Bioequivalence Study of Long-Acting Paliperidone Palmitate in Patients With Schizophrenia

NCT07268430 | Completed

• 1 other identifier: SYHF2036-001
• Study Type: interventional
• Target: 256
• Locations: 1 country
• Sites: 1

Brief Summary

This multicenter, randomized, open-label, parallel-group, multiple-dose study is designed to evaluate the bioequivalence, at pharmacokinetic steady state, of a paliperidone palmitate injection manufactured by CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co., Ltd. (Test Group) and a paliperidone palmitate injection manufactured by Janssen Pharmaceutica N.V. (Reference Group) in patients with schizophrenia in China. Bioequivalence will be assessed based on steady-state pharmacokinetic parameters after repeated intramuscular administration (e.g., Cmax,ss and AUCτ). The safety and tolerability of the test and reference products will also be evaluated.

Conditions

Schizophrenia

Outcome Measures

Primary Outcomes (2)

• Title:Steady-State Peak Concentration (Cmax,ss) of Paliperidone After Intramuscular Administration.

  Steady-state maximum plasma concentration (Cmax,ss) will be determined to assess bioequivalence between the test and reference formulations of paliperidone palmitate injection after multiple intramuscular doses in patients with schizophrenia.

  Day148~Day176

• Area Under the Concentration-Time Curve over Dosing Interval (AUCτ,ss) of Paliperidone After Intramuscular Administration.

  Area under the plasma concentration-time curve during the dosing interval (AUCτ,ss) will be determined to assess bioequivalence between the test and reference formulations of paliperidone palmitate injection after multiple intramuscular doses in patients with schizophrenia.

  Day148~Day176

Secondary Outcomes (12)

• Steady-State Trough Concentration (Ctau,ss)

  Day1~Day176

• Steady-State Average Concentration (Cav,ss)

  Day1~Day176

• Steady-State Minimum Concentration (Cmin,ss)

  Day1~Day176

• Time to Maximum Concentration at Steady State (Tmax,ss)

  Day1~Day176

• Degree of Fluctuation (DF) and Swing at Steady State

  Day1~Day176

Study Arms (2)

Paliperidone Palmitate 1-Month Formulation (PP1M) (Test Group)

EXPERIMENTAL

Participants will receive paliperidone palmitate injection manufactured by CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co., Ltd., administered intramuscularly. Dosing regimen: 150 mg on Day 1 and 100 mg on Day 8, followed by 100 mg every 28 days (starting Day 1 regimen); or 100 mg every 28 days (starting Day 36 regimen).

Drug: Paliperidone Palmitate Injection(PP1M); Drug: Paliperidone Palmitate Injection(PP1M)(Reference Group)

Paliperidone Palmitate 1-Month Formulation (PP1M) (Reference Group)

ACTIVE COMPARATOR

Participants will receive paliperidone palmitate injection (Invega Sustenna®) manufactured by Janssen Pharmaceutica N.V., administered intramuscularly. Dosing regimen: 150 mg on Day 1 and 100 mg on Day 8, followed by 100 mg every 28 days (starting Day 1 regimen); or 100 mg every 28 days (starting Day 36 regimen).

Drug: Paliperidone Palmitate Injection(PP1M); Drug: Paliperidone Palmitate Injection(PP1M)(Reference Group)

Interventions

Paliperidone Palmitate Injection(PP1M) DRUG

Paliperidone palmitate injection will be administered intramuscularly according to two dosing regimens based on participants' prior exposure to paliperidone palmitate: 1. Participants with no prior use of paliperidone palmitate injection, or whose last dose was administered more than 6 months ago (for the once-monthly formulation), or more than 5 half-lives ago (for the once-every-3-months formulation): Day 1: 150 mg, deltoid muscle Day 8: 100 mg, deltoid muscle Followed by 100 mg every 28 days thereafter Approximate treatment duration: 148 days 2. Participants who have previously received at least 3 injections (including 150 mg Day 1 loading dose and 100 mg Day 8 loading dose, deltoid muscle) of the once-monthly formulation (100 mg) of paliperidone palmitate and whose last dose was given within 4 to 6 weeks prior to enrollment: Continue with 100 mg every 28 days Approximate treatment duration: 113 days

Also known as: SYHF2036

Paliperidone Palmitate 1-Month Formulation (PP1M) (Reference Group); Paliperidone Palmitate 1-Month Formulation (PP1M) (Test Group)

Paliperidone Palmitate Injection(PP1M)(Reference Group) DRUG

Paliperidone palmitate injection will be administered intramuscularly according to two dosing regimens based on participants' prior exposure to paliperidone palmitate: 1. Participants with no prior use of paliperidone palmitate injection, or whose last dose was administered more than 6 months ago (for the once-monthly formulation), or more than 5 half-lives ago (for the once-every-3-months formulation): Day 1: 150 mg, deltoid muscle Day 8: 100 mg, deltoid muscle Followed by 100 mg every 28 days thereafter Approximate treatment duration: 148 days 2. Participants who have previously received at least 3 injections (including 150 mg Day 1 loading dose and 100 mg Day 8 loading dose, deltoid muscle) of the once-monthly formulation (100 mg) of paliperidone palmitate and whose last dose was given within 4 to 6 weeks prior to enrollment: Continue with 100 mg every 28 days Approximate treatment duration: 113 days

Also known as: Invega Sustenna

Paliperidone Palmitate 1-Month Formulation (PP1M) (Reference Group); Paliperidone Palmitate 1-Month Formulation (PP1M) (Test Group)

Eligibility Criteria

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

You may qualify if:

• Age 18 to 65 years inclusive at the time of consent.
• Diagnosis of schizophrenia (ICD-10 criteria) prior to screening.
• PANSS total score ≤70 at screening and at baseline.
• CGI-S score ≤4 at screening and at baseline.
• Body weight at screening: ≥50.0 kg (male) or ≥45.0 kg (female); body mass index (BMI) 19.0 to 35.0 kg/m2 (inclusive).
• The participant and/or partner have no plans for pregnancy during the study and for 6 months after the last dose, and agree to use effective contraception (oral contraceptives are not allowed).
• Signed informed consent and willingness and ability to comply with all study requirements.

You may not qualify if:

• Known or suspected hypersensitivity to the study drug (paliperidone palmitate) or any of its components.
• Diagnosis per ICD-10 or DSM-5 of any psychiatric disorder other than schizophrenia.
• Clinically significant diseases or abnormalities, as judged by the investigator, in the respiratory, cardiovascular, gastrointestinal, genitourinary, reproductive, nervous, endocrine, or immune systems that may affect participant safety or interfere with study participation.
• Laboratory abnormalities at screening or baseline meeting any of the following: (1) total bilirubin \>1.5 × ULN, or AST or ALT \>2 × ULN; (2) creatinine clearance (CLcr) \<90 mL/min; (3) white blood cell count \<3 × 10\^9/L, or absolute neutrophil count \<1.5 × 10\^9/L, or platelets \<80 × 10\^9/L.
• History of orthostatic hypotension or syncope due to orthostatic hypotension (except if stable for \>6 months); or at screening/baseline, a decrease in systolic blood pressure ≥20 mmHg or diastolic blood pressure ≥10 mmHg within 3 minutes after changing from supine to standing.
• Congenital long QT syndrome; uncontrolled or significant cardiovascular disease, including congestive heart failure of NYHA class II or higher, unstable angina, or myocardial infarction within 6 months prior to first study dose; significant arrhythmias (including frequent premature ventricular contractions), or clinically significant arrhythmias requiring treatment at screening; QTc \>450 ms (male) or \>460 ms (female) at screening or baseline; risk factors for torsades de pointes or sudden death (e.g., bradycardia, clinically significant hypokalemia or hypomagnesemia, current use of medications that prolong QTc); or other clinically significant ECG abnormalities as judged by the investigator.
• Past or current neuroleptic malignant syndrome.
• Parkinson's disease, Lewy body dementia, or dementia-related psychosis.
• Past or current seizure or convulsive disorders (except childhood febrile seizures), or stroke or transient ischemic attack within 1 year prior to consent.
• History of tardive dyskinesia induced by risperidone, paliperidone, or other antipsychotics.
• Uncontrolled diabetes mellitus, or HbA1c ≥7% at screening or baseline.
• Electroconvulsive therapy within 28 days prior to consent.
• Blood loss ≥400 mL within 3 months prior to consent, or ≥200 mL within 1 month prior to consent due to donation, surgery, or other causes.
• Esophageal motility disorders, dysphagia, or other conditions that confer risk of aspiration pneumonia.
• Positive tests for hepatitis B surface antigen, hepatitis C antibody, HIV antibody, or treponemal (syphilis) antibody.

Sponsors & Collaborators

• CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co., Ltd.: lead

Study Sites (1)

Beijing Anding Hospital Capital Medical University

Beijing, Beijing Municipality, China

Location

MeSH Terms

Conditions

Schizophrenia

Interventions

Paliperidone Palmitate

Condition Hierarchy (Ancestors)

Schizophrenia Spectrum and Other Psychotic Disorders; Mental Disorders

Intervention Hierarchy (Ancestors)

Isoxazoles; Azoles; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Pyrimidines

Study Officials

• Gang Wang, M.D.

  Beijing Anding Hospital Capital Medical University

  STUDY CHAIR

Study Design

• Study Type: interventional
• Phase: not applicable
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: September 30, 2025
• First Posted: December 5, 2025
• Study Start: December 18, 2023
• Primary Completion: December 25, 2024
• Study Completion: December 25, 2024
• Last Updated: December 5, 2025

Record last verified: 2025-09

Locations

CN (1)