Clinicaltrials.gov ID
EudraCT ID
EU CT Number
Not applicable
Trial status
Completed
Completed
Trial overview
Official title: An open-label, non-randomized [11C]carfentanil PET study in healthy male subjects to investigate brain mu-opioid receptor occupancy, pharmacokinetics, and pharmacodynamics of single oral doses of GSK1521498 and naltrexone.
Trial description: The purpose of this study is to determine whether GSK1521498 attaches to sites in the brain called mu-opioid receptors that are involved in the liking reactions to palatable high fat and high sugar foods. We hope that blocking these receptors may modify certain behaviours that may lead to obesity.
Primary purpose:
Basic Science
Trial design:
Parallel Assignment
Masking:
None (Open Label)
Allocation:
Non-randomized
Primary outcomes:
The degree and time-course of mu-opioid receptor occupancy by GSK1521498 in brain regions of interest as measured by PET
Timeframe: Assessed at various endpoints to be determined based on emerging results
The relationship between plasma concentration and mu-opioid receptor occupancy by GSK1521498
Timeframe: Assessed at various endpoints to be determined based on emerging results
Secondary outcomes:
Adverse events and clinically relevant changes in electrocardiography (ECG); vital signs (blood pressure, heart rate); POMS, Bond and Lader VAS, laboratory safety data and physical examination
Timeframe: Duration of study
Pharmacokinetic endpoints will be: AUC(0-∞), AUC(0-t), maximum observed plasma drug concentration (Cmax), time to maximum observed plasma drug concentration (Tmax), terminal elimination half-life (t½).
Timeframe: PK samples will be collected throughout the study
The degree and time-course of mu-opioid receptor occupancy by naltrexone in brain regions of interest as measured by PET
Timeframe: Assessed at various endpoints to be determined based on emerging results
The relationship between mu-opioid receptor occupancy by GSK1521498 and naltrexone and fMRI responses during expectation and receipt of a pleasant tasting reward (juice)
Timeframe: During fMRI scanning sessions
Interventions:
Drug: Part A Assessing GSK1521498
Drug: Part B Assessing GSK1521498
Drug: Part C Assessing Naltrexone
Enrollment:
26
Observational study model:
Not applicable
Primary completion date:
Not applicable
Time perspective:
Not applicable
Clinical publications:
Rabiner EA, Beaver J, Makwana A, et al. Pharmacological differentiation of opioid receptor antagonists by molecular and functional imaging of target occupancy and food reward-related brain activation in humans. [Mol Psychiatry]. 2011;16(8):826-835.
Medical condition
Obesity
Product
GSK1521498
Collaborators
Not applicable
Study date(s)
June 2009 to December 2009
Type
Interventional
Phase
1
Participation criteria
Sex
Male
Age
25 - 65 years
Accepts healthy volunteers
Yes
- Healthy male subjects aged between 25 and 65 years old inclusive.
- Body weight ≥ 50 kg and BMI within the range 18.5.0 – 30.0 kg/m2 (inclusive).
- A subject will not be eligible for inclusion in this study if any of the following criteria
- apply:
Inclusion and exclusion criteria
Inclusion criteria:
- Healthy male subjects aged between 25 and 65 years old inclusive.
- Body weight ≥ 50 kg and BMI within the range 18.5.0 – 30.0 kg/m2 (inclusive).
- Normal ECG.
- The subject is able to read, comprehend and record information.
- A signed and dated written informed consent is obtained from the subject.
- Compliance with birth control methods as described in the study protocol.
Exclusion criteria:
- A subject will not be eligible for inclusion in this study if any of the following criteria apply:
- The subject has a positive pre-study drug/alcohol screen.
- History of hepatitis B and /or C
- A positive result for an HIV test.
- Abnormal thyroid function
- Positive evaluation for depression.
- History of heavy alcohol use as described in the study protocol.
- The subject has participated in a clinical trial and has received an investigational product within: 90 days.
- Participation in other drug studies within a calendar year.
- Use of prohibited medications as described in the study protocol.
- History of sensitivity to any of the study medications.
- Where participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56 day period
- Unwillingness or inability to follow the procedures outlined in the protocol.
- Past or present use of tobacco products.
- Consumption of red wine, seville oranges, grapefruit or grapefruit juice from 7 days prior to the first dose of study medication.
- Previous radiation dosages in excess of levels acceptable to take part in this study.
- History of claustrophobia or history of neurological conditions.
- Presence of a cardiac pacemaker.
- Works as a welder, metal worker or machinist
Trial location(s)
Study documents
Clinical study report
Available language(s): English
Scientific result summary
Available language(s): English
If you wish to request for full study report, please contact - [email protected]
Results overview
Refer to study documents
Recruitment status
Completed
Actual primary completion date
Not applicable
Actual study completion date
2009-07-12
Plain language summaries
Plain language summaries of clinical trial results for Phase 2-4 clinical trials that were initiated on or after January 2022 will be posted by GSK within one year following study completion.
Additional information about the trial
Participate in clinical trial
Additional information
Researchers can use this site to request access to anonymised patient level data and/or supporting documents from clinical studies to conduct further research.
Click hereResults for study 111848 can be found on the GSK Clinical Study Register.
Click hereAccess to clinical trial data by researchers
Visit website