Trial reportBritish journal of clinical pharmacology2016
Pharmacokinetics, pharmacodynamics and adverse event profile of GSK2256294, a novel soluble epoxide hydrolase inhibitor.
Trial report in British journal of clinical pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 105 papers.
What it found
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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
105 citing papers in PubMed, 174 citations in OpenAlex.
- A Double-Blind, Randomized, Placebo-Controlled Trial of Soluble Epoxide Hydrolase Inhibition in Patients with Aneurysmal Subarachnoid Hemorrhage.Neurocritical care · 2022Trial
- Omega-3 polyunsaturated fatty acids protect against inflammation through production of LOX and CYP450 lipid mediators: relevance for major depression and for human hippocampal neurogenesis.Molecular psychiatry · 2021Trial
- GSK2256294 Decreases sEH (Soluble Epoxide Hydrolase) Activity in Plasma, Muscle, and Adipose and Reduces F2-Isoprostanes but Does Not Alter Insulin Sensitivity in Humans.Hypertension (Dallas, Tex. : 1979) · 2021Trial
- Pharmacokinetics, pharmacodynamics and adverse event profile of GSK2256294, a novel soluble epoxide hydrolase inhibitor.British journal of clinical pharmacology · 2016Trial
- On-DNA photochemical methods for expanding DNA-encoded library (DEL) chemical space.RSC medicinal chemistry · 2026Review
- The blood pressure-lowering effect of an anti-soluble epoxide hydrolase vaccine in angiotensin II-induced hypertension in mice.Hypertension research : official journal of the Japanese Society of Hypertension · 2026Article
- Design and synthesis of novel sEH inhibitors for the treatment of acute lung injury.European journal of medicinal chemistry · 2026Article
- Allosteric ensembles elucidate mechanisms of inhibition in the human soluble epoxide hydrolase.Communications biology · 2026Article
- Epoxyeicosatrienoic acids protect airway epithelial mitochondria by activating the cAMP/PKA-DRP1 Ser637 axis in cigarette smoke-induced lung injury.Respiratory research · 2026Article
- Soluble epoxide hydrolase in the liver orchestrates abdominal aortic aneurysm formation in mice.Communications biology · 2026Article
- Design, Synthesis, and Structure-Activity Relationships of Substituted Phenyl Cyclobutylureas as Potential Modulators of Inflammatory Responses.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Lipid metabolism in homeostasis and disease.Signal transduction and targeted therapy · 2026Review
- Epoxy-oxylipins direct monocyte fate in inflammatory resolution in humans.Nature communications · 2026Article
- Target Abundance in Pharmacological Target-Mediated Drug Disposition (TMDD) for Small Molecules - A Proteomics Approach.The AAPS journal · 2026Article
- Article
- Epoxide Hydrolase Inhibitors for the Treatment of Alzheimer's Disease and Other Neurological Disorders: A Comprehensive Review.Biomedicines · 2025Review
- Review
- Design and Synthesis of Novel sEH Inhibitors for the Treatment of Inflammatory Bowel Disease.Journal of medicinal chemistry · 2025Article
- Structure-Based Design of PROTACS for the Degradation of Soluble Epoxide Hydrolase.Journal of medicinal chemistry · 2025Article
- Coamorphous Solid Dispersion of a Soluble Epoxide Hydrolase Inhibitor t-TUCB with Amino Acid l-Arginine.Organic process research & development · 2025Article
45 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
11 authors at 5 institutions in 3 countries.
Funding
Abstract
aimsEndothelial-derived epoxyeicosatrienoic acids may regulate vascular tone and are metabolized by soluble epoxide hydrolase enzymes (sEH). GSK2256294 is a potent and selective sEH inhibitor that was tested in two phase I studies.
methodsSingle escalating doses of GSK2256294 2-20 mg or placebo were administered in a randomized crossover design to healthy male subjects or obese smokers. Once daily doses of 6 or 18 mg or placebo were administered for 14 days to obese smokers. Data were collected on safety, pharmacokinetics, sEH enzyme inhibition and blood biomarkers. Single doses of GSK2256294 10 mg were also administered to healthy younger males or healthy elderly males and females with and without food. Data on safety, pharmacokinetics and biliary metabolites were collected.
resultsGSK2256294 was well-tolerated with no serious adverse events (AEs) attributable to the drug. The most frequent AEs were headache and contact dermatitis. Plasma concentrations of GSK2256294 increased with single doses, with a half-life averaging 25-43 h. There was no significant effect of age, food or gender on pharmacokinetic parameters. Inhibition of sEH enzyme activity was dose-dependent, from an average of 41.9% on 2 mg (95% confidence interval [CI] -51.8, 77.7) to 99.8% on 20 mg (95% CI 99.3, 100.0) and sustained for up to 24 h. There were no significant changes in serum VEGF or plasma fibrinogen.
conclusionsGSK2256294 was well-tolerated and demonstrated sustained inhibition of sEH enzyme activity. These data support further investigation in patients with endothelial dysfunction or abnormal tissue repair, such as diabetes, wound healing or COPD.
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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.