Clinical Pharmacology of Elagolix: An Oral Gonadotropin-Releasing Hormone Receptor Antagonist for Endometriosis
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The clinical pharmacology of elagolix was extensively evaluated in clinical studies in healthy subjects and in women with endometriosis. Elagolix pharmacokinetics (PK) show significant population variability, however they are minimally affected by patients' baseline characteristics and demographics, except for clinically relevant extrinsic and intrinsic factors such as coadministrated strong organic anion transporting polypeptide (OATP) 1B1 inhibitors and severe hepatic impairment, which are contraindications for the use of elagolix. These studies enabled a comprehensive understanding of elagolix mechanism of action and the downstream pharmacodynamic (PD) effects on gonadotropin and ovarian hormones, as well as full characterization of the PK/PD (PKPD) relationships of elagolix at various dosages, including the approved 150 mg once daily and 200 mg twice daily dosing regimens for the management of moderate to severe pain associated with endometriosis. Several model-based analyses have contributed to understanding of the benefit-risk profile of elagolix in patients with endometriosis, through characterization of the exposure relationship with responder rates, with changes in bone mineral density over time, as well as the interaction with coadministered drugs. Collectively, these studies and analyses served as supportive evidence for the effectiveness of the approved dosages and provided general dosing instructions of the first approved oral gonadotropin-releasing hormone receptor antagonist.
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Elagolix is a non-peptide GnRH antagonist that enables dose-dependent reductions in estrogen levels and is effective in relieving moderate to severe endometriosis pain with long-lasting, sustained effects; it may reduce bone mineral density through estrogen reduction.
“Elagolix is a non-peptide GnRH (gonadotropin-releasing hormone) antagonist. Elagolix enables dose-dependent reductions in estrogen levels and is effective in relieving moderate to severe endometriosis pain with long-lasting, sustained effects. As a GnRH antagonist, elagolix may also reduce bone mineral density through its estrogen reduction mechanism [118].”
From Endometriosis: Epidemiology, Classification, Pathogenesis, Treatment and Genetics (Review of Literature) (2021) · cites this paper as [118]
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- Authors
- Shebley, M., Polepally, A. R., Nader, A., Ng, J. W., Winzenborg, I., Klein, C. E., Noertersheuser, P., Gibbs, M. A., & Mostafa, N. M.
- Affiliations
- AbbVie (United States) (US)
- Corresponding author
- Shebley, Mohamad
- ORCID
- Venue
- Clinical Pharmacokinetics
- Published
- 2019-11-21
- Volume
- 59
- Issue
- 3
- Pages
- 297-309
- ISSN
- 0312-5963 (ISSN-L)
- 1179-1926
- PMC
- PMC7051932
- OpenAlex
- W2990363083
- Cited by
- 68
- References
- 20
- Citations by year
- 2026: 9 · 2025: 9 · 2024: 4 · 2023: 7 · 2022: 18 · 2021: 10 · 2020: 10 · 2019: 1
- FWCI
- 9.57
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Clinical Pharmacokinetics (publishedVersion, cc-by-nc)
- Europe PMC (PubMed Central) (publishedVersion, cc-by-nc)
- PubMed Central (publishedVersion, cc-by-nc)
- PubMed (publishedVersion)
- Funders
- AbbVie
- Topics
- Health Sciences › Medicine › Reproductive Medicine › Endometriosis Research and Treatment
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- elagolix, endometriosis, GnRH antagonist, pharmacokinetics, pharmacodynamics, pharmacokinetic-pharmacodynamic modeling, liver dysfunction, ovarian hormones, gonadotropins, bone mineral density, drug interactions, dosing regimen, pain management
- MeSH terms
- Administration, Oral, Drug Interactions, Endometriosis, Female, Hormone Antagonists, Humans, Hydrocarbons, Fluorinated, Gonadotropin-Releasing Hormone, Liver Diseases, Pain, Pharmacogenetics, Pharmacology, Clinical, Pyrimidines, Receptors, LHRH, Bone Density, Treatment Outcome, Organic Anion Transporters
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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