Population Pharmacokinetics of Elagolix in Healthy Women and Women with Endometriosis

Clinical Pharmacokinetics
Insa WinzenborgJuki Ng

Abstract

Elagolix is a novel, orally active, non-peptide, competitive gonadotropin-releasing hormone (GnRH) receptor antagonist in development for the management of endometriosis with associated pain and heavy menstrual bleeding due to uterine fibroids. The pharmacokinetics of elagolix have been well-characterized in phase I studies; however, elagolix population pharmacokinetics have not been previously reported. Therefore, a robust model was developed to describe elagolix population pharmacokinetics and to evaluate factors affecting elagolix pharmacokinetic parameters. The data from nine clinical studies (a total of 1624 women) were included in the analysis: five phase I studies in healthy, premenopausal women and four phase III studies in premenopausal women with endometriosis. Elagolix population pharmacokinetics were best described by a two-compartment model with a lag time in absorption. Of the 15 covariates tested for effect on elagolix apparent clearance (CL/F) and/or volume of distribution only one covariate, organic anion transporting polypeptide (OATP) 1B1 genotype status, had a statistically significant, but not clinically meaningful, effect on elagolix CL/F. Elagolix pharmacokinetics were not affected by patient demographics...Continue Reading

References

May 26, 2004·Best Practice & Research. Clinical Obstetrics & Gynaecology·Paola ViganòPaolo Vercellini
Jun 28, 2005·Human Reproduction·Stephen KennedyUNKNOWN ESHRE Special Interest Group for Endometriosis and Endometrium Guideline Development Group
Feb 9, 2011·The AAPS Journal·Martin BergstrandMats O Karlsson
Sep 4, 2015·Journal of Psychosomatic Obstetrics and Gynaecology·Federica FacchinPaolo Vercellini
Mar 23, 2017·The Journal of Clinical Endocrinology and Metabolism·Juki NgCheri E Klein
May 20, 2017·The New England Journal of Medicine·Hugh S TaylorKristof Chwalisz

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Citations

Dec 21, 2018·Clinical Pharmacology in Drug Development·Juki NgCheri E Klein
Sep 9, 2018·Drugs·Yvette N Lamb
Nov 18, 2020·CPT: Pharmacometrics & Systems Pharmacology·Insa WinzenborgMohamad Shebley
Mar 9, 2021·Expert Review of Clinical Pharmacology·Mohamed AliAyman Al Hendy

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