The Pharmacokinetics, Tolerability and Safety of Brexpiprazole in Healthy Chinese Subjects

Health Clinical Trial

Official title:

A Single-center, Open-label Study Evaluating the Pharmacokinetics, Tolerability and Safety of Single Dose Oral Brexpiprazole Tablets in Healthy Chinese Subjects

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT03734354
• Other study ID #: 331-403-00024
• Status: Completed
• Phase: Phase 1
• Start date: April 7, 2019
• Est. completion date: May 18, 2020

Study information

• Verified date: July 2020
• Source: Otsuka Beijing Research Institute
• Contact: n/a
• Is FDA regulated: No
• Study type: Interventional

Clinical Trial 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.

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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 30
• Est. completion date: May 18, 2020
• Est. primary completion date: May 18, 2020
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: All
• Age group: 18 Years to 45 Years

Eligibility

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

Related Conditions & MeSH terms

• Health

Intervention

Drug:
• Brexpiprazole
Brexpiprazole , single/oral/with fasting

Locations

Country	Name	City	State
China	Beijing Anding Hospital of Capital Medical University	Beijing	Beijing

Sponsors (1)

Lead Sponsor	Collaborator
Otsuka Beijing Research Institute

Country where clinical trial is conducted

China, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	The peak concentration (Cmax) after the first administration	The peak concentration (Cmax) of Brexipiprazole and the metabolite DM-3411 after administration	0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
Primary	The peak time (Tmax) after the first administration	The peak-time of Brexipiprazole and the metabolite DM-3411 on the first day after administration are calculated.	0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
Primary	Area under the plasma concentration-time curve (AUC0-264h)	The area under the plasma concentration-time curve of Brexipiprazole after administration are calculated.	0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
Primary	Half time after the first administration	The half time of Brexipiprazole after administration are calculated.	0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
Primary	Apparent clearance after the first administration	To assess the apparent clearance after administration (CL/F) of Brexipiprazole after the first administration	0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
Primary	Proportional dose-response relationship between pharmacokinetic parameters Cmax and AUC of OPC-34712	To assess the 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
Secondary	Blood pressure	To seeess blood pressure after administration of brexpiprazole	0, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
Secondary	Heart rate	To seeess heart rate after administration of brexpiprazole	0, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
Secondary	Body weight	To seeess Body weight after administration of brexpiprazole	1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 hours
Secondary	12-lead ECG	To seeess 12-lead ECG after administration of brexpiprazole	3, 6, 24, 72, 96, 120, 264 hours
Secondary	Blood biochemistry	To seeess blood biochemistry after administration of brexpiprazole	24, 96, 264 hours
Secondary	Blood routine	To seeess blood routine after administration of brexpiprazole	24, 96, 264 hours
Secondary	urinary routine	To seeess urinary routine after administration of brexpiprazole	24, 96, 264 hours