effect on the bones, the heart and cardiovascular apparatus, and the central nervous system, while acting as an anti-oestrogen on the breast and the genital tract. It seems, however, that such a compound is not available for clinical use yet. The uterine tissue, and particularly the endometrium, defines an area of special interest in the SERM action, since endometrial hyperplasia and cancer has been linked to agonistic oestrogen effects. Additionally, tamoxifen, the SERM which accumulates most of the clinical experience, has been associated with stimulatory effects on endometrium, including the development of cancer. In contrast, the more recent benzothiophenes, led by raloxifene, seem to operate as endometrial antagonists, thus providing an interesting alternative for clinical use. This review analyses the endometrial action of tamoxifen, including the information gathered from laboratory models, the observed endometrial effects in women using tamoxifen, and the epidemiological and molecular data which link the use of tamoxifen with endometrial cancer. A parallel examination of the raloxifene data presents the available experimental and clinical information, suggesting the endometrial neutrality of this compound.
理想的选择性雌激素受体调节剂（SERM）应对骨骼、心脏及心血管系统和中枢神经系统具有类似雌激素的作用，而对乳腺和生殖道则发挥抗雌激素作用。然而，目前似乎尚无此类化合物可供临床使用。子宫组织，尤其是子宫内膜，是SERM作用中一个特别受关注的领域，因为子宫内膜增生和癌症与雌激素的激动效应有关。此外，他莫昔芬是积累了最多临床经验的SERM，已被发现对子宫内膜有刺激作用，包括引发癌症。相比之下，以雷洛昔芬为首的较新的苯并噻吩类药物似乎对子宫内膜起拮抗作用，从而为临床应用提供了一个有趣的选择。本综述分析了他莫昔芬对子宫内膜的作用，包括从实验室模型收集的信息、使用他莫昔芬的女性中观察到的子宫内膜效应，以及将他莫昔芬的使用与子宫内膜癌联系起来的流行病学和分子数据。对雷洛昔芬数据的平行研究展示了现有的实验和临床信息，表明该化合物对子宫内膜呈中性作用。
