Relugolix/Estradiol/Norethisterone (Norethindrone) Acetate: A Review in Symptomatic Uterine Fibroids

Abstract

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. Supplementary Information The online version contains supplementary material available at 10.1007/s40265-022-01790-4.

A comparative study on myomectomy and total hysterectomy in the treatment of perimenopausal uterine fibroids

“…Therefore, it can minimize the impact on ovarian function and improve life quality [8]. Myomectomy (laparoscopic-assisted) in patients with uterine fibroids hardly affects postoperative gastrointestinal function recovery or on its level [9]. Some have argued that laparoscopic myomectomy has less oxidative damage than open myomectomy.…”

Ultrasound-Guided Diagnosis of Multiple Uterine Fibroids in a Patient With Polycystic Ovaries and Treatment With Relugolix, Estradiol, and Norethisterone Acetate

“…Its mechanism of action involves inhibiting the production of gonadotropin-releasing hormone (GnRH), which reduces the production of estrogen and progesterone, the hormones that stimulate fibroid growth. It has been shown to significantly reduce menstrual bleeding while preserving bone mineral density in women with uterine fibroids [ 9 ]. Other medication treatment options include progestins, gonadotropin-releasing hormone agonists, and selective estrogen receptor modulators.…”

“…The medication was well tolerated and did not cause significant bone loss, a known adverse effect of similar therapies. With their once-daily dosing regimen, relugolix, estradiol, and norethisterone acetate provide a viable treatment option for premenopausal women suffering from symptomatic uterine fibroids [ 9 ].…”

Laparoscopic continuous seromuscular circumsuture for myomectomy: a real-world, retrospective, East-Asian cohort study

“…Treatment options for uterine fibroids include medical therapy, non-surgical methods and surgery. Medical therapy, such as hormonal contraceptives or gonadotropin-releasing hormone agonists, can relieve symptoms but may lead to adverse effect and be ineffective in reducing fibroid size 7 8. Non-surgical methods, such as uterine artery embolisation, focused ultrasonography or radiofrequency ablation, can be used as alternatives to surgery, but data about their long-term outcomes and safety are limited 9 10…”