Clinical trial NCT03734302: The Pharmacokinetics, and Safety of Brexpiprazole Tablets in Chinese Healthy Subjects
Official title: A Single-center, Open-label Study Evaluating the Pharmacokinetics, and Safety of Multiple Dose Oral Brexpiprazole Tablets (1 mg) in Chinese Healthy Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Otsuka Beijing Research Institute
Sponsor class: INDUSTRY
First posted: 2018-11-07
Enrollment: 10
Sex: ALL
Minimum age (years): 18
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: OTHER

Brief summary: This study is a single-center, open-label study evaluating the pharmacokinetics and safety of multiple dose oral administration of Brexpiprazole (1 mg) tablets in Chinese healthy subject.10 healthy adult subjects will be enrolled in this study. A single dose (Brexpiprazole 1 mg) group is set and the test drug will be administered for 14 consecutive days.

Detailed description: 10 healthy adult subjects will be enrolled in this study. A single dose (Brexpiprazole 1 mg) group is set and the test drug will be administered for 14 consecutive days.

After receiving the informed consent form the subject themselves, the investigators start the screening 14 days to 1 days prior to taking the study drug (D-14 to D-1).

One day before first dosing (D-1), subjects are hospitalized. On the next day (D1), after completed the hospitalization inspection, eligible subjects will be selected to start with the first dose, and from day 1 to day 14 (D1 to D14), continue once daily dosing and complete the corresponding inspection, observation and blood sampling. They continue hospitalization and are discharged on day 17 (D17) after completing the relevant examinations. On days 19, 21, 23，25 (D19, D21，D23 and D25), blood samples are collected and safety evaluation is performed.

Telephone follow-up is performed on day 44 (D44, 30 days after the last dose of the drug).

Subjects who early terminated the test after taking the study drug should be tested at the end of the study (D25/ET) as far as possible.

Blood samples for pharmacokinetic evaluation are collected before daily dosing; D1 (before dosing, and 1, 2, 3, 4, 5, 6, 8, 12 hours after dosing), D2 (before dosing and 24 hours after first dosing), D10 (before dosing), D11 (before dosing), D12 (before dosing), D13 (before dosing), D14 (before dosing, and 1, 2, 3, 4, 5, 6, 8, 12 hours after dosing), D15 (24 hours after last dosing), D16 (48 hours after last dosing), D17 (72 hours after last dosing), D18 (96 hours after last dosing), D19 (120 hours after last dosing), D21 (168 hours after last dosing),D23 (216 hours after last dosing), D25 (264 hours after last dosing). 31 Blood samples collecting points in total.

Eligibility criteria: Inclusion Criteria:

* 1. Sign the informed consent form
* 2. At the age of 18\~45 years old (including upper and lower limits).
* 3. Body weight of not less than 45 kg, body mass index 19 \~ 25kg/m2 range (including the upper and lower limits) \[ body mass index (BMI) = body weight (kg) / height2 (m2)\].

Exclusion Criteria:

* 1. Participated in any drug test within 12 weeks prior to enrollment.
* 2. Drug abuse in the past 2 years or a history of substance 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.
* 4. Drug abuse urine test at screening is positive.

Other protocol-defined inclusion and exclusion criteria may apply.

Primary outcomes:
measure: Steady-state peak time (Tss_max)
timeFrame: Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
measure: Steady-state valley concentration(Css_min)
timeFrame: Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
measure: Steady-state peak concentration (Css_max)
timeFrame: Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
measure: Average steady-state plasma concentration (Css_av)
timeFrame: Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
measure: Half-life (t1/2, z)
timeFrame: Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
measure: Steady-state clearance (CLss/F)
timeFrame: Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
measure: Area under steady state plasma concentration-time curve (AUC)ss
timeFrame: Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
measure: Fluctuation index (DF)
timeFrame: Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
measure: Cumulative coefficient (RAUC, Rcmax)
timeFrame: Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
Secondary outcomes:
measure: The peak concentration (Cmax) after the first administration
timeFrame: Day1, Day2
measure: The peak time (Tmax) after the first administration
timeFrame: Day1, Day2
measure: Area under the plasma concentration-time curve (AUC0-24h)
timeFrame: Day1, Day2
measure: Valley concentration points
timeFrame: Day10, Day11, Day12, Day13, Day14
Other outcomes:
Locations:
city: Beijing
country: China
facility: Beijing Anding Hospital of Capital Medical University
state: Beijing
Study officials:
affiliation: Beijing Anding Hospital of Capital Medical University
name: Tao Jiang, Master
role: PRINCIPAL_INVESTIGATOR
References: