Spitz Irving M
Institute of Hormone Research, Shaare Zedek Medical Center, PO Box 3235, Jerusalem, 91031, Israel.
Expert Opin Investig Drugs. 2003 Oct;12(10):1693-707. doi: 10.1517/13543784.12.10.1693.
Since the discovery of the antiprogestin RU 486 (mifepristone), other compounds have been synthesised that function as pure progesterone antagonists or progesterone receptor modulators. The latter are mixed agonists-antagonists. Mifepristone is usually used to terminate pregnancy but these compounds have numerous other applications in female healthcare. Mifepristone is an excellent agent for emergency contraception. Many progesterone antagonists and progesterone receptor modulators display antiproliferative effects on the endometrium and thus have application in the treatment of endometriosis and uterine myoma without being associated with hypoestrogenism and bone loss. They also have contraceptive potential by suppressing follicular development, blocking the luteinising hormone surge and retarding endometrial maturation. Finally, they have clinical application in GeneSwitch system, a plasmid-based method enabling controlled expression of specific genes (e.g., erythropoietin) using a progesterone antagonist as the inducer.
自从发现抗孕激素RU 486（米非司酮）以来，已合成了其他化合物，这些化合物可作为纯孕激素拮抗剂或孕激素受体调节剂发挥作用。后者是混合激动剂-拮抗剂。米非司酮通常用于终止妊娠，但这些化合物在女性医疗保健中有许多其他应用。米非司酮是紧急避孕的优良药物。许多孕激素拮抗剂和孕激素受体调节剂对子宫内膜具有抗增殖作用，因此可用于治疗子宫内膜异位症和子宫肌瘤，而不会导致雌激素缺乏和骨质流失。它们还具有避孕潜力，可通过抑制卵泡发育、阻断促黄体生成素高峰和延缓子宫内膜成熟来实现。最后，它们在基因开关系统中有临床应用，这是一种基于质粒的方法，可使用孕激素拮抗剂作为诱导剂来控制特定基因（如促红细胞生成素）的表达。
