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This study will investigate the safety and pharmacokinetics (PK) of a single dose of GSK2256294 in healthy young and elderly subjects to explore the effects of food, gender and age on drug exposure. The biliary metabolites in healthy young males will be investigated using the Entero-test after a single oral dose of GSK2256294. This study will be conducted in two cohorts (Cohort 1 and Cohort 2). Cohort 1 is open label in order to characterise the PK profile of GSK2256294 in healthy young males and also to investigate the biliary metabolites of GSK2256294. Cohort 2 uses a crossover design to allow comparison of the PK parameters of GSK2256294 between in the fed and fasted state within subject and also to compare the PK parameters of GSK2256294 between male and female subjects. A washout period of a minimum of 2 weeks has been chosen to allow and adequate washout of GSK2256294.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Cohort 1 | Experimental | Cohort 1 will enrol 8 healthy male volunteers, who will receive a single 10 mg dose of GSK225694 in the fasted state. |
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| Cohort 2 | Experimental | Cohort 2 will enrol 20 healthy elderly male and female volunteers (10 males and 10 females), who will receive a single 10 mg dose of GSK225694 in the fasted or fed state according to the randomization schedule. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| GSK2256294 | Drug | GSK2256294 is a 5 mg capsule administered orally as a 10 mg dose in the fasted or fed state |
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| Measure | Description | Time Frame |
|---|---|---|
| Cohort 2: PK profiles of a single oral dose of GSK2256294 | PK parameters including area under the concentration-time curve (AUC) and maximum blood concentrations (Cmax), half life (T1/2), time to Cmax (Tmax) following a single oral dose of GSK2256294 administered under fed and fasted conditions in healthy elderly male and female subjects will be estimated | Pre-dose, 15 minutes (min), 30 min, 1 hour (h), 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h (Day 1) and 24 h (Day 2), 48 h (Day 3) and 72 h (Day 4) |
| Cohort 2: Electrocardiogram (ECG) as a measure of safety and tolerability | Twelve-lead ECGs will be obtained as a measure of safety and tolerability | Screening, Pre-dose, 30 min, 2 h, 4 h, 6 h and at follow-up |
| Cohort 2: Adverse events (AEs ) as a measure of safety and tolerability | From the start of study treatment and until approximately 2 weeks after the final dose | |
| Cohort 2: Vital signs as a measure of safety and tolerability | Vital sign measurements will include systolic and diastolic blood pressure (BP) and pulse rate | Screening, Pre-dose, 30 min, 2 h, 4 h, 6 h and at follow-up |
| Cohort 2: Laboratory assessments as a measure of safety and tolerability | Clinical laboratory assessments will include haematology, clinical chemistry, urinalysis and other screening tests | Screening and follow-up. In addition, clinical chemistry will also be done at 12 h (Day 1) and 24 h (Day 2) |
| Measure | Description | Time Frame |
|---|---|---|
| Cohort 1: Biliary metabolite profile of GSK2256294 | Bile will be collected for metabolic analysis of GSK2256294 + metabolites via the use of the Entero-Test capsule in healthy male younger subjects | Until 7 hours post-dose on Day 1 |
| Cohort 1: AEs as a measure of safety and tolerability |
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Inclusion Criteria:
Cohort 1 only: BP <=130/80.
Exclusion Criteria:
Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
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| Name | Affiliation | Role |
|---|---|---|
| GSK Clinical Trials | GlaxoSmithKline | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| GSK Investigational Site | Baltimore | Maryland | 21225 | United States |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 26620151 | Derived | Lazaar AL, Yang L, Boardley RL, Goyal NS, Robertson J, Baldwin SJ, Newby DE, Wilkinson IB, Tal-Singer R, Mayer RJ, Cheriyan J. Pharmacokinetics, pharmacodynamics and adverse event profile of GSK2256294, a novel soluble epoxide hydrolase inhibitor. Br J Clin Pharmacol. 2016 May;81(5):971-9. doi: 10.1111/bcp.12855. Epub 2016 Jan 17. |
| Label | URL |
|---|---|
| Results for study 117023 can be found on the GSK Clinical Study Register. | View source |
| ID | Type | URL | Comment |
|---|---|---|---|
| 117023 | Annotated Case Report Form | View IPD |
Patient-level data for this study will be made available through www.clinicalstudydatarequest.com following the timelines and process described on this site.
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| ID | Term |
|---|---|
| D029424 | Pulmonary Disease, Chronic Obstructive |
| ID | Term |
|---|---|
| D008173 | Lung Diseases, Obstructive |
| D008171 | Lung Diseases |
| D012140 | Respiratory Tract Diseases |
| D002908 | Chronic Disease |
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| ID | Term |
|---|---|
| C584201 | N-((4-cyano-2-(trifluoromethyl)phenyl)methyl)-3-((4-methyl-6-(methylamino)-1,3,5-triazin-2-yl)amino)cyclohexanecarboxamide |
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| From the start of study treatment and until approximately 2 weeks after the final dose |
| Cohort 1: ECG as a measure of safety and tolerability | Twelve-lead ECGs will be obtained to assess safety and tolerability | Screening, Pre-dose, 30 min, 2 h, 4 h, 6 h and at follow-up |
| Cohort 1: Vital signs as a measure of safety and tolerability | Vital sign measurements will include systolic and diastolic BP and pulse rate | Screening, Pre-dose, 30 min, 2 h, 4 h, 6 h and at follow-up |
| Cohort 1: Laboratory assessments as a measure of safety and tolerability | Clinical laboratory assessments will include haematology, clinical chemistry, urinalysis and other screening tests | Screening and follow-up |
| Cohort 1 and Cohort 2: AUC, Cmax, t1/2,and Tmax of GSK2256294 | To compare the pharmacokinetic profiles of single oral doses of GSK2256294 in healthy elderly and healthy younger subjects, and between healthy elderly male and female subjects | Cohort 1: Pre-dose, 15 min, 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 7 h, 12 h and 24 h, 48 h, and 72 h; Cohort 2: Pre-dose, 15 min, 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h and 24 h, 48 h and 72 h |
| Researchers can use this site to request access to anonymised patient level data and/or supporting documents from clinical studies to conduct further research. | View source |
For additional information about this study please refer to the GSK Clinical Study Register |
| 117023 | Statistical Analysis Plan | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 117023 | Dataset Specification | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 117023 | Clinical Study Report | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 117023 | Informed Consent Form | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 117023 | Individual Participant Data Set | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 117023 | Study Protocol | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| D020969 |
| Disease Attributes |
| D010335 | Pathologic Processes |
| D013568 | Pathological Conditions, Signs and Symptoms |