An Open-label Positron Emission Tomography Study to Evaluate Use of Histamine H3 Receptor Radioligand [11C]AZ12807110 and to Determine Histamine H3 Receptor Occupancy of AZD5213 After Oral Administration to Healthy Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- AstraZeneca
- 入组人数
- 13
- 试验地点
- 1
- 主要终点
- Estimation of the plasma concentration resulting in 50% receptor occupancy (Ki, pl).
研究概览
简要总结
The purpose of this study is to investigate features of radioligand [11C]AZ12807110 and how much AZD5213 displaces radioligand from histamine receptors when given together.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Single Group
- 主要目的
- Basic Science
- 盲法
- Single (Participant)
入排标准
- 年龄范围
- 20 Years 至 45 Years（Adult）
- 性别
- Female
- 接受健康志愿者
- 是
入选标准
- •Healthy male and/or female volunteers between 20 to 45 years with suitable veins for cannulation or repeated venipuncture (pilot panel)
- •Female must be of non-child bearing potential (pilot panel)
- •BMI between 18 to 30 30 kg/m2
- •Normal MRI scan
- •Provision of signed, written and dated informed consent
排除标准
- •History of any clinically significant disease or disorder
- •History or presence of gastrointestinal, hepatic or renal disease
- •Prolonged QTcF >450 ms or shortened QTcF <340 ms or family history of long QT syndrome
- •History of severe allergy or hypersensitivity or ongoing allergy or hypersensitivity
- •Healthy volunteer suffers from claustrophobia
研究组 & 干预措施
Main panel
Histamine receptor occupancy reached by AZD5213
干预措施: AZD5213 (Drug)
Pilot panel
[11C]AZ12807110 distribution and kinetics
干预措施: [11C]AZ12807110 (Other)
Main panel
Histamine receptor occupancy reached by AZD5213
干预措施: [11C]AZ12807110 (Other)
结局指标
主要结局
Estimation of the plasma concentration resulting in 50% receptor occupancy (Ki, pl).
时间窗: Venous blood samples for determination of concentrations of AZD5213 in plasma will be taken on many occasions from pre-dose until 48 h post-dose.
Each healthy volunteer in the main panel will complete 3 PET measurements using radioligand; one at baseline and 2 after treatment with AZD5213.
Distribution volume (VT)
时间窗: Venous blood samples for determination of concentrations of AZD5213 in plasma will be taken on many occasions from pre-dose until 48 h post-dose. Single PET measurement will take maximum 2 hours.
次要结局
- Adverse events(Collected from Day 1 to follow-up)
- Vital signs (body temperature, BP and pulse)(Measured at screening, study days -1 to day 3 and at follow-up)