Evaluate the PK of LY03010 Process 1 and Process 2 Drug Product vs INVEGA SUSTENNA After Intramuscular Injection in Schizophrenia Patients

NCT04572685 | Completed Phase 1 FDA Drug

• 1 other identifier: LY03010/CT-USA-102
• Study Type: interventional
• Target: 36
• Locations: 1 country
• Sites: 1

Brief Summary

The primary objectives of the study are to characterize the pharmacokinetic (PK) profiles of paliperidone in LY03010 P1 and P2 following a single IM injection in schizophrenia patients and to compare the PK of LY03010 P1 and P2 with that of INVEGA SUSTENNA® following a single IM injection of 156 mg dosage level.

Conditions

Schizophrenia Patients

Outcome Measures

Primary Outcomes (4)

• To characterize the Maximum Plasma Concentration [Cmax]of LY03010 P1, P2 and INVEGA SUSTENNA following a single IM injection of 156 mg dosage level in schizophrenia patients

  The Cmax of LY03010 P1, P2 and INVEGA SUSTENNA will be measured

  120-Day

• To characterize Area under the plasma concentration versus time curve (AUC) of LY03010 P1 and P2 and INVEGA SUSTENNA following a single IM injection of 156 mg dosage level in schizophrenia patients.

  The AUCs of LY03010 P1, P2 and INVEGA SUSTENNA will be evaluated

  120-Day

• To compare the Cmax of LY03010 P1 and P2 with the Cmax of INVEGA SUSTENNA

  The relative bioavailability of LY03010 P1 and P2 to Invega Sustenna will be assessed

  120-Day

• To compare the AUCs of LY03010 P1 and P2 with the AUCs of INVEGA SUSTENNA

  The relative bioavailability of LY03010 P1 and P2 to Invega Sustenna will be assessed

  120-Day

Secondary Outcomes (6)

• To evaluate the safety and tolerability of tested drugs. Safety assessments include Incidence of adverse events.

  120 day

• To evaluate the safety of the tested drugs-- Incident of abnormal vital sign

  120 Day

• To evaluate the safety of the tested drugs-- Incident of abnormal ECG Findings

  120 Day

• To evaluate any abnormal movement symptoms measured by Abnormal Involuntary Movement Scale (AIMS). AIMS measures movement of each part of body muscle with score range of 0-4, 0 means None and 4 means Severe.

  120-Day

• To evaluate any abnormal movement symptoms measured by Barnes Akathisia Rating Scale (BARS). BARS is a rating scale for drug-induced akathisia with a range of 0-14; 0 means Normal and 14 means Severe.

  120-Day

Study Arms (3)

LY03010 Process 1

EXPERIMENTAL

Drug Product of Process 1 ( P1): 156 mg/vial; Single Injection on Day 1 during the entire 120 Day's study. LY03010 P1 using a non-sterile Active Pharmaceutical Ingredients (API) with an absolute ethanol recrystallization was manufactured by an optimized production process

Drug: Paliperidone Palmitate

LY03010 Process 2

EXPERIMENTAL

Drug Product of Process 2 (P2): 156 mg/vial; Single Injection on Day 1 during the entire 120 Day's study. LY03010 P2 using a sterile Active Pharmaceutical Ingredients (API) with an isopropanol recrystallization was manufactured by the same optimized production process as that used in P1.

Drug: Paliperidone Palmitate

INVEGA SUSTENNA

EXPERIMENTAL

INVEGA SUSTENNA 156 mg/vial; Single Injection on Day 1 during the entire 120 Day's study

Drug: Paliperidone Palmitate

Interventions

Paliperidone Palmitate DRUG

A long acting extended release injectable suspension intended for monthly intramuscular administration

Also known as: Paliperidone Injectable Product

INVEGA SUSTENNA; LY03010 Process 1; LY03010 Process 2

Eligibility Criteria

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

You may qualify if:

• Male or female ≥18 to ≤65 years of age who meets diagnostic criteria for schizophrenia according to the Diagnostic and Statistical Manual of Mental Disorders Fifth Edition (DSM-V) for at least 1 year before screening
• 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
• Clinically stable based on clinical assessments and a Positive and Negative Syndrome Scale (PANSS) total score ≤70 as well as a PANSS HATE (hostility, anxiety, tension and excitement) subtotal score \<16 at screening
• Clinical Global Impression-Severity (CGI-S) score of 1 to 4, inclusive
• Body mass index (BMI) ≥17.0 and ≤37kg/m2; body weight ≥50 kg
• Creatinine level within the normal range
• All female patients (childbearing potential and non-childbearing potential) must have a negative pregnancy test result at both screening and baseline.
• 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 another 80 days after the EOT visit (or at least 200 days after the dose, whichever is longer) if their partners are women of childbearing potential.

You may not qualify if:

• Primary and active DSM-V Axis I diagnosis other than schizophrenia
• Patients who meet DSM-V criteria for substance abuse (moderate or severe) with the exception of caffeine or nicotine in the past 6 months prior to screening, or test positive for barbiturate or alcohol at screening or baseline
• Patients who received any of following treatment:
• Use of oral risperidone or paliperidone within 2 weeks before screening.
• Use of clozapine, thioridazine or ziprasidone within 4 weeks before screening.
• Use of 2-week depot formulation of risperidone within 3 months, 1-month depot formulation of risperidone or 9-hydroxy risperidone (INVEGA SUSTENNA) within 1 year,
• Known or suspected hypersensitivity or intolerance of risperidone, paliperidone, or any of their excipients (oral risperidone tolerability test should be completed during the screening period
• QTcF interval greater than 450 msec for males and 470 msec for females or a prior history or presence of circumstances
• Medical history (within 2 years) of clinically significant, gastrointestinal, cardiovascular, cerebrovascular, musculoskeletal, endocrine, hematologic, renal, hepatic, bronchopulmonary, neurologic, immunologic disorders, or drug hypersensitivity which, in the judgement of the Investigator, would interfere with the patient's ability to participate in the study
• History of dementia-related psychosis or Parkinson's Disease

Sponsors & Collaborators

• Luye Pharma Group Ltd.: lead
• Alliance for Clinical Trials in Oncology: collaborator
• Evolution Research Group: collaborator

Study Sites (1)

Hassman Research Institute

Berlin, New Jersey, 08009, United States

Location

MeSH Terms

Interventions

Paliperidone Palmitate

Intervention Hierarchy (Ancestors)

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

Study Officials

• Luye Pharma

  Luye Pharma Group

  STUDY CHAIR

Study Design

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

Model Details: A single dose study in three parallel dosing groups of schizophrenia patients

Study Record Dates

• First Submitted: May 8, 2020
• First Posted: October 1, 2020
• Study Start: January 22, 2020
• Primary Completion: June 26, 2020
• Study Completion: August 20, 2020
• Last Updated: November 9, 2020

Record last verified: 2020-11

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)