A Single-center, Open-label Study Evaluating the Pharmacokinetics, Tolerability and Safety of Single Dose Oral Brexpiprazole Tablets in Healthy Chinese Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 30
- 试验地点
- 1
- 主要终点
- The peak concentration (Cmax) after the first administration
研究概览
简要总结
This study is a single-center, open-label study evaluating the pharmacokinetics, tolerability and safety of single dose oral brexpiprazole tablets in healthy Chinese subjects. A total of 30 healthy adult subjects are to be enrolled into the study. Three dose groups will be set up, with about 10 subjects in each dose group. Subjects will enter 1 mg, 2 mg and 4 mg dose groups in sequence.
详细描述
A total of 30 healthy adult subjects are to be enrolled into the study. Three dose groups will be set up, with about 10 subjects in each dose group. Subjects will enter 1 mg, 2 mg and 4 mg dose groups in sequence.
After the clinical trial responsible physicians obtain the informed consent forms from subjects, the subjects will be screened 14 days to 1 days prior to taking the study drug (D-14~D-1).
One day prior to dosing in each group (D-1), the included subjects are hospitalized On the next day (D1), after completed the hospitalization inspection, eligible subjects will be assigned subject numbers to start with the first dose, complete corresponding examination, stay in hospital for observation and be discharged on Day 4 of medication. On days 6, 8, 10, 12 blood samples are collected and safety evaluation will be performed. Telephone follow-up will be performed on day Day31.
Blood samples are collected to determine and evaluate blood concentrations of Brexpiprazole and its main metabolite DM-3411 before dosing, and 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours after dosing, with 18 sampling points in total.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Parallel
- 主要目的
- Other
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 45 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Sign the informed consent form
- •2.At the age of 18~45 years old (including upper and lower limits) when signing the informed consent form.
- •3.Body weight of not less than 50kg, BMI 19 ~ 24kg/m2 (including the upper and lower limits) [ body mass index (BMI) = body weight (kg) / height2 (m2)].
排除标准
- •Participated in any interventional clinical trial within 12 weeks prior to enrollment.
- •2.Drug abuse in the past 2 years or a history of abuse
- •3.Drinking alcohol more than 2 unit per day (1 unit= 360 ml beer , or 45 ml 4.0% alcohol, or 150 ml liquor, or 50 ml wine ) 6 months before the screening, or subjects can not stop drinking during the hospitalization
研究组 & 干预措施
1 mg dosing group
Dosing group 1, single/oral/with fasting, Brexpiprazole 1.0 mg, 1 tablets
干预措施: Brexpiprazole (Drug)
2 mg dosing group
Dosing group 2, single/oral/with fasting, Brexpiprazole 1.0 mg, 2 tablets
干预措施: Brexpiprazole (Drug)
4 mg dosing group
Dosing group 3, single/oral/with fasting, Brexpiprazole 1.0 mg, 4 tablets
干预措施: Brexpiprazole (Drug)
结局指标
主要结局
The peak concentration (Cmax) after the first administration
时间窗: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
The peak concentration (Cmax) of Brexipiprazole and the metabolite DM-3411 after administration
Half time after the first administration
时间窗: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
The half time of Brexipiprazole after administration are calculated.
Proportional dose-response relationship between pharmacokinetic parameters Cmax and AUC of OPC-34712
时间窗: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
To assess the Proportional dose-response relationship between pharmacokinetic parameters Cmax and AUC of OPC-34712
The peak time (Tmax) after the first administration
时间窗: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
The peak-time of Brexipiprazole and the metabolite DM-3411 on the first day after administration are calculated.
Area under the plasma concentration-time curve (AUC0-264h)
时间窗: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
The area under the plasma concentration-time curve of Brexipiprazole after administration are calculated.
Apparent clearance after the first administration
时间窗: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
To assess the apparent clearance after administration (CL/F) of Brexipiprazole after the first administration
次要结局
- Body weight(1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours)
- urinary routine(24, 96, 264 hours)
- Blood pressure(0, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours)
- Blood biochemistry(24, 96, 264 hours)
- Heart rate(0, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours)
- Blood routine(24, 96, 264 hours)
- 12-lead ECG(3, 6, 24, 72, 96, 120, 264 hours)