Cited by 68Endometriosis Research and TreatmentReproductive Health and ContraceptionPharmacogenetics and Drug Metabolism

Clinical Pharmacology of Elagolix: An Oral Gonadotropin-Releasing Hormone Receptor Antagonist for Endometriosis

Open access
Shebley, Mohamad, Polepally, Akshanth R., Nader, Ahmed, Ng, Juki W., Winzenborg, Insa, Klein, Cheri E., Noertersheuser, Peter, Gibbs, Megan A. +1 more·2020·Clinical Pharmacokinetics

Abstract

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.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Integrity signals

Registry

Crossref · 10.1007/s40262-019-00840-7

Cites

20 of 20 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

  • 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].”

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Cites

Flagged first, then by citations

Cited by

Sorted by citations

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
Venue
Clinical Pharmacokinetics
Published
2019-11-21
Volume
59
Issue
3
Pages
297-309
ISSN
  • 0312-5963 (ISSN-L)
  • 1179-1926
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
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 ›

Are you an author, or do you see a problem with this page? Request a review