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CTRI Number  CTRI/2025/01/079051 [Registered on: 20/01/2025] Trial Registered Prospectively
Last Modified On: 17/01/2025
Post Graduate Thesis  No 
Type of Trial  BA/BE 
Type of Study    
Study Design  Single Arm Study 
Public Title of Study   The Pharmacokinetics, Safety and Tolerability study of Brexpiprazole 15.3 mg for extended-Release Injection in Subjects with Schizophrenia. 
Scientific Title of Study   An Open-Label, Multi-Center, Single-Arm, Single Dose Study to Evaluate the Pharmacokinetics, Safety and Tolerability of Brexpiprazole 15.3 mg for extended-Release Injection in Subjects with Schizophrenia. 
Trial Acronym  NIL 
Secondary IDs if Any  
Secondary ID  Identifier 
MW230026, Version 6.0 dated 02/Sep/2024  Protocol Number 
 
Details of Principal Investigator or overall Trial Coordinator (multi-center study)  
Name  Dr Sandeep Singh 
Designation  Vice President - Clinical Operations 
Affiliation  CBCC Global Research  
Address  TURQUOISE-IV 6th Floor, Sardar Patel Ring Rd, Opp. Apple Woods, Near Shantipura circle, Ahmedabad - 382210

Ahmadabad
GUJARAT
382210
India 
Phone  9637555304  
Fax    
Email  sandeep.singh@cbccusa.com  
 
Details of Contact Person
Scientific Query
 
Name  Dr Sandeep Singh 
Designation  Vice President - Clinical Operations 
Affiliation  CBCC Global Research  
Address  TURQUOISE-IV 6th Floor, Sardar Patel Ring Rd, Opp. Apple Woods, Near Shantipura circle, Ahmedabad - 382210

Ahmadabad
GUJARAT
382210
India 
Phone  9637555304  
Fax    
Email  sandeep.singh@cbccusa.com  
 
Details of Contact Person
Public Query
 
Name  Dr Sandeep Singh 
Designation  Vice President - Clinical Operations 
Affiliation  CBCC Global Research  
Address  TURQUOISE-IV 6th Floor, Sardar Patel Ring Rd, Opp. Apple Woods, Near Shantipura circle, Ahmedabad - 382210

Ahmadabad
GUJARAT
382210
India 
Phone  9637555304  
Fax    
Email  sandeep.singh@cbccusa.com  
 
Source of Monetary or Material Support  
Bostal Drug Delivery Co., Ltd. 6F, Building C1-C2, No. 11 Kaiyuan Road, Guangzhou Science Park, Guangzhou High-tech Industrial Development Zones, Guangzhou, Guangdong, China (510530)  
 
Primary Sponsor  
Name  Bostal Drug Delivery Co., Ltd. 
Address  6F, Building C1-C2, No. 11 Kaiyuan Road, Guangzhou Science Park, Guangzhou High-tech Industrial Development Zones, Guangzhou, Guangdong, China (510530)  
Type of Sponsor  Pharmaceutical industry-Global 
 
Details of Secondary Sponsor  
Name  Address 
CBCC Global Research  TURQUOISE-IV, 6th Floor, Sardar Patel Ring Rd, opp. Apple Woods, Near Shantipura circle, Ahmedabad, Gujarat – 382210, India 
 
Countries of Recruitment     India  
Sites of Study  
No of Sites = 1  
Name of Principal Investigator  Name of Site  Site Address  Phone/Fax/Email 
Dr Rajendra Anand  Anand Multispeciality Hospital and Research Centre  4th floor Sarthak mall, Mahatma mandir road, Sargasan cross road, Gandhinagar - 382421
Gandhinagar
GUJARAT 
9824017400

drrajendraanand@yahoo.com 
 
Details of Ethics Committee  
No of Ethics Committees= 1  
Name of Committee  Approval Status 
Anand Ethics Committee  Approved 
 
Regulatory Clearance Status from DCGI  
Status 
Approved/Obtained 
 
Health Condition / Problems Studied  
Health Type  Condition 
Patients  (1) ICD-10 Condition: F209||Schizophrenia, unspecified,  
 
Intervention / Comparator Agent  
Type  Name  Details 
Intervention  Brexpiprazole 15.3 mg for extended-Release Injection of Bostal Drug Delivery Co., Ltd.  Dosage: 15.3 mg, Route of Administration: Subcutaneous Injection, Duration of Therapy: Single, Frequency: Once a month.  
Comparator Agent  Rexulti® (Brexpiprazole 0.5 mg tablet) Otsuka Pharmaceutical Co. Ltd., Tokyo 101-8535, Japan  Dosage: 0.5 mg, Route of Administration: Oral, Duration of Therapy: 14 days, Frequency: Once in a day.  
 
Inclusion Criteria  
Age From  18.00 Year(s)
Age To  65.00 Year(s)
Gender  Both 
Details  1. Subjects and/or subjects 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.
2. Male or female subjects diagnosed with schizophrenia as per Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition, Text Revision (DSM-V-TR) (or later) criteria.
3. Subjects with a Clinical Global Impression-Severity of Illness (CGI-S) Score of less than or equal to 4 at screening.
4. Subjects with Positive and Negative syndrome-scale (PANSS) total score less than or equal to 75 at screening
5. Subjects aged 18-65 years (both inclusive) having Body Mass Index between 18.50 to 30.00 kg per m2
6. 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. NOTE: Subjects must NOT be taking greater than or equal to 2 antipsychotic medications for their disease.
7. Subjects who have tolerated oral Brexpiprazole prior to dosing.
8. Subjects with acceptable hematology status:
Hemoglobin greater than or equal to 9 g per dL
Absolute neutrophil count (ANC) greater than or equal to 1500 cells per micro L
Platelet count greater than or equal to 100,000 cells per micro L
White blood cell count (WBC) greater than or equal to 4000 cells per micro L
9. Subjects with acceptable liver function
Alanine aminotransferase (ALT) less than or equal to 2X upper limit of normal (ULN)
Aspartate aminotransferase (AST) less than or equal to 2X ULN
Bilirubin less than 1.2 mg per dL
Alkaline phosphatase less than or equal to 2X ULN
10. Subjects with creatinine clearance greater than or equal to 60 mL per minute (using the Cockcroft-Gault Equation).
11. Female subjects of child bearing potential with negative pregnancy test at screening and at enrollment day, and agree to practice acceptable methods of contraception during the study.
Acceptable methods of contraception are
Oral or other (eg. injection, patch or implant) hormonal contraception which has been used continuously for at least one month prior to the first dose of study medication
Intrauterine device or intrauterine system
Double barrier method of contraception (condom and occlusive cap or condom and spermicidal agent)
Female sterilization (surgical bilateral oophorectomy) or tubal ligation at least 6 weeks prior to study participation
12. Subjects who agree to avoid drinking alcohol during the study.


 
 
ExclusionCriteria 
Details  1. Subjects with known hypersensitivity to Brexpiprazole or related class of drugs or to any of the excipients of the formulation.
2. Subjects currently in acute, manic episodes of schizophrenia, as assessed by the Investigator.
3. Subjects with history of or a current DSM-V-TR diagnosis of concurrent mental disorder besides schizophrenia (eg. 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).
4. Subjects who have any suicidal ideation based on history, routine psychiatric status examination, investigators judgment, or who have an answer of "yes" on any of the questions of ‘Suicidal Ideation’ on the C-SSRS for screening.
5. Subjects with history or presence of neuroleptic malignant syndrome (NMS), tardive dyskinesia, Parkinsons disease, epilepsy or other seizure disorders, cognitive and motor impairment, pathological gambling, dysphagia or other compulsive behavior
6. Subjects with a prior personal or family history of dystonic reactions to medications.
7. Subjects with clinically significant dyslipidemia
8. 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 supine) at screening.
9. Subjects with known history or presence of any systemic disease (e.g., cardiovascular disease, cerebrovascular disease, diabetes mellitus, etc.)
10. Subject who are on concurrent treatment with other anti-psychotic Long-acting Injection (LAIs).
11. 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.
12. 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.
13. Any other condition(s) which could significantly interfere with protocol compliance
14. Subjects found positive for urine screen for drugs of abuse (except for benzodiazepine, which is a permissible medication if supported by prescription)
15. Subjects with major surgical procedure (including periodontal) within 28 days of IP dosing or plan to have major surgical procedure during the study
16. Subjects with current surgical or other non-healing wounds.
17. Subjects who have participated in any clinical trial with another investigational drug or other investigational intervention within 90 days of enrollment.
18. Loss of ≥ 350 mL (1 unit) of blood within 90 days before enrollment in the study.
19. Subjects with history of difficulty with donating blood or difficulty in accessibility of veins.
20. Subjects with seropositive results for Hepatitis B Virus (HBV), Hepatitis C Virus (HCV), or Human Immunodeficiency Virus (HIV)
21. Alcoholics (alcohol consumption of more than 14 units per week for men and more than 7 units per week for women, each unit equivalent to 360 mL of beer or 150 mL of wine or 45 mL of spirits with 40% alcohol content) or those who have a positive urine alcohol test
22. Subjects who have consumed tobacco-containing products (smoking, tobacco chewing, etc.), xanthine containing food, poppy seeds, and beverages (chocolates, tea, coffee, or cola drinks) or alcohol within 48.00 hours (02 days) prior to dosing or subject who is not ready to abstain from them till last study-related procedure.
23. Subjects who have consumed grapefruit or its juice and cranberry juice within 96.00 hours (04 days) prior to dosing or subject who is not ready to abstain from them till last study-related procedure.
24. Subjects currently smoking greater than or equal to 10 cigarettes or equivalent per day.
25. Pregnant or lactating women.

 
 
Method of Generating Random Sequence   Other 
Method of Concealment   Not Applicable 
Blinding/Masking   Open Label 
Primary Outcome  
Outcome  TimePoints 
To assess the Pharmacokinetics, Safety and Tolerability, of once-a-month ER injection of Brexpiprazole 15.3 mg, for subcutaneous use in subjects with schizophrenia.   0.00, 0.25, 0.50, 1.00, 2.00, 4.00, 8.00, 24.00, 72.00, 120.00, 192.00, 264.00, 336.00, 432.00, 504.00, 576.00, 672.00, 840.00, 1008.00, 1176.00, 1344.00, 1512.00, 1680.00, 1848.00, 2016.00, 2184.00, 2352.00, 2520.00 hrs.
 
 
Secondary Outcome  
Outcome  TimePoints 
To compare the PK profile of Brexpiprazole 15.3 mg for subcutaneous ER injection with steady state PK profile of Oral Brexpiprazole (Rexulti®, Otsuka) at a dose of 0.5 mg.   For oral Brexpiprazole: 0.00, 0.50, 1.00, 2.00, 3.00, 4.00, 6.00, 8.00, 12.00, 16.00, 24.00 hrs.
For subcutaneous Brexpiprazole 15.3 mg injection: 0.00, 0.25, 0.50, 1.00, 2.00, 4.00, 8.00, 24.00, 72.00, 120.00, 192.00, 264.00, 336.00, 432.00, 504.00, 576.00, 672.00, 840.00, 1008.00, 1176.00, 1344.00, 1512.00, 1680.00, 1848.00, 2016.00, 2184.00, 2352.00, 2520.00 hrs.
 
 
Target Sample Size   Total Sample Size="12"
Sample Size from India="12" 
Final Enrollment numbers achieved (Total)= "Applicable only for Completed/Terminated trials"
Final Enrollment numbers achieved (India)="Applicable only for Completed/Terminated trials" 
Phase of Trial   N/A 
Date of First Enrollment (India)   28/01/2025 
Date of Study Completion (India) Applicable only for Completed/Terminated trials 
Date of First Enrollment (Global)  Date Missing 
Date of Study Completion (Global) Applicable only for Completed/Terminated trials 
Estimated Duration of Trial   Years="0"
Months="9"
Days="0" 
Recruitment Status of Trial (Global)   Not Applicable 
Recruitment Status of Trial (India)  Open to Recruitment 
Publication Details   N/A 
Individual Participant Data (IPD) Sharing Statement

Will individual participant data (IPD) be shared publicly (including data dictionaries)?  

Response - NO
Brief Summary  

This is an open label Multi-Center, Single-Arm, Single Dose Study to Evaluate the Pharmacokinetics, Safety and Tolerability of Brexpiprazole 15.3 mg for extended-Release Injection in Subjects with Schizophrenia. It is planned to enroll 12 subjects with a confirmed diagnosis of schizophrenia. Each subject will undergo a screening period within 28 days before the Brexpiprazole tolerability assessment period. Eligible subject will enter tolerability period of 14 days and will receive 0.5 mg of oral Brexpiprazole formulation prior to dosing of Brexpiprazole 15.3 mg ER subcutaneous injection.       

 
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