Elagolix, sold under the brand name Orilissa, is a gonadotropin-releasing hormone antagonist (GnRH antagonist) medication which is used in the treatment of pain associated with endometriosis in women.[1][2][3][7][6][4][8][9] It is also under development for the treatment of uterine fibroids and heavy menstrual bleeding in women.[9] 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.[9] Elagolix is taken by mouth once or twice per day.[1][9] It can be taken for up to 6 to 24 months, depending on the dosage.[1]
Side effects of elagolix include menopausal-like symptoms such as hot flashes, night sweats, insomnia, amenorrhea, mood changes, anxiety, and decreased bone density, among others.[1] Elagolix is a GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor (GnRHR), the biological target of the hypothalamic hormone gonadotropin-releasing hormone (GnRH).[1] By blocking the GnRHR, it dose-dependently suppresses the gonadal production and hence circulating levels of sex hormones such as estradiol, progesterone, and testosterone.[1] Elagolix is a short-acting GnRH antagonist, and can be used to achieve either partial or more substantial suppression of sex hormone levels.[8] Reduced estrogen levels in the endometrium are responsible for the efficacy of elagolix in the treatment of endometriosis.[8]
Elagolix was first described in 2008 and was approved for medical use in July 2018.[10][9] It has been described as a "second-generation" GnRH modulator due to its non-peptide and small-molecule nature and its oral activity.[6][9] Unlike GnRH agonists and older GnRH antagonists, which are peptides and first-generation GnRH modulators, elagolix is not a GnRH analogue as it is not structurally related to GnRH.[6][9] Elagolix was the first second-generation and orally active GnRH modulator to be introduced for medical use.[9] The introduction of elagolix in the United States and Canada was followed by that of relugolix (brand name Relumina), the next second-generation GnRH antagonist, in Japan in January 2019.[11] The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[12]
^ abcdefghijklm"Orilissa- elagolix tablet, film coated". DailyMed. 5 May 2020. Archived from the original on 24 September 2020. Retrieved 30 May 2020.
^ ab"Orilissa Product information". Health Canada. 25 April 2012. Archived from the original on 1 June 2022. Retrieved 31 May 2022.
^ ab"Orilissa (elagolix) Health Canada Product Monograph" (PDF). 4 October 2018. Archived (PDF) from the original on 16 February 2019. Retrieved 15 February 2019.
^ abTukun FL, Olberg DE, Riss PJ, Haraldsen I, Kaass A, Klaveness J (December 2017). "Recent Development of Non-Peptide GnRH Antagonists". Molecules. 22 (12): 2188. doi:10.3390/molecules22122188. PMC 6149776. PMID 29232843.
^ abCite error: The named reference pmid19033369 was invoked but never defined (see the help page).
^ abcdEzzati M, Carr BR (January 2015). "Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain". Women's Health. 11 (1): 19–28. doi:10.2217/whe.14.68. PMID 25581052.
^Lamb YN (September 2018). "Elagolix: First Global Approval". Drugs. 78 (14): 1501–1508. doi:10.1007/s40265-018-0977-4. PMC 6244606. PMID 30194661.
^ abcClemenza S, Sorbi F, Noci I, Capezzuoli T, Turrini I, Carriero C, Buffi N, Fambrini M, Petraglia F (February 2018). "From pathogenesis to clinical practice: Emerging medical treatments for endometriosis". Best Pract Res Clin Obstet Gynaecol. 51: 92–101. doi:10.1016/j.bpobgyn.2018.01.021. PMID 29559388. S2CID 3952054.
^ abcdefghCite error: The named reference AdisInsight was invoked but never defined (see the help page).
^Cite error: The named reference pmid19006286 was invoked but never defined (see the help page).
^"Relugolix - Myovant/Takeda - AdisInsight". Archived from the original on 2018-09-20. Retrieved 2019-02-16.
^New Drug Therapy Approvals 2018 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2019. Archived from the original on 17 September 2020. Retrieved 16 September 2020.
Elagolix, sold under the brand name Orilissa, is a gonadotropin-releasing hormone antagonist (GnRH antagonist) medication which is used in the treatment...
the elagolix NDA. A final regulatory decision on the drug will come during the third quarter of 2018. The companies are also developing elagolix for the...
hormone receptor. Unlike most other GnRH modulators, but similarly to elagolix (brand name Orilissa), relugolix is a non-peptide, small-molecule compound...
fumarate hydratase gene in the long arm of chromosome 1. Leiomyosarcoma Elagolix/estradiol/norethindrone acetate El Sabeh M, Saha SK, Afrin S, Islam MS...
Neurocrine Biosciences does not hold a final patent for valbenazine or elagolix, they do hold a patent for the VMAT2 inhibitor [9,10-dimethoxy-3-(2-methylpropyl)-1H...
include GnRH agonists such as leuprorelin and GnRH antagonists such as elagolix and are thought to work by decreasing estrogen levels. A 2010 Cochrane...
finasteride; nonsteroidal antiandrogens include compounds like bicalutamide, elagolix, diethylstilbestrol, aminoglutethimide, and ketoconazole; and peptides...
contrast to GnRH agonists, GnRH antagonists, such as degarelix (Firmagon) and elagolix (Orilissa), work by binding to the GnRH receptor without activating it...
provided the source is acknowledged. Ezzati M, Carr BR (January 2015). "Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the...