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GSK1034702 is being developed for improving cognitive impairment in diseases such as Alzheimer's disease and schizophrenia. This study will be done in healthy men to investigate how much of the study drug gets into the brain. This will be done using Positron Emission Tomography (PET).
This is an open label, single dose, non-randomized PET study in healthy male subjects to ascertain if GSK1034702 is crossing the blood-brain barrier to enable it to elicit a central effect. GSK1034702 has been shown in vitro to be a substrate for human Pgp, therefore the distribution of GSK1034702 into human brain could be adversely affected. This use of PET in conjunction with radioactively labelled GSK1034702 will help ascertain the role Pgp plays in limiting brain penetration in the presence and absence of a pharmacological relevant oral non labelled dose of 5 mg. Subjects will have an MRI scan to aid definition of brain anatomy, a baseline PET scan and a post-dose PET scan. For each subject the study will consist of at least three visits; screening visit, scanning day and follow-up.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| GSK1034702 | Experimental | Single oral 5 mg dose in liquid formulation |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| GSK1034702 | Drug | Single oral 5 mg dose in liquid formulation |
|
| Measure | Description | Time Frame |
|---|---|---|
| Volume of distribution of [11C]GSK1034702 at tracer and pharmacological doses. | Scanning day |
| Measure | Description | Time Frame |
|---|---|---|
| The kinetic rate constants at tracer and pharmacological doses. | Scanning day | |
| GSK1034702 PK parameters: Cmax; tmax; AUC(0-t). | Scanning day | |
| Safety and tolerability endpoints consisting of: AEs; 12-lead ECG; 12 lead digital Holter and lead II telemetry; vital signs; clinical laboratory evaluations. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| GSK Clinical Trials | GlaxoSmithKline | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| GSK Investigational Site | London | NW10 7EW | United Kingdom | |||
| GSK Investigational Site |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 26116126 | Derived | Ridler K, Cunningham V, Huiban M, Martarello L, Pampols-Maso S, Passchier J, Gunn RN, Searle G, Abi-Dargham A, Slifstein M, Watson J, Laruelle M, Rabiner EA. An evaluation of the brain distribution of [(11)C]GSK1034702, a muscarinic-1 (M 1) positive allosteric modulator in the living human brain using positron emission tomography. EJNMMI Res. 2014 Dec;4(1):66. doi: 10.1186/s13550-014-0066-y. Epub 2014 Dec 5. |
| Label | URL |
|---|---|
| Results for study 110771 can be found on the GSK Clinical Study Register. | View source |
| ID | Type | URL | Comment |
|---|---|---|---|
| 110771 | Clinical Study Report | 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 |
|---|---|
| D060825 | Cognitive Dysfunction |
| D012559 | Schizophrenia |
| D000544 | Alzheimer Disease |
| ID | Term |
|---|---|
| D003072 | Cognition Disorders |
| D019965 | Neurocognitive Disorders |
| D001523 | Mental Disorders |
| D019967 | Schizophrenia Spectrum and Other Psychotic Disorders |
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| ID | Term |
|---|---|
| C568644 | GSK 1034702 |
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| 2 weeks |
| London |
| W12 ONN |
| United Kingdom |
| 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 |
| 110771 | Individual Participant Data Set | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 110771 | Statistical Analysis Plan | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 110771 | Study Protocol | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 110771 | Informed Consent Form | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 110771 | Dataset Specification | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 110771 | Annotated Case Report Form | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| D003704 | Dementia |
| D001927 | Brain Diseases |
| D002493 | Central Nervous System Diseases |
| D009422 | Nervous System Diseases |
| D024801 | Tauopathies |
| D019636 | Neurodegenerative Diseases |