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| Pronunciation | /ˌɛləˈɡoʊlɪks/ EL-ə-GOH-liks |
| Trade names | Orilissa, Oriahnn |
| Other names | NBI-56418, ABT-620 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a618044 |
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| Routes of administration | By mouth[1] |
| Drug class | GnRH antagonist |
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| Pharmacokinetic data | |
| Bioavailability | Low (5.8% in rats, 11% in monkeys; no human data)[4] |
| Protein binding | 80%[1] |
| Metabolism | Liver (CYP3A)[1] |
| Elimination half-life | Typical: 4–6 hours[1] Single dose: 2.4–6.3 hrs[5][6] Continuous: 2.2–10.8 hours[5] |
| Excretion | Urine: <3%[1] Feces: 90%[1] |
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| ECHA InfoCard | 100.259.758 |
| Chemical and physical data | |
| Formula | C32H30F5N3O5 |
| Molar mass | 631.600 g·mol−1 |
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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]
- ^ a b c d e f g h i j k l m "Orilissa- elagolix tablet, film coated". DailyMed. 5 May 2020. Archived from the original on 24 September 2020. Retrieved 30 May 2020.
- ^ a b "Orilissa Product information". Health Canada. 25 April 2012. Archived from the original on 1 June 2022. Retrieved 31 May 2022.
- ^ a b "Orilissa (elagolix) Health Canada Product Monograph" (PDF). 4 October 2018. Archived (PDF) from the original on 16 February 2019. Retrieved 15 February 2019.
- ^ a b Tukun 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.
- ^ a b Cite error: The named reference
pmid19033369was invoked but never defined (see the help page). - ^ a b c d Ezzati 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.
- ^ a b c Clemenza 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.
- ^ a b c d e f g h Cite error: The named reference
AdisInsightwas invoked but never defined (see the help page). - ^ Cite error: The named reference
pmid19006286was 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.