新型孕激素及抗孕激素国外研发进展

Advance in new generation of progestin and anti-progestin

文中介绍新一代孕激素和抗孕激素的特点和国外研发进展,为我国新型避孕药研发提供参考。通过查阅国外近期文献,总结并介绍新一代孕激素诺美孕酮(nomegestrol acetate)、烯诺孕酮(nestor-one)、曲美孕酮(trimegestone)、屈螺酮(drospirnone)、地诺孕素(dienogest)以及新型抗孕激素优力司(ulip-ristal acetate)的药理作用特点和研发进展。新一代孕激素/抗孕激素与孕酮受体的结合更具选择性和专一性,降低了第1～3代孕激素因雄激素活性而导致的多种不良反应,总体上提高了避孕药的安全性和耐受性;但个别孕激素也表现出新的不良反应。我国应加大投入对新型孕激素和抗孕激素及新剂型的研发,同时也应预测到化合物结构改造时可能带来的新的不良反应。

The development of new generation of progestin and anti-progestin compounds was reviewed in this paper. Based on R ＆ D achievements of new generation progestin and anti-progestin in recent years, we summarized the pharmacological effects and the applications of drospirenone, dienogest, nestorone, nomegestrol ace- tate, trimegestone and ulipristal acetate. The ability of the new generation of progestin and anti-progestin binding to progesterone receptor has been greatly improved. The natures of the new progestin are closer to native steroid hormones. They have no androgen, estrogen or glucocorticoid activities, which greatly improved the safety of oral contraceptives and HRT, and the tolerance. Some of progestin also has potential adverse reaction. China should speed up the development of the new generation of progestin/anti-progestin, while some new side-effects should be considered in advance.