Exposure‐Safety Analyses Identify Predictors of Change in Bone Mineral Density and Support Elagolix Labeling for Endometriosis‐Associated Pain

Ahmed Abbas Suleiman, Ahmed A. Suleiman, Ahmed Nader, Insa Winzenborg, Denise Beck, Akshanth R Polepally, Juki Ng, Peter Noertersheuser, Nael M Mostafa
CPT: pharmacometrics & systems pharmacology · 2020 · vol. 9(11) , pp. 639–648 · doi:10.1002/psp4.12560 · PMID:32945631 · PMC7679073 · W3087237744
article OA: gold CC0 ⤵ 8 in-corpus citations
📄 Open PDF View on OpenAlex View on PubMed View at publisher
⚙ AI-generated summary by claude@2026-06, 2026-06-09 ⓘ

A population exposure-response model using phase III data described elagolix's pharmacokinetic exposure-dependent changes in bone mineral density, identifying race, BMI, and collagen levels as predictors and supporting current labeling for endometriosis pain.

One-sentence paraphrase of the abstract; not a substitute for reading it. No clinical advice. How this works

Abstract

Elagolix is a novel oral gonadotropin releasing hormone receptor antagonist, that can suppress estradiol in a dose‐dependent manner. It is indicated for management of moderate‐to‐severe pain associated with endometriosis. A population exposure‐response model describing the relationship between elagolix exposure and changes in bone mineral density (BMD) was developed using data from four phase III studies in premenopausal women with endometriosis‐associated pain. Elagolix pharmacokinetic exposure‐dependent changes in BMD were described by an indirect‐response maximum effect (E max ) model through stimulation of bone resorption. African American race, higher body mass index (BMI), and lower type‐I collagen C‐telopeptide concentrations were significantly associated with higher baseline BMD. Higher BMI was significantly associated with higher bone formation rates. Simulations using the final model demonstrated that elagolix 150 mg q.d. dosing for 24 months is predicted to result in −1.45% (−2.04 to −0.814) decrease from baseline in BMD and were used to support corresponding dosing recommendations in the label.

My notes (saved in your browser only)

Condition tags

endometriosis

MeSH descriptors

Bone Density Hydrocarbons, Fluorinated Hydrocarbons, Fluorinated Pain Pyrimidines Pyrimidines Receptors, LHRH Absorptiometry, Photon Absorptiometry, Photon Administration, Oral Adult Biological Variation, Population Black or African American Black or African American Body Mass Index Bone Density Case-Control Studies Collagen Type I Collagen Type I Computer Simulation

Citation neighborhood

Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

References (22)

Cited by (8)

Source provenance

europepmc
last seen: 2026-06-13T06:22:48.782012+00:00
openalex
last seen: 2026-06-10T17:14:06.276822+00:00
pubmed
last seen: 2026-05-13T22:21:42.008780+00:00
License: CC0 · commercial use OK