An Open Label Positron Emission Tomography (PET) Study to Investigate the Brain Biodistribution of 18F-GSK2647544 in Healthy Subjects
试验速览
- 阶段
- 1 期
- 状态
- 终止
- 入组人数
- 4
- 试验地点
- 1
- 主要终点
- Whole brain PET VT of [18F]-GSK2647544
研究概览
简要总结
This is an open label, PET study in healthy male subjects to determine if GSK2647544 is able to cross the blood-brain-barrier. The study will use GSK2647544 radiolabelled with fluorine-18 ([18F] GSK2647544) to determine the ratio of the concentration of the compound in tissue to that in plasma at equilibrium, expressed as the PET volume of distribution (VT). The study will consist of at least four visits; 2 screening visits, scanning day and follow-up. On Day 1 (scanning day) the subject will receive a single oral dose of GSK2647544 (100 mg) followed approximately 2 hours later by a single intravenous (IV) infusion of [18F]-GSK2647544 and a dynamic PET scan. Arterial and venous blood sampling will be used to determine the plasma kinetics of [18F]-GSK2647544 and unlabeled GSK2647544. In addition, each subject will undergo a structural magnetic resonance imaging (MRI) scan of the brain to aid in the definition of neuroanatomy. The dose of GSK2647544 was selected based on the review of the safety, tolerability, pharmacokinetics (PK), and pharmacodynamic (PD) data obtained in the first time in human (FTIH) study.
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 30 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- 未提供
排除标准
- 未提供
研究组 & 干预措施
GSK2647544 oral and [18F]GSK2647544 IV bolus
All subjects will receive a single oral dose of GSK2647544 100 milligram (mg) approximately 2 hours before administration of [18F] GSK2647544 and a dynamic PET scan. [18F]-GSK2647544 will be administered to the subject as an IV bolus during the PET scan, which will be conducted for up to 120 minute post the injection of [18F]GSK2647544
干预措施: GSK2647544 oral (Drug)
GSK2647544 oral and [18F]GSK2647544 IV bolus
All subjects will receive a single oral dose of GSK2647544 100 milligram (mg) approximately 2 hours before administration of [18F] GSK2647544 and a dynamic PET scan. [18F]-GSK2647544 will be administered to the subject as an IV bolus during the PET scan, which will be conducted for up to 120 minute post the injection of [18F]GSK2647544
干预措施: [18F]GSK2647544 IV bolus (Drug)
结局指标
主要结局
Whole brain PET VT of [18F]-GSK2647544
时间窗: At Day 1
The subject will be administered GSK2647544 radiolabelled with fluorine-18 (\[18F\]-GSK2647544) to determine the ratio of the concentration of the compound in tissue to that in plasma at equilibrium, expressed as the PET VT
次要结局
- Safety and tolerability assessment following oral administration of GSK2647544(Up to Day 14)
- GSK2647544 PK assessment(Pre dose and at 30minute, 1, 2, 4, 6 hours post dose on Day 1)