Relugolix/estradiol/norethisterone acetate

Relugolix/estradiol/norethisterone acetate (RGX/E2/NETA), 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.[1][3][4] It contains relugolix (RGX), an orally active gonadotropin-releasing hormone antagonist (GnRH antagonist), estradiol (E2), an estrogen, and norethisterone acetate (NETA), a progestin.[1][3] The medication is taken by mouth.[1]

Relugolix/estradiol/norethisterone acetate
Combination of
RelugolixGnRH antagonist
Estradiol (medication)Estrogen
Norethisterone acetateProgestogen
Clinical data
Trade namesMyfembree, Ryeqo
Other namesRGX/E2/NETA; MVT-601
License data
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Identifiers
KEGG

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.[1]

RGX/E2/NETA was approved for medical use in the United States in May 2021,[1][5][6] and in the European Union in July 2021.[2]

Medical uses

RGX/E2/NETA 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.[1][4]

Available forms

RGX/E2/NETA is formulated as an oral tablet containing a fixed-dose combination of 40 mg relugolix, 1 mg estradiol, and 0.5 mg norethisterone acetate.[1]

Pharmacology

Pharmacodynamics

Relugolix acts as an GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor.[7] 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.[8] Relugolix suppresses ovarian sex hormone production, whereas estradiol and norethisterone acetate provide hormonal add-back to reduce hypogonadal and menopausal-like symptoms.[7]

History

RGX/E2/NETA was approved for medical use in the United States in May 2021.[1][5] On 20 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.[3] The applicant for this medicinal product is Gedeon Richter Plc.[3] RGX/E2/NETA was approved for medical use in the European Union in July 2021.[2] In August 2022, RGX/E2/NETA was approved for the treatment of moderate to severe pain associated with endometriosis in the United States.[4]

Research

RGX/E2/NETA is also under development as a birth control pill for prevention of pregnancy in premenopausal women.[9]

References
  1. https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214846s000lbl.pdf
  2. "Ryeqo EPAR". European Medicines Agency. 19 May 2021. Retrieved 24 April 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  3. "Ryeqo: Pending EC decision". European Medicines Agency (EMA). 20 May 2021. Retrieved 25 May 2021. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  4. "Myovant Sciences and Pfizer Receive U.S. FDA Approval of MYFEMBREE®, a Once-Daily Treatment for the Management of Moderate to Severe Pain Associated With Endometriosis". Pfizer. 8 August 2022. Retrieved 28 August 2022.
  5. "Myfembree: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 28 August 2022.
  6. "Myovant Sciences and Pfizer Receive FDA Approval for Myfembree, the First Once-Daily Treatment for Heavy Menstrual Bleeding Associated With Uterine Fibroids". Pfizer (Press release). 26 May 2021. Retrieved 26 May 2021.
  7. Ali M, Chen HY, Chiang YF, Badary OA, Hsia SM, Al-Hendy A (March 2022). "An evaluation of relugolix/estradiol/norethindrone acetate for the treatment of heavy menstrual bleeding associated with uterine fibroids in premenopausal women". Expert Opin Pharmacother. 23 (4): 421–429. doi:10.1080/14656566.2022.2030705. PMID 35068291.
  8. Kuhl H (August 2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration". Climacteric. 8 Suppl 1: 3–63. doi:10.1080/13697130500148875. PMID 16112947.
  9. Name, Drug (22 August 2022). "Estradiol/norethisterone acetate/relugolix - Myovant Sciences". AdisInsight. Retrieved 28 August 2022.

Further reading
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