Combination of | |
---|---|
Relugolix | GnRH antagonist |
Estradiol (medication) | Estrogen |
Norethisterone acetate | Progestogen |
Clinical data | |
Trade names | Myfembree, Ryeqo |
Other names | RGX/E2/NETA; MVT-601 |
AHFS/Drugs.com | Multum Consumer Information |
MedlinePlus | a622069 |
License data | |
Pregnancy category |
|
Routes of administration | By mouth |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
KEGG |
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. [8] [9] [10] It contains relugolix, an orally active gonadotropin-releasing hormone antagonist (GnRH antagonist), estradiol, an estrogen, and norethisterone acetate, a progestin. [8] [9] The medication is taken by mouth. [8]
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. [8]
The medication was approved for medical use in the United States in May 2021, [8] [11] [12] and in the European Union in July 2021. [9]
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. [8] [10]
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. [8]
Relugolix acts as an GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor. [13] 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. [14] Relugolix suppresses ovarian sex hormone production, whereas estradiol and norethisterone acetate provide hormonal add-back to reduce hypogonadal and menopausal-like symptoms. [13]
The medication was approved for medical use in the United States in May 2021. [8] [11]
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. [15] The applicant for this medicinal product is Gedeon Richter Plc. [15] The combination was approved for medical use in the European Union in July 2021. [9] [16]
In August 2022, the medication was approved for the treatment of moderate to severe pain associated with endometriosis in the United States. [10]
The combination is also under development as a birth control pill for prevention of pregnancy in premenopausal women. [17]
The combined oral contraceptive pill (COCP), often referred to as the birth control pill or colloquially as "the pill", is a type of birth control that is designed to be taken orally by women. It is the oral form of combined hormonal contraception. The pill contains two important hormones: a progestin and estrogen. When taken correctly, it alters the menstrual cycle to eliminate ovulation and prevent pregnancy.
Heavy menstrual bleeding (HMB), previously known as menorrhagia or hematomunia, is a menstrual period with excessively heavy flow. It is a type of abnormal uterine bleeding (AUB).
Leuprorelin, also known as leuprolide, is a manufactured version of a hormone used to treat prostate cancer, breast cancer, endometriosis, uterine fibroids, for early puberty, or as part of transgender hormone therapy. It is given by injection into a muscle or under the skin.
Progestogen-only pills (POPs), colloquially known as "mini pills", are a type of oral contraceptive that contain synthetic progestogens (progestins) and do not contain estrogens. They are primarily used for the prevention of undesired pregnancy, although additional medical uses also exist.
Norethisterone acetate (NETA), also known as norethindrone acetate and sold under the brand name Primolut-Nor among others, is a progestin medication which is used in birth control pills, menopausal hormone therapy, and for the treatment of gynecological disorders. The medication available in low-dose and high-dose formulations and is used alone or in combination with an estrogen. It is ingested orally.
Norgestimate, sold under the brand name Ortho Tri-Cyclen among others, is a progestin medication which is used in birth control pills for women and in menopausal hormone therapy. The medication is available in combination with an estrogen and is not available alone. It is taken by mouth.
Ethinylestradiol/norethisterone acetate (EE/NETA), or ethinylestradiol/norethindrone acetate, is a combination of ethinylestradiol (EE) and norethisterone acetate (NETA) which is used as birth control and menopausal hormone therapy. EE is an estrogen, while norethisterone acetate (NETA) is a progestin. It is taken by mouth. Some preparations of EE/NETA used in birth control additionally contain an iron supplement in the form of ferrous fumarate.
Triptorelin, sold under the brand name Decapeptyl among others, is a medication that acts as an agonist analog of gonadotropin-releasing hormone, repressing expression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
Gestrinone, sold under the brand names Dimetrose and Nemestran among others, is a medication which is used in the treatment of endometriosis. It has also been used to treat other conditions such as uterine fibroids and heavy menstrual bleeding and has been investigated as a method of birth control. Gestrinone is used alone and is not formulated in combination with other medications. It is taken by mouth or in through the vagina.
Norethisterone, also known as norethindrone and sold under the brand name Norlutin among others, is a progestin medication used in birth control pills, menopausal hormone therapy, and for the treatment of gynecological disorders. The medication is available in both low-dose and high-dose formulations and both alone and in combination with an estrogen. It is used by mouth or, as norethisterone enanthate, by injection into muscle.
Cetrorelix, or cetrorelix acetate, sold under the brand name Cetrotide, is an injectable gonadotropin-releasing hormone (GnRH) antagonist. A synthetic decapeptide, it is used in assisted reproduction to inhibit premature luteinizing hormone surges The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In addition, cetrorelix can be used to treat hormone-sensitive cancers of the prostate and breast and some benign gynaecological disorders. It is administered as either multiple 0.25 mg daily subcutaneous injections or as a single-dose 3 mg subcutaneous injection. The duration of the 3 mg single dose is four days; if human chorionic gonadotropin (hCG) is not administered within four days, a daily 0.25 mg dose is started and continued until hCG is administered.
Dienogest, sold under the brand name Visanne among others, is a progestin medication which is used in birth control pills and in the treatment of endometriosis. It is also used in menopausal hormone therapy and to treat heavy periods. Dienogest is available both alone and in combination with estrogens. It is taken by mouth.
Ulipristal acetate, sold under the brand name Ella among others, is a medication used for emergency contraception and uterine fibroids. As emergency contraception it should be used within 120 hours of vaginally penetrating intercourse. For fibroids it may be taken for up to six months. It is taken by mouth.
Conjugated estrogens (CEs), or conjugated equine estrogens (CEEs), sold under the brand name Premarin among others, is an estrogen medication which is used in menopausal hormone therapy and for various other indications. It is a mixture of the sodium salts of estrogen conjugates found in horses, such as estrone sulfate and equilin sulfate. CEEs are available in the form of both natural preparations manufactured from the urine of pregnant mares and fully synthetic replications of the natural preparations. They are formulated both alone and in combination with progestins such as medroxyprogesterone acetate. CEEs are usually taken by mouth, but can also be given by application to the skin or vagina as a cream or by injection into a blood vessel or muscle.
Elagolix, sold under the brand name Orilissa, is a gonadotropin-releasing hormone antagonist medication which is used in the treatment of pain associated with endometriosis in women. It is also under development for the treatment of uterine fibroids and heavy menstrual bleeding in women. The medication was under investigation for the treatment of prostate cancer and enlarged prostate in men as well, but development for these conditions was discontinued. Elagolix is taken by mouth once or twice per day. It can be taken for up to 6 to 24 months, depending on the dosage.
Relugolix, sold under the brand names Orgovyx and Relumina among others, is a gonadotropin-releasing hormone antagonist medication which is used in the treatment of prostate cancer in men and uterine fibroids in women. It is taken by mouth.
Estradiol (E2) is a medication and naturally occurring steroid hormone. It is an estrogen and is used mainly in menopausal hormone therapy and to treat low sex hormone levels in women. It is also used in hormonal birth control for women, in feminizing hormone therapy for transgender women and some non-binary individuals, and in the treatment of hormone-sensitive cancers like prostate cancer in men and breast cancer in women, among other uses. Estradiol can be taken by mouth, held and dissolved under the tongue, as a gel or patch that is applied to the skin, in through the vagina, by injection into muscle or fat, or through the use of an implant that is placed into fat, among other routes.
Linzagolix, sold under the brand name Yselty, is a medication used in the treatment of uterine fibroids. Linzagolix is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist developed by Kissei Pharmaceutical and ObsEva.
Elagolix/estradiol/norethisterone acetate, sold under the brand name Oriahnn, is a fixed-dose combination medication used to treat heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women. It contains elagolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist, estradiol, an estrogen, and norethisterone acetate, a progestin. It is taken by mouth. Oriahnn is co-packaged as a combination of elagolix/estradiol/norethisterone acetate capsules with elagolix capsules.