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

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.

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