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.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
SUPPORTIVE_CARE
Masking
NONE
Enrollment
4
Single oral 5 mg dose in liquid formulation
GSK Investigational Site
London, United Kingdom
GSK Investigational Site
London, United Kingdom
Volume of distribution of [11C]GSK1034702 at tracer and pharmacological doses.
Time frame: Scanning day
The kinetic rate constants at tracer and pharmacological doses.
Time frame: Scanning day
GSK1034702 PK parameters: Cmax; tmax; AUC(0-t).
Time frame: 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.
Time frame: 2 weeks
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.