An Open Label Positron Emission Tomography (PET) Study of GSK618334 in Healthy Male Subjects Using 11C-PHNO as PET Ligand

An Open Label Positron Emission Tomography Study in Healthy Male Subjects to Investigate Brain Dopamine D3 Receptor Occupancy, Pharmacokinetics and Safety of Single Oral Doses of GSK618334, Using 11C-PHNO as PET Ligand.

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT00814957

Enrollment

Registered

2008-12-25

Start date

2008-12-08

Completion date

2009-06-11

Last updated

2017-07-07

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Substance Dependence

Keywords

positron emission tomography, addiction

Brief summary

The purpose of this study is to investigate the relationship between the plasma concentrations of the study drug and the amount of the study drug bound to the D3 receptors of the brain after dosing of a new compound GSK618334.

Detailed description

This imaging study will be an open label, non-randomised PET receptor occupancy study using healthy male volunteers. The time course and degree of D3 receptor occupancy (RO) after single doses of GSK618334 will be determined using 11C-PHNO as a PET ligand labeling dopamine receptor. The PK/PD relationship between plasma concentrations of GSK618334 and D3 RO will be described. Potential relationships between D3 RO and functional magnetic resonance imaging (fMRI) endpoints will be assessed as an exploratory aim.

Interventions

DRUGGSK618334

D3 receptor antagonist

Study design

Allocation

NON_RANDOMIZED

Intervention model

SINGLE_GROUP

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

MALE

Age

30 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

* healthy, male subjects aged between 30 and 55 old inclusive. * normal body weight. * normal ECG and vital signs. * agree to use acceptable contraceptive methods required. * capable of giving written informed consent.

Exclusion criteria

* smoker or uses other nicotine-containing products. * certain medical conditions including heart disease, neurological disease, gastrointestinal disease, kidney or liver dysfunction - abnormal laboratory tests. * certain psychiatric conditions and use of certain psychoactive drugs . * positive blood alcohol or urine drug test. * alcohol intake over 14 drinks per week. * participation in another drug trial within 30 days or a study involving significant radiation exposure. * donation of more than 450 mL blood within the 56 days. * family history of cancer (one or more first-degree relative diagnosed before the age of 55 years old). * having cardiac pacemaker or other electronic device. * suffers from claustrophobia or feels that he will be unable to lie still on his back in the PET camera.

Design outcomes

Primary

Measure	Time frame
Binding of PHNO, PET ligand, in each region of interest at each scan.	up to 48 hours
Percentage of PHNO, PET ligand, occupancy in each region of interest after a single oral dose of GSK618334 for each individual.	up to 48 hours
Time course of GSK618334 concentration in blood following a single oral dose.	up to 48 hours

Secondary

Measure	Time frame
Adverse events and other safety assessments such as clinically relevant changes in electrocardiography (ECG); vital signs (blood pressure, heart rate); laboratory safety data and physical examination.	screening to follow-up
Measuring GSK618334 in the body (pharmacokinetic endpoints): PK parameters of GSK618334 Cmax, AUCinf, tmax.	up to 48 hours

Countries

United Kingdom

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026