A Study to Evaluate the Pharmacokinetics, Safety and Tolerability of Brexpiprazole for Extended-Release Injection in Subjects With Schizophrenia

NCT07742280 | Not Yet Recruiting Phase 2 FDA Drug

• 1 other identifier: MW250033
• Study Type: interventional
• Target: 16
• Locations: 0 countries
• Sites: N/A

Brief Summary

This study is to evaluate the pharmacokinetics (PK), safety and tolerability of Brexpiprazole, administered subcutaneously, in subjects with schizophrenia.

Conditions

Schizophrenia

Outcome Measures

Primary Outcomes (21)

• Cmax

  Maximum peak plasma concentration

  Pre-dose to 190 days post-dose

• Clast

  Last measurable plasma concentration

  Pre-dose to 190 days post-dose

• Tmax

  Time of occurence of Cmax

  Pre-dose to 190 days post-dose

• AUC0-last

  Area under curve from time zero to last measurable concentration

  Pre-dose to 190 days post-dose

• Kel

  Pre-dose to 190 days post-dose

• T1/2

  Half-life

  Pre-dose to 190 days post-dose

• Vd/F

  Volume of distribution

  Pre-dose to 190 days post-dose

• CL/F

  Apparent clearance of drug from plasma

  Pre-dose to 190 days post-dose

• MRT

  Mean residence time of the drug in the body

  Pre-dose to 190 days post-dose

• AUC_%Extrap_obs

  Percentage of AUC due to extrapolation from Tlast to infinity

  Pre-dose to 190 days post-dose

• AEs

  Adverse events

  Day 1 to Day 190

• SAEs

  Serious AEs

  Day 1 to Day 190

• Change from baseline in physical examination findings

  Change from baseline in clinical physical examination findings will be assessed descriptively for safety monitoring. The assessment includes general appearance, skin, head, ears, eyes, nose and throat, chest and lungs, cardiovascular, abdomen, musculoskeletal and extremities, neurological, psychiatric, and mental status examinations. Individual findings will be evaluated for clinically meaningful changes from baseline.

  Day 1 to Day 190

• Blood Pressure

  Evaluate the clinical significance of test value outside of the reference range.

  Day 1 to Day 190

• Orthostatic hypotension

  Drop in blood pressure due to a change in body position from standing to supine

  Day 1 to Day 190

• Columbia-Suicide Severity Rating Scale (C-SSRS) assessment

  Change in suicidality from baseline.

  Day 1 to Day 190

• Clinical Laboratory Tests

  Evaluate the clinical significance of each test value outside of the reference range. Lab tests including blood test for Human immunodeficiency virus (HIV), Hepatitis B virus (HBsAg and HBcAb) and Hepatitis C virus (HCV), haematology (Total WBC count, total RBC count, hemoglobin, HCT (PCV), lymphocytes, monocytes, granulocytes, platelet count, and ANC), biochemistry (Fasting blood glucose, BUN, serum creatinine, creatinine clearance, total bilirubin, SGPT, SGOT, ALP, serum cholesterol, sodium, calcium, potassium, chloride, magnesium, LDL, HDL and TG), serum pregnancy test (only for females of childbearing potential) and urine test

  Day 1 to Day 190

• 12-lead ECG Assessment

  For safety assessment. ECG findings will be evaluated descriptively based on the overall interpretation (Normal, Abnormal Not Clinically Significant \[NCS\], or Abnormal Clinically Significant \[CS\]).

  Day 1 to Day 190

• Pulse Rate

  Evaluate the clinical significance of test value outside of the reference range.

  Day 1 to Day 190

• Respiratory Rate

  Evaluate the clinical significance of test value outside of the reference range.

  Day 1 to Day 190

• Body Temperature

  Evaluate the clinical significance of test value outside of the reference range.

  Day 1 to Day 190

Study Arms (2)

Brexpiprazole for ER injection, 45 mg

EXPERIMENTAL

Drug: Brexpiprazole for ER injection, 45 mg

Brexpiprazole for ER injection, 100 mg

EXPERIMENTAL

Drug: Brexpiprazole for ER injection, 100 mg

Interventions

Brexpiprazole for ER injection, 45 mg DRUG

Single-dose, Subcutaneous

Brexpiprazole for ER injection, 45 mg

Brexpiprazole for ER injection, 100 mg DRUG

Single-dose, Subcutaneous

Brexpiprazole for ER injection, 100 mg

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Subjects and/or subject's legally acceptable representative (LAR) is able to sign informed consent and subject is willing to comply with the trial protocol and to attend the clinic visits.
• Male or female subjects diagnosed with schizophrenia as per Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition, Text Revision (DSM-5-TR) (or later) criteria.
• Subjects with a Clinical Global Impression-Severity of Illness (CGI-S) Score of ≤ 4 at screening and on enrolment prior to IP dosing (Day -1).
• Subjects with Positive and Negative syndrome-scale (PANSS) total score ≤75 at screening and on enrolment prior to IP dosing (Day -1).
• Subjects aged 18-65 years (both inclusive) having Body Mass Index (BMI) between 18.50 to 30.00 kg/m2
• Schizophrenic subjects who are clinically stable on their current antipsychotic medication other than Brexpiprazole, for a duration of at least 8 weeks prior to screening. \[Refer to Appendix A for List of Allowable medications\] NOTE: Subjects must NOT be taking \> 2 antipsychotic medications for their disease
• Subjects who have tolerated oral Brexpiprazole prior to dosing.
• Subjects with acceptable haematology status:
• Hemoglobin ≥ 9 g/dL
• Absolute neutrophil count (ANC) ≥ 1500 cells/μL
• Platelet count ≥ 100,000 cells/μL
• White blood cell count (WBC) ≥ 4000 cells/μL
• Subjects with acceptable liver function:
• Alanine aminotransferase (ALT) ≤ 2 X upper limit of normal (ULN)
• Aspartate aminotransferase (AST) ≤ 2 X ULN

You may not qualify if:

• Subjects with known hypersensitivity to Brexpiprazole or related class of drugs or to any of the excipients of the formulation.
• Subjects currently in acute, manic episodes of schizophrenia, as assessed by the Investigator.
• Subjects with history of or a current DSM-5-TR diagnosis of concurrent mental disorder besides schizophrenia (e.g., schizoaffective-disorder, major depressive disorder, bipolar I disorder, bipolar II disorder, general anxiety disorder, obsessive-compulsive disorder, post-traumatic stress disorder, dementia or mild neurocognitive disorder, and personality disorder).
• Subjects who have any suicidal ideation based on history, routine psychiatric status examination, investigator's judgment, or who have an answer of "yes" on any of the questions of 'Suicidal Ideation' on the CSSRS for screening. \[Refer to Appendix B\]
• Subjects with history or presence of neuroleptic malignant syndrome (NMS), tardive dyskinesia, Parkinson's disease, epilepsy or other seizure disorders, cognitive and motor impairment, pathological gambling, dysphagia or other compulsive behaviour
• Subjects with a prior personal or family history of dystonic reactions to medications.
• Subjects with clinically significant dyslipidemia.
• Subjects with a history of syncope or a presence of significant orthostatic hypotension (i.e., a drop in systolic blood pressure of 20 mm Hg or more and/or a drop in diastolic blood pressure of 10 mm Hg or more within 3 minutes of standing from a minimum of 5 minutes in supine position) at screening.
• Subjects with known history or presence of any systemic disease (e.g., cardiovascular disease, cerebrovascular disease, diabetes mellitus, etc.)
• Subject who are on concurrent treatment with other anti-psychotic Longacting Injection (LAIs).
• Subject who has received concomitant medications that are strong CYP3A4 inhibitors, CYP2D6 inhibitors, or CYP3A4 inducers within 14 days prior to study drug administration (or within five half-lives since the last drug administration, whichever is greater), or is expected to require such treatment during the study.
• Subjects with any other medical condition or serious inter-current illness that, in the opinion of the Investigator, may make it undesirable for the subject to participate in the study including but not limited to cirrhosis or psychiatric illness other than schizophrenia /social situations that would limit adherence to study requirements.
• Any other condition(s) which could significantly interfere with protocol compliance
• Subjects found positive for urine screen for drugs of abuse (except for benzodiazepine, which is a permissible medication if supported by prescription)
• Subjects with major surgical procedure (including periodontal) within 28 days of IP dosing or plan to have major surgical procedure during the study

Sponsors & Collaborators

• Bostal Drug Delivery Co., Ltd: lead

MeSH Terms

Conditions

Schizophrenia

Interventions

brexpiprazole

Condition Hierarchy (Ancestors)

Schizophrenia Spectrum and Other Psychotic Disorders; Mental Disorders

Study Design

• Study Type: interventional
• Phase: phase 2
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 15, 2026
• First Posted: August 3, 2026
• Study Start: August 1, 2026
• Primary Completion (Estimated): August 1, 2027
• Study Completion (Estimated): December 1, 2027
• Last Updated: August 3, 2026

Record last verified: 2026-07