Benagiano Giuseppe, Bastianelli Carlo, Farris Manuela
Dean University 'la Sapienza', Postgraduate School of Gynaecology and Obstetrics, Policlinico Umberto I degrees , Viale Regina Margherita 245, 00161 Roma, Italy.
Expert Opin Pharmacother. 2008 Oct;9(14):2459-72. doi: 10.1517/14656566.9.14.2459.
A large number of synthetic compounds known as selective progesterone receptor modulators can bind to progesterone receptors: the ligands exhibit a spectrum of activities ranging from pure antagonism to a mixture of agonism and antagonism.
Only a dozen or so selective progesterone receptor modulators have been tested to any significant extent: among them are mifepristone (RU 486), asoprisnil (J867), onapristone (ZK 98 299), ulipristal (CDB 2914), Proellex() (CDB 4124), ORG 33628 and ORG 31710. Their clinical applications during pregnancy are discussed.
A careful evaluation of existing major review papers and recently published articles was carried out focusing on mifepristone, the most widely studied selective progesterone receptor modulator, which was first used for the voluntary interruption of an early gestation. Other selective progesterone receptor modulators, especially those with partial agonist action, have shown little activity during pregnancy in animal models.
RESULTS/CONCLUSIONS: Besides early and late voluntary interruption of gestation, selective progesterone receptor modulators have been tested in a variety of obstetrical situations: to obtain a ripening of the cervix, for the medical management of early embryonic loss and foetal death, for the induction of labour at term and for the medical treatment of extra-uterine pregnancies. The only applications that seem worthy of large-scale utilisation during pregnancy are voluntary interruption of early and late gestation, medical management of early delayed miscarriage and late foetal demise.
大量被称为选择性孕激素受体调节剂的合成化合物能够与孕激素受体结合:这些配体表现出一系列活性,从纯粹的拮抗作用到激动和拮抗作用的混合。
仅有大约十二种选择性孕激素受体调节剂得到了任何显著程度的测试:其中包括米非司酮(RU 486)、阿索普瑞诺(J867)、奥那司酮(ZK 98 299)、乌利司他(CDB 2914)、Proellex()(CDB 4124)、ORG 33628和ORG 31710。讨论了它们在孕期的临床应用。
对现有主要综述论文和近期发表的文章进行了仔细评估,重点关注米非司酮,这是研究最广泛的选择性孕激素受体调节剂,它最初用于早期妊娠的自愿终止。其他选择性孕激素受体调节剂,尤其是那些具有部分激动作用的,在动物模型孕期几乎没有活性。
结果/结论:除了早期和晚期妊娠的自愿终止外,选择性孕激素受体调节剂还在多种产科情况中进行了测试:用于使宫颈成熟、早期胚胎丢失和胎儿死亡的药物治疗、足月引产以及宫外孕的药物治疗。孕期似乎值得大规模应用的唯一情况是早期和晚期妊娠的自愿终止、早期稽留流产和晚期胎儿死亡的药物治疗。