Selective progesterone receptor modulators (SPRMs) are a new class of compounds developed to target the progesterone receptor (PR) with a mix of agonist and antagonist properties. These compounds have been introduced for the treatment of several gynecological conditions based on the critical role of progesterone in reproduction and reproductive tissues. In patients with uterine fibroids, mifepristone and ulipristal acetate have consistently demonstrated efficacy, and vilaprisan is currently under investigation, while studies of asoprisnil and telapristone were halted for safety concerns. Mifepristone demonstrated utility for the management of endometriosis, while data are limited regarding the efficacy of asoprisnil, ulipristal acetate, telapristone, and vilaprisan for this condition. Currently, none of the SPRMs have shown therapeutic success in treating endometrial cancer. Multiple SPRMs have been assessed for efficacy in treating PR-positive recurrent breast cancer, with in vivo studies suggesting a benefit of mifepristone, and multiple in vitro models suggesting the efficacy of ulipristal acetate and telapristone. Mifepristone, ulipristal acetate, vilaprisan, and asoprisnil effectively treated heavy menstrual bleeding (HBM) in patients with uterine fibroids, but limited data exist regarding the efficacy of SPRMs for HMB outside this context. A notable class effect of SPRMs are benign, PR modulator-associated endometrial changes (PAECs) due to the actions of the compounds on the endometrium. Both mifepristone and ulipristal acetate are effective for emergency contraception, and mifepristone was approved by the US Food and Drug Administration (FDA) in 2012 for the treatment of Cushing’s syndrome due to its additional antiglucocorticoid effect. Based on current evidence, SPRMs show considerable promise for treatment of several gynecologic conditions.

中文翻译：

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选择性黄体酮受体调节剂-机制和治疗效用。


选择性黄体酮受体调节剂 (SPRM) 是一类新型化合物，旨在针对黄体酮受体 (PR)，具有激动剂和拮抗剂的混合特性。基于孕酮在生殖和生殖组织中的关键作用，这些化合物已被用于治疗多种妇科疾病。对于子宫肌瘤患者，米非司酮和醋酸乌利司他始终有效，维拉普桑目前正在研究中，而阿索普尼和特拉普司酮的研究因安全问题而停止。米非司酮已被证明可用于治疗子宫内膜异位症，而有关阿索普利尼、醋酸乌利司他、特拉普司酮和维拉普桑治疗这种疾病的疗效的数据有限。目前，没有一种 SPRM 在治疗子宫内膜癌方面取得成功。已对多种 SPRM 治疗 PR 阳性复发性乳腺癌的功效进行了评估，体内研究表明米非司酮的益处，多种体外模型表明醋酸乌利司他和特拉司酮的功效。米非司酮、醋酸乌利司他、维拉普生和阿索普尼可有效治疗子宫肌瘤患者的严重月经出血 (HBM)，但关于 SPRM 在这种情况下对 HMB 的疗效的数据有限。 SPRM 的一个显着类别效应是良性、PR 调节剂相关的子宫内膜变化 (PAEC)，这是由于化合物对子宫内膜的作用所致。米非司酮和醋酸乌利司他对于紧急避孕均有效，并且米非司酮由于其额外的抗糖皮质激素作用于2012年被美国食品和药物管理局（FDA）批准用于治疗库欣综合征。 根据目前的证据，SPRM 在治疗多种妇科疾病方面显示出巨大的前景。