Springer Nature, Mairangi Bay, Private Bag 65901, Auckland, 0754, New Zealand.
Drugs. 2022 Oct;82(15):1549-1556. doi: 10.1007/s40265-022-01790-4. Epub 2022 Nov 4.
An oral fixed-dose combination of relugolix/estradiol/norethisterone (also known as norethindrone) acetate (Ryeqo; Myfembree) has been approved for the management of heavy menstrual bleeding associated with uterine fibroids in the USA and management of moderate to severe symptoms of uterine fibroids in the EU. Relugolix is a gonadotropin releasing hormone (GnRH) receptor antagonist that decreases serum estradiol and progesterone concentrations to postmenopausal levels. The addition of estradiol/norethisterone acetate to relugolix ameliorates relugolix-induced bone loss and hot flush. In the two phase 3 LIBERTY trials, relugolix + estradiol/norethisterone substantially decreased menstrual bleeding and improved a range of other uterine fibroid symptoms in women with uterine fibroids-associated heavy menstrual bleeding. The combination was generally well tolerated, with vasomotor symptoms being the most common adverse reaction. Treatment with this combination for over up to 2 years did not induce a clinically meaningful bone loss in the majority of women. Relugolix/estradiol/norethisterone acetate, with its convenient once-daily administration, is a useful addition to current pharmacological treatment options for premenopausal women with symptomatic uterine fibroids.
一种口服固定剂量的瑞戈非尼/雌二醇/炔诺酮（也称为炔诺酮）醋酸酯（Ryeqo；Myfembree）已在美国获批用于治疗与子宫肌瘤相关的重度月经过多，在欧盟获批用于治疗中度至重度子宫肌瘤症状。瑞戈非尼是一种促性腺激素释放激素（GnRH）受体拮抗剂，可降低血清雌二醇和孕激素浓度至绝经后水平。雌二醇/炔诺酮醋酸酯与瑞戈非尼联合使用可改善瑞戈非尼引起的骨质流失和热潮红。在两项 3 期 LIBERTY 试验中，瑞戈非尼+雌二醇/炔诺酮显著减少了月经出血，并改善了与子宫肌瘤相关的重度月经过多的女性的一系列其他子宫肌瘤症状。该联合用药通常具有良好的耐受性，血管舒缩症状是最常见的不良反应。在大多数女性中，该联合用药超过 2 年的治疗并未导致临床上有意义的骨质流失。瑞戈非尼/雌二醇/炔诺酮醋酸酯，每日一次给药方便，为有症状的子宫肌瘤的绝经前妇女提供了一种有用的治疗选择。
