Cited by 38Endometriosis Research and TreatmentMenstrual Health and DisordersEctopic Pregnancy Diagnosis and Management

Clinical evaluation of the oral gonadotropin-releasing hormone-antagonist elagolix for the management of endometriosis-associated pain

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Taylor, Hugh S, Dun, Erica C, Chwalisz, Kristof·2019·Pain Management

Abstract

Endometriosis is an estrogen-dependent chronic inflammatory disease associated with pelvic pain symptoms that are often severe, mainly dysmenorrhea, nonmenstrual pelvic pain and dyspareunia. This condition is also associated with peripheral and central sensitization. The current medical treatment options for endometriosis-associated pain are limited. Recently, the US FDA approved the novel, oral, nonpeptide gonadotropin-releasing hormone antagonist elagolix for the management of moderate to severe endometriosis-associated pain. Elagolix produces dose-dependent estrogen suppression, from partial suppression at lower doses to nearly full suppression at higher doses. This review article summarizes the current understanding of the pathophysiology of endometriosis, with a focus on the role of estrogen and the mechanisms of pain symptoms, and reviews the clinical development of elagolix in women with endometriosis-associated pain.

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Crossref · 10.2217/pmt-2019-0010

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98 of 98 references verified0 citation errors · 0 not checkable

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  • The recommended treatment duration in women with normal liver function or mild hepatic impairment is up to 24 months with elagolix 150 mg once daily, and up to 6 months with 200 mg twice daily.

    “As reported by Taylor et al. [107], the recommended treatment duration in women with normal liver function or mild hepatic impairment is up to 24 months with elagolix 150 mg once daily, and up to 6 months with 200 mg twice daily.”
  • 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].”
  • The pharmacokinetic properties of elagolix at 150 mg once daily and 200 mg twice daily do not appear to be affected, to a clinically meaningful extent, by body weight, body mass index, race/ethnicity or the presence of endometriosis.

    “Overall, the pharmacokinetic properties of elagolix at 150 mg once daily and 200 mg twice daily do not appear to be affected, to a clinically meaningful extent, by body weight, body mass index, race/ethnicity or the presence of endometriosis [102,103,107].”

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Authors
Taylor, H. S., Dun, E. C., & Chwalisz, K.
Affiliations
  • Yale University (US)
  • AbbVie Inc., 1 North Waukegan Road, Bldg. AP4A-3, North Chicago, IL60064, USA
Venue
Pain Management
Published
2019-08-22
Volume
9
Issue
5
Pages
497-515
ISSN
  • 1758-1869 (ISSN-L)
  • 1758-1877
OpenAlex
W2969537575
Cited by
38
References
98
Citations by year
2026: 2 · 2025: 3 · 2024: 3 · 2023: 4 · 2022: 8 · 2021: 10 · 2020: 6 · 2017: 2
FWCI
0.88
Type
journal article
Language
en
Open access
Locations
  • Pain Management (publishedVersion, cc-by-nc-nd)
  • PubMed (publishedVersion)
Funders
  • AbbVie Inc
  • National Institutes of Health
Topics
  • Health Sciences › Medicine › Reproductive Medicine › Endometriosis Research and Treatment
  • Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Menstrual Health and Disorders
  • Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Ectopic Pregnancy Diagnosis and Management
Keywords
elagolix, endometriosis-associated pain, GnRH antagonist, estrogen suppression, dysmenorrhea, dyspareunia, peripheral sensitization, central sensitization, endometriosis pathophysiology, clinical development
MeSH terms
Administration, Oral, Animals, Clinical Trials as Topic, Endometriosis, Estrogen Antagonists, Female, Humans, Hydrocarbons, Fluorinated, Gonadotropin-Releasing Hormone, Pain, Pyrimidines, Treatment Outcome, Pain Management

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