A Phase I , Open-Label Study to Evaluate the Absorption, Metabolism and Excretion of [14C]-PBT2 and to Estimate the Absolute Bioavailability of PBT2 in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 6
- 试验地点
- 1
- 主要终点
- Mass Balance
研究概览
简要总结
The purpose of the study is to investigate how the test drug, PBT2, is taken up, broken down and removed from the body when given as an oral capsule, a radiolabelled oral suspension and a radiolabelled intravenous injection.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Single Group
- 主要目的
- Basic Science
- 盲法
- None
入排标准
- 年龄范围
- 30 Years 至 65 Years（Adult, Older Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy males
- •Body mass index of 18.0 to 35.0 kg/m2
排除标准
- •History of any drug or alcohol abuse in the past 2 years
- •Regular alcohol consumption >21 units per week (1 unit = ½ pint beer, 25 mL of 40% spirit or a 125 mL glass of wine)
- •Current smokers and those who have smoked within the last 12 months
- •Radiation exposure, including that from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years.
- •Clinically significant abnormal biochemistry, haematology or urinalysis as judged by the investigator
- •Positive drugs of abuse test result
- •Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) results
- •History of cardiovascular, renal, hepatic, chronic respiratory or GI disease as judged by the investigator
研究组 & 干预措施
Absolute Bioavailability
IV PBT2 microtracer and oral PBT2 single dose
干预措施: IV PBT2 microtracer and oral PBT2 single dose (Drug)
Radiolabelled AME
oral 14C PBT2
干预措施: oral 14C-PBT2 (Drug)
结局指标
主要结局
Mass Balance
时间窗: 168 h (7 days) post dose
Amount excreted as a percentage of the administered dose (%Ae)
Absolute Bioavailability of PBT2 (F%)
时间窗: 0 to 72 hours post oral dose
Absolute bioavailability is the amount of drug from a formulation that reaches the systemic circulation relative to an IV dose, computed as AUC(oral)/AUC(IV), with range from 0% (no drug) to 100% (all of the administered drug).
次要结局
- Oral PK Profile of PBT2 as Assessed by AUC(0-last)(72 h post oral dose)
- Ratio of Whole Blood, Plasma [14C] PBT2 at 24 Hours(0 to 24 hours)
- Oral PK Profile of [14C]-PBT2 as Assessed by AUC(0-last)(0 to 72 hours)
- IV PK Profile of [14C]-PBT2 and Total Radioactivity as Assessed by AUC(0 Last)(0 to 72 h post oral dose)
- Safety and Tolerability of PBT2(72 h post oral dose)