Health
Conditions
Brief summary
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.
Detailed description
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.
Interventions
DRUGBrexpiprazole
Brexpiprazole , single/oral/with fasting
Sponsors
Otsuka Beijing Research Institute
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
OTHER
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* 1\. 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) \[ body mass index (BMI) = body weight (kg) / height2 (m2)\].
Exclusion criteria
* 1\. 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
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| The peak concentration (Cmax) after the first administration | 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 |
| The peak time (Tmax) after the first administration | 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) | 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. |
| Half time after the first administration | 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. |
| Apparent clearance after the first administration | 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 |
| Proportional dose-response relationship between pharmacokinetic parameters Cmax and AUC of OPC-34712 | 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 |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Blood pressure | 0, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours | To seeess blood pressure after administration of brexpiprazole |
| urinary routine | 24, 96, 264 hours | To seeess urinary routine after administration of brexpiprazole |
| Heart rate | 0, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours | To seeess heart rate after administration of brexpiprazole |
| Body weight | 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours | To seeess Body weight after administration of brexpiprazole |
| 12-lead ECG | 3, 6, 24, 72, 96, 120, 264 hours | To seeess 12-lead ECG after administration of brexpiprazole |
| Blood biochemistry | 24, 96, 264 hours | To seeess blood biochemistry after administration of brexpiprazole |
| Blood routine | 24, 96, 264 hours | To seeess blood routine after administration of brexpiprazole |
Countries
China
Outcome results
None listed