Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
| NCT ID | Title | Phase | Status | Enrollment | Velocity | Design | Start | Completion | Last Updated | Sites | Countries |
|---|---|---|---|---|---|---|---|---|---|---|---|
| NCT00976066 | [11C]Carfentanil PET Study of GSK1521498 | PHASE1 | COMPLETED | 26 | — | — | Jun 15, 2009 | Dec 7, 2009 | Jun 20, 2017 | 1 | United Kingdom |
| Arm | Type | Description |
|---|---|---|
| GSK1521498 | EXPERIMENTAL | Subjects will receive a dose of the experimental compound GSK1521498 |
| Naltrexone | ACTIVE_COMPARATOR | Subjects will receive a dose of the licensed pharmaceutical product, Naltrexone |
| Name | Type | Description |
|---|---|---|
| Part A Assessing GSK1521498 | DRUG | Each participant will receive up to three \[11C\]carfentanil PET scans and up to two doses of GSK1521498 in total. The doses used will span the expected receptor occupancy range providing these were well tolerated in the first-time in human study. Each subject will receive baseline \[11C\]carfentanil PET and fMRI scans (PET Scan 1 and fMRI Scan 1, respectively), followed by two treatment sessions (Treatment Sessions 1 and 2). Treatment session 1 and 2 are followed by PET scans and an fMRI scan (session 1 only). Sessions will be separated by at least 12 days. PET scans will be timed to coincide with peak brain occupancy. fMRI will begin approximately 30-60 minutes after completion of the PET scan. |
| Part B Assessing GSK1521498 | DRUG | The purpose of Part B is to establish the timecourse of receptor occupancy of GSK1521498. Each participant in Part B will receive up to three \[11C\]carfentanil PET scans and one single oral dose of GSK1521498 expected to provide 50-75% receptor occupancy (selected with reference to data from Part A). Each Part B subject will receive baseline \[11C\]carfentanil PET and fMRI scans (PET Scan 1 and fMRI Scan 1, respectively) followed by a single treatment session. The treatment session will consist of a single oral dose of GSK1521498 followed by two subsequent PET scans (PET Scans 2 and 3) and one fMRI scan (fMRI Scan 2). |
| Part C Assessing Naltrexone | DRUG | A range of doses of naltrexone will be tested in up to 12 participants in an adaptive design. Each Part C participant will receive up to three \[11C\]carfentanil PET scans and a single oral dose of naltrexone. No dose of naltrexone will exceed 50 mg, the dose usually used therapeutically in the treatment of opiate and alcohol dependence. Each Part C subject will receive baseline \[11C\]carfentanil PET and fMRI scans (PET Scan 1 and fMRI Scan 1, respectively) followed by a single treatment session. The treatment session will consist of a single oral dose of naltrexone followed by two subsequent PET scans (PET Scans 2 and 3) and one fMRI scan (fMRI Scan 2). |
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 ob...