ArticleClinical pharmacokinetics2020
Quantitative Assessment of Elagolix Enzyme-Transporter Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling.
Article in Clinical pharmacokinetics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 25 citations in OpenAlex.
- A Physiologically Based Pharmacokinetic Model to Predict Potential Drug-Drug Interactions of TPN171, a Novel Phosphodiesterase Type 5 Inhibitor.CPT: pharmacometrics & systems pharmacology · 2026Article
- Pharmacokinetic-Pharmacodynamic Modeling and Simulation of Merigolix, a Nonpeptide Gonadotropin-Releasing Hormone Antagonist.Clinical pharmacokinetics · 2026Article
- Indirect Modeling of Post-Prandial Intestinal Lymphatic Uptake of Halofantrine Using PBPK Approaches: Limitations and Implications.Pharmaceutics · 2025Article
- PBBM Considerations for Base Models, Model Validation, and Application Steps: Workshop Summary Report.Molecular pharmaceutics · 2024Review
- Advances in Modeling Approaches for Oral Drug Delivery: Artificial Intelligence, Physiologically-Based Pharmacokinetics, and First-Principles Models.Pharmaceutics · 2024Review
- Pharmacokinetic and Pharmacodynamic Drug-Drug Interactions: Research Methods and Applications.Metabolites · 2023Review
- Virtual Bioequivalence Assessment of Elagolix Formulations Using Physiologically Based Pharmacokinetic Modeling.The AAPS journal · 2023Article
- Physiologically based pharmacokinetic modeling and simulations to inform dissolution specifications and clinical relevance of release rates on elagolix exposure.Biopharmaceutics & drug disposition · 2022Article
- Effects of elagolix on the pharmacokinetics of omeprazole and its metabolites in healthy premenopausal women.Clinical and translational science · 2022Article
- Elagolix in the treatment of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.Expert review of clinical pharmacology · 2021Review
- Drug-Drug Interaction Studies of Elagolix with Oral and Transdermal Low-Dose Hormonal Add-Back Therapy.Clinical pharmacokinetics · 2021Article
- Computational Models for Diagnosing and Treating Endometriosis.Frontiers in reproductive health · 2021Review
- Clinical Pharmacology of Elagolix: An Oral Gonadotropin-Releasing Hormone Receptor Antagonist for Endometriosis.Clinical pharmacokinetics · 2020Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
introductionElagolix is approved for the management of moderate-to-severe pain associated with endometriosis. The aim of this analysis was to develop a physiologically based pharmacokinetic (PBPK) model that describes the enzyme-transporter interplay involved in the disposition of elagolix and to predict the magnitude of drug-drug interaction (DDI) potential of elagolix as an inhibitor of P-glycoprotein (P-gp) and inducer of cytochrome P450 (CYP) 3A4.
methodsA PBPK model (SimCYP
resultsAfter accounting for the interplay between elagolix metabolism by CYP3A4 and uptake by OATP1B1, the model-predicted PK parameters of elagolix along with the DDI AUC
conclusionsA PBPK model of elagolix was developed, verified, and applied to characterize the disposition interplay between CYP3A4 and OATP1B1, and to predict the DDI potential of elagolix as a perpetrator under dosing conditions that were not tested clinically. PBPK model-based predictions were used to support labeling language for DDI recommendations of elagolix.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.