Combination medication
Relugolix/estradiol/norethisterone acetate, sold under the brand names Myfembree and Ryeqo, is a fixed-dose combination hormonal medication which is used for the treatment of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) and for moderate to severe pain associated with endometriosis.[7][8][9] It contains relugolix, an orally active gonadotropin-releasing hormone antagonist (GnRH antagonist), estradiol, an estrogen, and norethisterone acetate, a progestin.[7][8] The medication is taken by mouth.[7]
The most common side effects of the medication include hot flushes, excessive sweating or night sweats, uterine bleeding, hair loss or thinning, and decreased interest in sex.[7]
The medication was approved for medical use in the United States in May 2021,[7][10][11] and in the European Union in July 2021.[8]
Medical uses
The medication is used in the treatment of heavy menstrual bleeding associated with uterine fibroids and for moderate to severe pain associated with endometriosis, both in premenopausal women.[7][9]
Available forms
The medication is formulated as an oral tablet containing a fixed-dose combination of 40 mg relugolix, 1 mg estradiol, and 0.5 mg norethisterone acetate.[7]
Pharmacology
Pharmacodynamics
Relugolix acts as an GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor.[12] Estradiol is an estrogen, or an agonist of the estrogen receptors, whereas norethisterone acetate is a progestin (synthetic progestogen), or an agonist of the progesterone receptors.[13] Relugolix suppresses ovarian sex hormone production, whereas estradiol and norethisterone acetate provide hormonal add-back to reduce hypogonadal and menopausal-like symptoms.[12]
History
The medication was approved for medical use in the United States in May 2021.[7][10]
In May 2021, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Ryeqo, intended for the treatment of symptoms of uterine fibroids.[14] The applicant for this medicinal product is Gedeon Richter Plc.[14] The combination was approved for medical use in the European Union in July 2021.[8][15]
In August 2022, the medication was approved for the treatment of moderate to severe pain associated with endometriosis in the United States.[9]
Research
The combination is also under development as a birth control pill for prevention of pregnancy in premenopausal women.[16]
