Brain Uptake of GSK1034702: a Positron Emission Tomography (PET) Scan Study

This study has been completed.
Sponsor:
Information provided by (Responsible Party):
GlaxoSmithKline
ClinicalTrials.gov Identifier:
NCT00937846
First received: June 25, 2009
Last updated: August 23, 2012
Last verified: February 2011
  Purpose

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).


Condition Intervention Phase
Healthy Subjects
Cognitive Disorders
Drug: GSK1034702
Phase 1

Study Type: Interventional
Study Design: Endpoint Classification: Pharmacokinetics/Dynamics Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Supportive Care
Official Title: An Open Label Positron Emission Tomography (PET) Study to Investigate Brain Penetration by [11C] GSK1034702 in Healthy Subjects

Resource links provided by NLM:


Further study details as provided by GlaxoSmithKline:

Primary Outcome Measures:
  • Volume of distribution of [11C]GSK1034702 at tracer and pharmacological doses. [ Time Frame: Scanning day ] [ Designated as safety issue: No ]

Secondary Outcome Measures:
  • The kinetic rate constants at tracer and pharmacological doses. [ Time Frame: Scanning day ] [ Designated as safety issue: No ]
  • GSK1034702 PK parameters: Cmax; tmax; AUC(0-t). [ Time Frame: Scanning day ] [ Designated as safety issue: No ]
  • Safety and tolerability endpoints consisting of: AEs; 12-lead ECG; 12 lead digital Holter and lead II telemetry; vital signs; clinical laboratory evaluations. [ Time Frame: 2 weeks ] [ Designated as safety issue: Yes ]

Enrollment: 4
Study Start Date: July 2009
Study Completion Date: October 2009
Primary Completion Date: October 2009 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: GSK1034702 Drug: GSK1034702
Single oral 5 mg dose in liquid formulation

Detailed Description:

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.

  Eligibility

Ages Eligible for Study:   35 Years to 55 Years
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Generally healthy.
  • Male between 35 and 55 years of age.
  • Willing to use appropriate contraception method.
  • Weight more than 50 kg.
  • BMI within the range 19 - 29 kg/m2.
  • Adequate blood supply to the hand.

Exclusion Criteria:

  • Abuse of drugs or alcohol.
  • Smoker or history of regular use of tobacco- or nicotine-containing products in the past 6 months.
  • ECG abnormality (personal or family history).
  • Psychiatric disorder.
  • Asthma or a history of asthma.
  • Medical illness.
  • Worked as a welder, metal worker or machinist.
  • Suffers from claustrophobia or would be unable to lie still in a PET or MRI scanner for 1-2 hours.
  • Has a cardiac pacemaker or other electrical device or ferromagnetic metal foreign bodies.
  • Neurological disorder
  Contacts and Locations
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT00937846

Locations
United Kingdom
GSK Investigational Site
London, United Kingdom, NW10 7EW
GSK Investigational Site
London, United Kingdom, W12 ONN
Sponsors and Collaborators
GlaxoSmithKline
Investigators
Study Director: GSK Clinical Trials GlaxoSmithKline
  More Information

No publications provided

Responsible Party: GlaxoSmithKline
ClinicalTrials.gov Identifier: NCT00937846     History of Changes
Other Study ID Numbers: 110771
Study First Received: June 25, 2009
Last Updated: August 23, 2012
Health Authority: United Kingdom: Appointing Authority for Phase 1 Ethics Committees (AAPEC)
United States: Food and Drug Administration

Keywords provided by GlaxoSmithKline:
Cognitive impairment
Schizophrenia
Alzheimer's Disease
PET

Additional relevant MeSH terms:
Cognition Disorders
Delirium, Dementia, Amnestic, Cognitive Disorders
Mental Disorders

ClinicalTrials.gov processed this record on August 28, 2014