Human Proof of Concept Positron Emission Tomography Study to Investigate [11C]-RO5011232 as a Radiotracer for Brain mGlu5 Receptor Occupancy and to Investigate the Binding of RO4917523 to Human mGlu5 Brain Receptor at Steady-state.
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 56
- 主要终点
- Part I: mGlu5 receptor binding of [11C]-RO5011232 radiotracer in human brain, assessed by positron emission tomography (PET)
研究概览
简要总结
This open label, non-randomized, parallel group study will evaluate [11C]-RO5011232 as radiotracer for brain mGlu5 receptor occupancy and investigate the binding of RO49917523 to human mGlu5 brain receptor at steady-state in healthy volunteers. In Parts I, II and III, positron emission tomography (PET) assessments of specific uptake of the radiotracer and whole body dosimetry will be made after intravenous injection of [11C]-RO5011232. In Part IV, subjects will receive RO4917523 orally daily for 14 days while receiving three single intravenous bolus injections of [11C]-RO5011232. The anticipated time on study treatment is up to 4 weeks.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Parallel
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 65 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Healthy male and female volunteers as determined by medical history, physical examination, 12-lead ECG, and routine clinical laboratory measurements
- •Age 18 to 65 years inclusive
- •Body mass index (BMI) between 18 to30 kg/m2 inclusive and body weight at least 50 kg
- •Appropriate body size (less than 195 cm [6 feet and 5 inches]) in order to accommodate the whole body scanning
排除标准
- •History of or presence of clinically significant psychiatric condition, as evaluated by a psychiatrist before enrolment
- •History of head trauma with prolonged loss of consciousness (>10 minutes) or any neurological condition or a history of migraine headaches
- •Contraindications to MRI procedures (Part I, III and IV)
- •Subjects suffering from claustrophobia or who would be unable to undergo magnetic resonance imaging (MRI) or PET scanning
- •Positive pregnancy test at screening or on any day preceding a PET scan
- •Lactating women
- •Positive for hepatitis B, hepatitis C or HIV infection
- •Any history of alcohol or drug abuse within the last 6 months
- •Regular smoker or nicotine user (>10 cigarettes per day)
- •Participation in an investigational drug or device study within three months prior to screening
研究组 & 干预措施
Concept Proof
干预措施: RO5011232 (Drug)
Receptor Occupancy
干预措施: RO4917523 (Drug)
Receptor Occupancy
干预措施: RO5011232 (Drug)
结局指标
主要结局
Part I: mGlu5 receptor binding of [11C]-RO5011232 radiotracer in human brain, assessed by positron emission tomography (PET)
时间窗: approximately 6 months
Part IV: Correlation between RO4917523 plasma concentration and R04917523 binding to mGlu5 receptor in brain
时间窗: approximately 6 months
Part II: Dosimetry/radiation safety of [11C]-RO5011232 assessments by whole body PET scan
时间窗: approximately 6 months
Part III: Measurement of test-retest precision of PET images of regions of interest in the human brain
时间窗: approximately 6 months
次要结局
- Part IV: In vitro binding potential (reference region with no specific binding of radiotracer) assessed by PET(approximately 6 months)
- Part IV: Safety of 14-day treatment with RO4917523: Incidence of adverse events(approximately 6 months)
- Safety of [11C]-RO5011232 administered intravenously at microdose level: Incidence of adverse events(approximately 6 months)