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

A Single-center, Open-label Study Evaluating the Pharmacokinetics, and Safety of Multiple Dose Oral Brexpiprazole Tablets (1 mg) in Chinese Healthy Subjects

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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Brexpiprazole

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.

• Study Type: Interventional
• Enrollment (Actual): 10
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Beijing
    • Beijing, Beijing, China, 100088
      • Beijing Anding Hospital of Capital Medical University

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

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.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Multiple dose oral administration; 1mg Once Daily (QD) , oral administration,14 consecutive days	Drug: Brexpiprazole; Brexpiprazole , mutiple dose /oral/empty stomach; Other Names: Brex

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Steady-state peak time (Tss_max)	Assessment of the steady-state peak time of Brexpiprazole	Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
Steady-state valley concentration(Css_min)	Assessment of the steady-state valley concentration of Brexpiprazole	Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
Steady-state peak concentration (Css_max)	Assessment of the steady-state peak concentration of Brexpiprazole	Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
Average steady-state plasma concentration (Css_av)	Assessment of the average steady-state plasma concentration (Css_av) of Brexpiprazole	Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
Half-life (t1/2, z)	Assessment of the Half-life of Brexpiprazole	Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
Steady-state clearance (CLss/F)	Assessment of the steady-state clearance of Brexpiprazole	Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
Area under steady state plasma concentration-time curve (AUC)ss	Assessment of the area under steady state plasma concentration-time curve of Brexpiprazole	Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
Fluctuation index (DF)	Assessment of the fluctuation index of Brexpiprazole	Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25
Cumulative coefficient (RAUC, Rcmax)	Assessment of the cumulative coefficient of Brexpiprazole	Day1, Day2, Day10, Day11, Day12, Day13, Day14, Day15, Day16, Dv17, Day18, Day19, Dv21,Day23, Day25

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
The peak concentration (Cmax) after the first administration	The peak concentration (Cmax) of Brexipiprazole and the metabolite DM-3411 on the first day after administration are calculated.	Day1, Day2
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.	Day1, Day2
Area under the plasma concentration-time curve (AUC0-24h)	The area under the plasma concentration-time curve of Brexipiprazole and the metabolite DM-3411 on the first day after administration are calculated.	Day1, Day2
Valley concentration points	Descriptive statistics about the valley concentration points before taking the study drug on days 10, 11, 12, 13 and 14	Day10, Day11, Day12, Day13, Day14

Collaborators and Investigators

• Sponsor: Otsuka Beijing Research Institute
• Investigators: Principal Investigator: Tao Jiang, Master, Beijing Anding Hospital of Capital Medical University

Study record dates

Study Major Dates

• Study Start (Actual): April 24, 2019
• Primary Completion (Actual): June 10, 2020
• Study Completion (Actual): June 10, 2020

Study Registration Dates

• First Submitted: November 2, 2018
• First Submitted That Met QC Criteria: November 6, 2018
• First Posted (Actual): November 7, 2018

Study Record Updates

• Last Update Posted (Actual): November 1, 2023
• Last Update Submitted That Met QC Criteria: October 30, 2023
• Last Verified: January 1, 2020

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Serotonin Agents; Dopamine Agonists; Dopamine Agents; Brexpiprazole
• Other Study ID Numbers: 331-403-00025

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No