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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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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]
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