Trial reportClinical pharmacokinetics2015
Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection.
Trial report in Clinical pharmacokinetics, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 57 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
57 citing papers in PubMed, 134 citations in OpenAlex.
- A Study on the Safety, Pharmacokinetics, and Pharmacodynamics of H018 Tablets, a Selective JAK1 Inhibitor, Upon Single- and Multiple-Dose Administration in Chinese Healthy Subjects.Clinical drug investigation · 2026Trial
- Mucosal p-STAT1/3 correlates with histologic disease activity in Crohn's disease and is responsive to filgotinib.Tissue barriers · 2023Trial
- Exposure-response relationships for the efficacy and safety of filgotinib and its metabolite GS-829845 in subjects with rheumatoid arthritis based on phase 2 and phase 3 studies.British journal of clinical pharmacology · 2022Trial
- Phase I and scintigraphy studies to evaluate safety, tolerability, pharmacokinetics, and lung deposition of inhaled GDC-0214 in healthy volunteers.Clinical and translational science · 2022Trial
- Assessment of the Effect of Filgotinib on the Pharmacokinetics of Atorvastatin, Pravastatin, and Rosuvastatin in Healthy Adult Participants.Clinical pharmacology in drug development · 2022Trial
- Exposure-Response Analyses for Upadacitinib Efficacy and Safety in the Crohn's Disease CELEST Study and Bridging to the Extended-Release Formulation.Clinical pharmacology and therapeutics · 2020Trial
- Population Pharmacokinetics of Upadacitinib Using the Immediate-Release and Extended-Release Formulations in Healthy Subjects and Subjects with Rheumatoid Arthritis: Analyses of Phase I-III Clinical Trials.Clinical pharmacokinetics · 2019Trial
- Evaluation of a Janus kinase 1 inhibitor, PF-04965842, in healthy subjects: A phase 1, randomized, placebo-controlled, dose-escalation study.British journal of clinical pharmacology · 2018Trial
- Efficacy, Safety, Pharmacokinetics, and Pharmacodynamics of Filgotinib, a Selective JAK-1 Inhibitor, After Short-Term Treatment of Rheumatoid Arthritis: Results of Two Randomized Phase IIa Trials.Arthritis & rheumatology (Hoboken, N.J.) · 2017Trial
- Pharmacokinetics, Safety and Tolerability of ABT-494, a Novel Selective JAK 1 Inhibitor, in Healthy Volunteers and Subjects with Rheumatoid Arthritis.Clinical pharmacokinetics · 2016Trial
- Comparative Effectiveness and Safety of Tofacitinib, Filgotinib, and Upadacitinib in Ulcerative Colitis: A Multicenter Real-World Cohort Study.Advances in therapy · 2026Article
- Novel Therapeutic Strategies and Biomarkers in the Management of Inflammatory Bowel Disease: A Narrative Review.Cureus · 2026Review
- Structure-Based Identification of JAK1-Selective Candidates Using Ensemble Docking and Interaction Analysis.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Therapeutic drug monitoring with non-anti-TNF advanced therapies in inflammatory bowel disease: current and evolving paradigms.Frontiers in gastroenterology (Lausanne, Switzerland) · 2026Review
- From AI-AssistedPharmaceuticals (Basel, Switzerland) · 2025Review
- Janus kinase 1 inhibitors for treating immune checkpoint inhibitor-induced enterocolitis - report of two filgotinib-treated cases and literature review.Acta oncologica (Stockholm, Sweden) · 2025Review
- JAK Inhibitor and Crohn's Disease.Biomedicines · 2025Review
- Continuous Treatment with Tofacitinib but Not Filgotinib Is Effective in Non-Responders with Active Ulcerative Colitis: A Propensity Score-Matching Analysis.Journal of clinical medicine · 2025Article
- First-in-human study of CPL'116 - a dual JAK/ROCK inhibitor - in healthy subjects.Frontiers in pharmacology · 2025Article
- Novel Therapies for Patients With Inflammatory Bowel Disease.Gastroenterology & hepatology · 2022Article
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectivesFilgotinib (GLPG0634) is a selective inhibitor of Janus kinase 1 (JAK1) currently in development for the treatment of rheumatoid arthritis and Crohn's disease. While less selective JAK inhibitors have shown long-term efficacy in treating inflammatory conditions, this was accompanied by dose-limiting side effects. Here, we describe the pharmacokinetics of filgotinib and its active metabolite in healthy volunteers and the use of pharmacokinetic-pharmacodynamic modeling and simulation to support dose selection for phase IIB in patients with rheumatoid arthritis.
methodsTwo trials were conducted in healthy male volunteers. In the first trial, filgotinib was administered as single doses from 10 mg up to multiple daily doses of 200 mg. In the second trial, daily doses of 300 and 450 mg for 10 days were evaluated. Non-compartmental analysis was used to determine individual pharmacokinetic parameters for filgotinib and its metabolite. The overall pharmacodynamic activity for the two moieties was assessed in whole blood using interleukin-6-induced phosphorylation of signal-transducer and activator of transcription 1 as a biomarker for JAK1 activity. These data were used to conduct non-linear mixed-effects modeling to investigate a pharmacokinetic/pharmacodynamic relationship.
resultsModeling and simulation on the basis of early clinical data suggest that the pharmacokinetics of filgotinib are dose proportional up to 200 mg, in agreement with observed data, and support that both filgotinib and its metabolite contribute to its pharmacodynamic effects. Simulation of biomarker response supports that the maximum pharmacodynamic effect is reached at a daily dose of 200 mg filgotinib.
conclusionBased on these results, a daily dose range up to 200 mg has been selected for phase IIB dose-finding studies in patients with rheumatoid arthritis.
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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.