Antipsychotic Agents, Central Nervous System Depression, Mental Disorders, Molecular Mechanisms of Pharmacological Action, Mood Disorders, Neurotransmitter Agents, Physiological Effects of Drugs, Psychotic Disorders, Psychotropic Drugs, Schizophrenia, Schizophrenia Spectrum and Other Psychotic Disorders, Tranquilizing Agents
Conditions
Keywords
Schizophrenia, Paliperidone Palmitate, Serotonin 5-HT2 Receptor Antagonists, Serotonin Antagonists, Serotonin Agents, Dopamine D2 Receptor Antagonists, Dopamine Antagonists, Dopamine Agents
Brief summary
This is a randomized, single-dose, open-label, parallel-group study. Patients will undergo the screening evaluations to determine eligibility within 28 days prior to study drug administration. Approximately 80 eligible patients will be randomized in a 1:1:1:1 ratio to 1 of 4 treatment groups.
Detailed description
This is a randomized, single-dose, open-label, parallel-group study. Patients will undergo the screening evaluations to determine eligibility within 28 days prior to study drug administration. Approximately 80 eligible patients will be randomized in a 1:1:1:1 ratio to 1 of 4 treatment groups. Patients will be admitted to the clinical facilities the day (Day 0) before dosing, and will be randomized and receive a single dose on Day 1. Patients will be discharged on Day 2 after PK collection. All patients will return to the clinical site at designated study days for PK sample collections and assigned clinical procedures (Table 1). End of study evaluation will be completed on Day 176 or at early withdrawal. For patients who have never taken paliperidone or risperidone, tolerability will be tested with oral risperidone (1 mg risperidone taken orally for 3 consecutive days) at Screening approximately 14 days but no less than 9 days prior to dosing.
Interventions
DRUGLY03010 156 mg treatment group, deltoid
LY03010 is white to off-white sterile aqueous extended-release suspension of paliperidone palmitate for IM injection.
DRUGLY03010 156 mg treatment group, gluteal
LY03010 is white to off-white sterile aqueous extended-release suspension of paliperidone palmitate for IM injection.
DRUGLY03010 351 mg treatment group, deltoid
LY03010 is white to off-white sterile aqueous extended-release suspension of paliperidone palmitate for IM injection.
DRUGLY03010 351 mg treatment group, gluteal
LY03010 is white to off-white sterile aqueous extended-release suspension of paliperidone palmitate for IM injection.
Sponsors
Luye Pharma Group Ltd.
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
NONE
Intervention model description
Approximately 80 eligible patients will be randomized in a 1:1:1:1 ratio to 1 of 4 treatment groups as shown below. Treatment Group Treatment (LY03010) Injection Site 1. 156 mg Deltoid 2. 156 mg Gluteal 3. 351 mg Deltoid 4. 351 mg Gluteal
Eligibility
Sex/Gender
ALL
Age
18 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
* To participate in the study, patients must meet all inclusion criteria at screening: 1. Capable of giving informed consent and complying with study procedures. 2. Have an identified support person (e.g., family member, case worker, social worker) considered reliable by the Investigator to help ensure compliance with study visits and to alert staff of any issues of concern. 3. Have a stable place of residence for the 3 months prior to screening and throughout the study. 4. Male or female ≥18 to ≤65 years of age who meets diagnostic criteria for schizophrenia or schizoaffective disorder according to the Diagnostic and Statistical Manual of Mental Disorders Fifth Edition (DSM-V) for at least 1 year before screening. 5. Have been on a stable dose of oral antipsychotic medication(s) other than risperidone, paliperidone, clozapine, ziprasidone, or thioridazine for at least 4 weeks prior to screening. 6. Be clinically stable based on clinical assessments and a Positive and Negative Syndrome Scale (PANSS) total score ≤75 as well as a PANSS HATE (hostility, anxiety, tension and excitement) subtotal score \<16 at screening. 7. Clinical Global Impression-Severity (CGI-S) score of 1 to 4, inclusive. 8. For patients with schizoaffective disorder only: Young Mania Rating Scale (YMRS) ≤12 and Hamilton Rating Scale for Depression, 17-item version (HAM-D) ≤12. 9. Body mass index (BMI) ≥17.0 and ≤37 kg/m2; body weight ≥50 kg. 10. All female patients (childbearing potential and non-childbearing potential) must have a negative pregnancy test result at both screening and baseline. Female patients must meet 1 of the following 3 conditions: (i) postmenopausal for at least 12 months without an alternative medical cause, (ii) surgically sterile (hysterectomy, bilateral oophorectomy, bilateral salpingectomy, or bilateral tubal occlusion) based on patient report, or (iii) if of childbearing potential (WOCBP) and heterosexually active, practicing or agree to practice a highly effective contraception method of birth control. Highly effective methods of birth control include an intrauterine device (IUD), intrauterine hormone-releasing system (IUS), and contraceptives (oral, skin patches, or implanted or injectable products) using combined or progestogen-only hormonal contraception associated with inhibition of ovulation. A vasectomized male partner is an acceptable birth control method if the vasectomized partner is the sole sexual partner of the female patient and the vasectomized partner has received medical confirmation of surgical success. Highly effective methods of birth control must be used for at least 21 days prior to study drug dosing, throughout the study, and for at least 30 days after the end-of-study (EOS) visit to minimize the risk of pregnancy. 11. Sexually active fertile male patients must be willing to use acceptable contraception methods (such as double barrier methods of a combination of male condom with either cap, diaphragm or sponge with spermicide) from study drug dosing, throughout the study, and for at least 30 days after the EOS visit if their partners are women of childbearing potential.
Exclusion criteria
\- Patients will be excluded from study entry if 1 or more
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetic (PK) profiles of paliperidone in LY03010 | 176 days | To characterize the PK profile of paliperidone in LY03010 from time zero through the last quantifiable concentration The PK profile of LY03010 will be evaluated by the analysis of the area under the concentration-time curve from time zero through the time of the last quantifiable concentration (AUC0-t) and extrapolated through infinity (AUC0-inf). |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Safety and tolerability of LY03010 | 176 days | To characterize the PK profile of LY03010. The PK profile of LY03010 will be evaluated by the analysis of the maximum peak (Cmax) of plasma paliperidone concentration, comparing the two doses. |
Countries
United States
Outcome results
None listed