Elagolix sodium for the treatment of women with moderate to severe endometriosis-associated pain
Abstract
First-line medical therapies for treating pain associated with endometriosis mainly consist in combined oral contraceptives and progestins. However, some women, having persistence of symptoms, may require further therapeutic options. Among these, gonadotropin-releasing hormone (GnRH) agonists (GnRH-as) have been widely employed in the last 30 years, despite being characterized by an unfavorable safety profile. Currently, new alternative investigational options are being investigated to treat this benign chronic disease. GnRH antagonists (GnRH-ants) are innovative hormonal drugs that do not induce flare-up effects and present also a limited onset of hypoestrogenic symptoms; in fact, their pharmacological mechanism of action, which consists in pure antagonistic activity, differs from that of traditional GnRH-as. In July 2018, the U.S. Food and Drug Administration (FDA) approved elagolix sodium for the management of moderate to severe pain associated with endometriosis, after the drug showed promising efficacy and safety results in previous phase III trials. This monograph aims to provide a complete overview of the pharmacokinetics, clinical efficacy and safety of this GnRH-ant for treat¬ing patients with endometriosis.
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Estrogens play a crucial role not only in survival of endometriotic implants, but also in coordinated vasculogenesis and neurogenesis by different pathways involving ER signaling.
“As estrogens play a crucial role not only in survival of endometriotic implants, but also in coordinated vasculogenesis and neurogenesis [110] by different pathways involving ER signaling [15,16], it is logical to consider lowering estrogen levels as a therapeutic approach.”
From Endometriosis and Medical Therapy: From Progestogens to Progesterone Resistance to GnRH Antagonists: A Review (2021) · cites this paper as [110]
Elagolix is rapidly absorbed after oral administration and its mean plasma half-life ranges from 2.4 to 6.3 h.
“Elagolix is rapidly absorbed after oral administration and its mean plasma half-life (t1/2) ranges from 2.4 to 6.3 h [99,107,110].”
From Endometriosis and Medical Therapy: From Progestogens to Progesterone Resistance to GnRH Antagonists: A Review (2021) · cites this paper as [110]
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“Additionally, the clinical studies found that the pharmacokinetic characteristics of Elagolix at 150 mg once a day and 200 mg twice a day seem not affected by factors including body weight, body mass index, race, or endometriosis status (Taylor et al., 2017; Surrey et al., 2018; Barra et al., 2019).”
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“Elagolix, a new oral nonpeptide GnRH antagonist that can partially or fully suppress estrogen, has shown efficacy in controlling both dysmenorrhea and chronic pelvic pain [15].”
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“ELX is an orally administered GnRH-ant that is rapidly absorbed and quickly suppresses gonadotropins and estradiol levels [115].”
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“Elagolix has been extensively researched [97], particularly in two large multicenter, double-blind, randomized, placebo-controlled phase 3 trials known as Elaris Endometriosis I and II [98].”
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“Elagolix has a relatively short half-life (4 to 6 hours), necessitating twice-daily dosing in some regimens and enabling fine-tuned control of ovarian suppression [45,48–50].”
Self-citation
- Authors
- Barra, F., Scala, C., & Ferrero, S.
- Affiliations
- Ospedale Policlinico San Martino (IT)
- Venue
- Drugs of today
- Publisher
- Portico
- Published
- 2019
- Volume
- 55
- Issue
- 4
- Pages
- 237
- ISSN
- 0025-7656 (ISSN-L)
- 1699-4019
- OpenAlex
- W2942452981
- Cited by
- 26
- References
- 0
- Citations by year
- 2026: 3 · 2025: 1 · 2024: 3 · 2023: 5 · 2022: 4 · 2021: 5 · 2020: 4 · 2019: 1
- FWCI
- 3.35
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drugs of today (publishedVersion)
- PubMed (publishedVersion)
- CINECA IRIS Institutial Research Information System (University of Genoa) (submittedVersion)
- Topics
- Health Sciences › Medicine › Reproductive Medicine › Endometriosis Research and Treatment
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Ectopic Pregnancy Diagnosis and Management
- Keywords
- endometriosis-associated pain, GnRH antagonist, gonadotropin-releasing hormone, pharmacokinetics, clinical efficacy, drug safety, FDA approval, chronic pelvic pain
- MeSH terms
- Endometriosis, Female, Hormone Antagonists, Humans, Hydrocarbons, Fluorinated, Pain, Pyrimidines
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