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
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.[5][6][7] It contains relugolix, an orally active gonadotropin-releasing hormone antagonist (GnRH antagonist), estradiol, an estrogen, and norethisterone acetate, a progestin.[5][6] The medication is taken by mouth.[5]

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.[5]

The medication was approved for medical use in the United States in May 2021,[5][8][9] and in the European Union in July 2021.[6]

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.[5][7]

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.[5]

Pharmacology

Pharmacodynamics

Relugolix acts as an GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor.[10] 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.[11] Relugolix suppresses ovarian sex hormone production, whereas estradiol and norethisterone acetate provide hormonal add-back to reduce hypogonadal and menopausal-like symptoms.[10]

History

The medication was approved for medical use in the United States in May 2021.[5][8]

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.[12] The applicant for this medicinal product is Gedeon Richter Plc.[12] The combination was approved for medical use in the European Union in July 2021.[6][13]

In August 2022, the medication was approved for the treatment of moderate to severe pain associated with endometriosis in the United States.[7]

Research

The combination is also under development as a birth control pill for prevention of pregnancy in premenopausal women.[14]

References

  1. ↑ "TGA eBS - Product and Consumer Medicine Information Licence". Archived from the original on 2023-03-18. Retrieved 2023-03-18.
  2. ↑ "Ryeqo (Gedeon Richter Australia Pty Ltd)". Therapeutic Goods Administration (TGA). 7 October 2022. Archived from the original on 18 March 2023. Retrieved 29 April 2023.
  3. ↑ "Notice: Multiple additions to the Prescription Drug List (PDL) [2023-12-22]". Health Canada. 22 December 2023. Retrieved 3 January 2024.
  4. ↑ "Ryeqo 40mg/1mg/0.5mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 12 September 2022. Archived from the original on 18 March 2023. Retrieved 17 March 2023.
  5. 1 2 3 4 5 6 7 8 9 "Myfembree- relugolix, estradiol hemihydrate, and norethindrone acetate tablet, film coated". DailyMed. 2 February 2023. Archived from the original on 12 March 2023. Retrieved 11 March 2023.
  6. 1 2 3 4 5 "Ryeqo EPAR". European Medicines Agency. 19 May 2021. Archived from the original on 29 April 2022. Retrieved 24 April 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  7. 1 2 3 "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. Archived from the original on 28 August 2022. Retrieved 28 August 2022.
  8. 1 2 "Myfembree: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 11 August 2022. Retrieved 28 August 2022.
  9. ↑ "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. Archived from the original on 26 May 2021. Retrieved 26 May 2021.
  10. 1 2 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. PMC 8866208. PMID 35068291.
  11. ↑ 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. S2CID 24616324.
  12. 1 2 "Ryeqo: Pending EC decision". European Medicines Agency (EMA). 20 May 2021. Archived from the original on 26 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.
  13. ↑ "Ryeqo Product information". Union Register of medicinal products. Archived from the original on 4 March 2023. Retrieved 3 March 2023.
  14. ↑ "Estradiol/norethisterone acetate/relugolix - Myovant Sciences". AdisInsight. 22 August 2022. Archived from the original on 28 August 2022. Retrieved 28 August 2022.

Further reading

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