Clinical trial NCT03734354: The Pharmacokinetics, Tolerability and Safety of Brexpiprazole in Healthy Chinese Subjects
Official title: A Single-center, Open-label Study Evaluating the Pharmacokinetics, Tolerability and Safety of Single Dose Oral Brexpiprazole Tablets in Healthy Chinese Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Health
Lead sponsor: Otsuka Beijing Research Institute
Sponsor class: INDUSTRY
First posted: 2018-11-07
Enrollment: 30
Sex: ALL
Minimum age (years): 18
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: OTHER

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.

Eligibility criteria: 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

Primary outcomes:
measure: The peak concentration (Cmax) after the first administration
timeFrame: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
measure: The peak time (Tmax) after the first administration
timeFrame: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
measure: Area under the plasma concentration-time curve (AUC0-264h)
timeFrame: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
measure: Half time after the first administration
timeFrame: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
measure: Apparent clearance after the first administration
timeFrame: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
measure: Proportional dose-response relationship between pharmacokinetic parameters Cmax and AUC of OPC-34712
timeFrame: 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
Secondary outcomes:
measure: Blood pressure
timeFrame: 0, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
measure: Heart rate
timeFrame: 0, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
measure: Body weight
timeFrame: 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
measure: 12-lead ECG
timeFrame: 3, 6, 24, 72, 96, 120, 264 hours
measure: Blood biochemistry
timeFrame: 24, 96, 264 hours
measure: Blood routine
timeFrame: 24, 96, 264 hours
measure: urinary routine
timeFrame: 24, 96, 264 hours
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: