The Purpose of This Study is to Determine the Safety, Tolerability, and Pharmacokinetics of Brexpiprazole Long-acting Injection Following a Single Administration in Healthy Subjects/Patients With Schizophrenia.

NCT06674694 | Recruiting Phase 1

• 1 other identifier: KL414-3-Ⅰ-01-CTP
• Study Type: interventional
• Target: 56
• Locations: 1 country
• Sites: 1

Brief Summary

Study to evaluate the safety and tolerability of single ascending doses of brexpiprazole long-acting injection in healthy subjects/patients with schizophrenia.

Conditions

Schizophrenia Disorders

Outcome Measures

Primary Outcomes (8)

• Number of reported Adverse Events (AE)

  Safety and tolerability was assessed by the number of participants with adverse events (AE).

  Collected from signing of informed consent until 90 days after a single dose.

• Clinical Laboratory Tests

  Hematology, Serum chemistry, Lipid Panel, Glycated Hemoglobin, Urinalysis, Coagulation Panel will be performed.

  Collected from signing of informed consent until 90 days after a single dose.

• Change in physical exam results

  Investigator will perform complete physical exam and document any clinically significant conditions. Body height and weight will also be measured for BMI calculation and weight will be measured as part of all subsequent physical exams.

  Collected from signing of informed consent until 90 days after a single dose.

• Vital signs

  Vital signs include respiration, temperature, pulse, and blood pressure.

  Collected from signing of informed consent until 90 days after a single dose.

• ECG Reading

  12-lead ECG include heart rate, ventricular rate, RR interval, PR interval, QRS duration and QT intervals will be recorded.

  Collected from signing of informed consent until 90 days after a single dose.

• Extrapyramidal Symptoms (EPS) Rating Scale

  SAS, AIMS , BARS will be assess by trained trial center staff \[Only patients with schizophrenia\].

  Collected from signing of informed consent until 90 days after a single dose.

• Change in Suicidality via Columbia-Suicide Severity Rating Scale

  Baseline version and Since Last Visit version of CSSRS will be completed by trained trial center staff \[Only patients with schizophrenia\].

  Collected from signing of informed consent until 90 days after a single dose.

• Injection site assessment

  Injection site will be assessed by Investigator.Which includes pain, swelling, redness, induration, etc.

  Collected from signing of informed consent until 90 days after a single dose.

Secondary Outcomes (5)

• Maximum peak plasma concentration (Cmax) [Pharmacokinetics]

  90 days after a single dose.

• Time of Cmax (tmax) [Pharmacokinetics]

  90 days after a single dose.

• Area under the concentration-time curve (AUC) from time zero to time "t" [Pharmacokinetics]

  90 days after a single dose.

• AUC from time zero to infinity (AUC∞) [Pharmacokinetics]

  90 days after a single dose.

• Terminal-phase elimination half-life (t1/2,z) [Pharmacokinetics]

  90 days after a single dose.

Study Arms (6)

20mg dosing group

EXPERIMENTAL

The starting dose is 20 mg and the obtained research results will determine the adjustment of dosage in subsequent study groups.

Drug: Brexpiprazole long-acting injection

40mg dosing group

EXPERIMENTAL

The starting dose is 20 mg and the obtained research results will determine the adjustment of dosage in subsequent study groups.

Drug: Brexpiprazole long-acting injection

80mg dosing group

EXPERIMENTAL

The starting dose is 20 mg and the obtained research results will determine the adjustment of dosage in subsequent study groups.

Drug: Brexpiprazole long-acting injection

160mg dosing group

EXPERIMENTAL

The starting dose is 20 mg and the obtained research results will determine the adjustment of dosage in subsequent study groups.

Drug: Brexpiprazole long-acting injection

240mg dosing group

EXPERIMENTAL

The starting dose is 20 mg and the obtained research results will determine the adjustment of dosage in subsequent study groups.

Drug: Brexpiprazole long-acting injection

320mg dosing group

EXPERIMENTAL

The starting dose is 20 mg and the obtained research results will determine the adjustment of dosage in subsequent study groups.

Drug: Brexpiprazole long-acting injection

Interventions

Brexpiprazole long-acting injection DRUG

A single injection was administered.

160mg dosing group; 20mg dosing group; 240mg dosing group; 320mg dosing group; 40mg dosing group; 80mg dosing group

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy Volunteers:
• Male and female subjects aged 18 to 65 years (including) at the time of signing the informed consent (the number of single sex in each group is not less than 1/4);
• Body mass index (BMI) in the range of 19.0-26.0 (including the critical value), and female weight ≥ 45 kg, male weight ≥ 50 kg;
• Subjects of childbearing potential (including partners) have no pregnancy plan or sperm donation and egg donation plan since signing the informed consent form to within 1 year after the last dose of the investigational drug, and voluntarily take effective contraceptive measures;
• Sign informed consent before the trial, and fully understand the trial content, process and possible adverse reactions;
• Subjects can communicate well with the investigator, and understand and comply with the requirements of this study.
• Patients with schizophrenia:
• Male and female subjects aged 18 to 65 years (including) at the time of signing the informed consent (the number of single sex in each group is not less than 1/4);
• Patients diagnosed with schizophrenia according to ICD-10, and the positive and negative symptom scale (PANSS) score ≤ 70 points, and the investigator judged stable disease within 4 weeks before screening;
• Body mass index (BMI) ≥ 18.5 kg/m2 and \< 35.0 kg/m2, and female weight ≥ 45 kg, male weight ≥ 50 kg;
• Subjects need to complete the tolerance test according to the protocol requirements;
• Subjects of childbearing potential (including partners) have no pregnancy plan or sperm donation and egg donation plan since signing the informed consent form to within 1 year after the last dose of the investigational drug, and voluntarily take effective contraceptive measures;
• Subjects and their guardians signed informed consent;
• Subjects and their guardians agree to comply with the protocol and cooperate with the investigator to complete the trial.

You may not qualify if:

• Healthy Volunteers:
• History of cardiovascular system (such as history of ischemic heart disease), endocrine system, urinary system, nervous system, hematology, immunology (including personal or family history of hereditary immunodeficiency), metabolic abnormalities, and the researchers believe that there is still clinical significance;
• Physical examination, vital signs, 12-lead electrocardiogram, clinical laboratory tests (including hematology, urinalysis, serum biochemistry, thyroid panel, coagulation panel, serum prolactin, virological examination, lipid panel, serum pregnancy test (only women of childbearing age) and glycosylated hemoglobin, etc.), chest X-ray or CT and B-ultrasound with Injection site results in injection site are abnormal and clinically significant;;
• Those who have taken any brexpiprazole preparation within 28 days prior to oral tolerance test drugs (brexpiprazole tablets);
• Those who have been enrolled in clinical trials of brepiprazole long-acting injection and have received the test drug administration;
• Participate in any drug or medical device clinical trial and receive the treatment of the investigational drug or medical device within 28 days before dosing (other than the drug/equipment used in this study), except for subjects participating in the research or observational study;
• Those who have used any drugs that interact with brepiprazole within 30 days before administration \[including CYP3A4 inducers and inhibitors, CYP2D6 inducers and inhibitors\] (except topical preparations with local effects);
• Those who have used any drugs within 14 days before administration \[including prescription drugs, over-the-counter drugs, traditional Chinese medicine, etc.\] (except topical preparations with local effects);
• Consumption of foods or beverages rich in xanthine (such as sardines, animal liver, etc.), grapefruit (such as grapefruit, western grapefruit, lime, carambola, etc.), caffeine (such as coffee, strong tea, cola, milk tea, etc.) within 48 hours before dosing, or other special diet that can affect drug absorption, distribution, metabolism and excretion;
• Those who drink excessive amounts (more than 8 cups, 1 cup = 250 mL) of tea or coffee or beverages rich in xanthine/caffeine/grapefruit (such as milk tea, cola, fruit juice, etc.) before administration;
• Previous alcohol abuse (i.e., men drink more than 28 standard units per week, women drink more than 21 standard units per week (1 standard unit contains 14 g alcohol, such as 360 mL beer or 45 mL spirits with 40% alcohol or 150 mL wine), or frequent alcohol consumption within the first 6 months before screening (more than 14 standard units per week) and determined by the investigator to affect the test, or unwilling to stop drinking or any alcohol-containing products from the date of screening to the last PK blood collection period;
• Those who smoke more than 3 cigarettes per day within 3 months before dosing, or are unwilling to stop using any tobacco products from the date of screening to the last PK blood collection in the trial;
• Those with a history of drug dependence or a history of drug abuse;
• Positive urine drug abuse screening;
• Alcohol breath test positive;

Sponsors & Collaborators

• Sichuan Kelun Pharmaceutical Research Institute Co., Ltd.: lead

Study Sites (1)

Beijing Anding Hospital Capital Medical University

Beijing, Beijing Municipality, 100000, China

RECRUITING

MeSH Terms

Conditions

Schizophrenia

Condition Hierarchy (Ancestors)

Schizophrenia Spectrum and Other Psychotic Disorders; Mental Disorders

Central Study Contacts

Wei Qi

CONTACT

028-82339360; qiw@kelun.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 26, 2024
• First Posted: November 5, 2024
• Study Start: April 10, 2024
• Primary Completion (Estimated): June 30, 2026
• Study Completion (Estimated): October 30, 2026
• Last Updated: November 17, 2025

Record last verified: 2025-11

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)