Characterization of Intramuscular Injections of Risperidone 4 Week Long-acting Injectable (LAI) Formulation in the Buttock of Patients With Schizophrenia

Sponsor

Johnson & Johnson Pharmaceutical Research & Development, L.L.C. (Industry)

Overall Status

Completed

CT.gov ID

NCT00821600

Collaborator

(none)

Enrollment

Locations

Arm

Duration (Months)

Patients Per Site

1.3

Patients Per Site Per Month

Study Details

Study Description

Brief Summary

The purpose of this study is to explore the pharmacokinetics, safety and tolerability of a 4-week long-acting injectable (LAI) formulation of risperidone after single intramuscular (i.m.) injection of 75 mg risperidone LAI in the gluteal muscle.

Condition or Disease	Intervention/Treatment	Phase
Psychotic Disorders Schizophrenia	Drug: risperidone IR and LAI formulation	Phase 1

Detailed Description

An intramuscular injectable formulation of risperidone long-acting formulation is under development with the aim to provide a sustained and stable level of risperidone during each treatment cycle given every 4 weeks. As this formulation is a long acting formulation, patients will be treated with a 1 mg immediate release (IR) formulation in the first week to confirm that the patient does not develop an allergic reaction to the drug before receiving the long acting injectable (LAI) formulation. Each patient receives a total of two injections. The first one is the immediate release formulation and the second one, which is given at least a week later, is the new long acting formulation. Eligible patients can stay on their previous oral medication, no tapering of medication is needed. Blood samples will be collected to determine the levels of risperidone and its major metabolite in plasma. Blood samples will be obtained by venipuncture (needle stick) immediately before (pre-dose) and at 5, 10, 20, 30, 45 min, 1, 1.5, 2, 4, 6, 8,12, 16, 24, 36, 48, 72, 96 hours after the 1st injection and at 2, 6, 12, 24, 48, 96 hrs, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 39, 43, 50, 57, 64, 71, 78, 85 days after the second injection of risperidone. Safety will assessed at visits throughout the study by monitoring scores of the Clinical Global Impression - Severity (CGI-S), scores of Extrapyramidal Symptom Rating Scale (ESRS), adverse events (AE), changes in clinical laboratory results, changes in physical examinations (PE), changes in electrocardiograms (ECGs), as well as patient and investigator evaluation of the injection site. The study has two periods. In the first period all patients will receive one injection of 1 mg risperidone IR (immediate release) solution (liquid). The follow-up duration is 96 hours. In the second period, patients will receive one injection of risperidone 4-week formulation of 75 mg. The follow-up duration is 85 days. The injections, administered in the muscle of the buttocks, will be given 7 to 14 days apart.

Study Design

Study Type:

Interventional

Actual Enrollment :

24 participants

Allocation:

Non-Randomized

Intervention Model:

Single Group Assignment

Masking:

None (Open Label)

Primary Purpose:

Treatment

Official Title:

Single-Dose, Open-Label Pilot Study to Explore the Pharmacokinetics, Safety and Tolerability of a Gluteal Intramuscular Injection of a 4-Week Long-Acting Injectable Formulation of Risperidone in Patients With Chronic Stable Schizophrenia

Study Start Date :

Dec 1, 2008

Actual Primary Completion Date :

Jun 1, 2009

Actual Study Completion Date :

Jun 1, 2009

Arms and Interventions

Arm	Intervention/Treatment
Experimental: 001 risperidone IR and LAI formulation 1 mg risperidone IR single injection followed after 7 to 14 days with 75mg risperidone 4-week-LAI single injection	Drug: risperidone IR and LAI formulation 1 mg risperidone IR single injection, followed after 7 to 14 days with 75mg risperidone 4-week-LAI single injection

Arm

Intervention/Treatment

Experimental: 001

risperidone IR and LAI formulation 1 mg risperidone IR single injection followed after 7 to 14 days with 75mg risperidone 4-week-LAI single injection

Drug: risperidone IR and LAI formulation

1 mg risperidone IR single injection, followed after 7 to 14 days with 75mg risperidone 4-week-LAI single injection

Outcome Measures

Primary Outcome Measures

To explore the pharmacokinetics of a 4-week long acting injectable (LAI) formulation of risperidone after single intramuscular (IM) injection of 75 mg in the gluteal muscle. [Up to 85 days for 4-week LAI formulation of risperidone and up to 96 hrs for immediate release (IR) formulation]

Secondary Outcome Measures

To explore safety and tolerability of a 4-week LAI formulation of risperidone by monitoring scores on CGI-S, scores on ESRS, AEs, PE, lab values, ECG values and injection site reactions. [Up to 85 days]

Eligibility Criteria

Criteria

Ages Eligible for Study:

18 Years to 55 Years

Sexes Eligible for Study:

All

Accepts Healthy Volunteers:

Inclusion Criteria:

Patients with a diagnosis of schizophrenia
Clinically stable with no change in current antipsychotic medications
Meet Positive and Negative Symptom Score (PANSS) and Clinical Global Impression (CGI) score criteria
Have a body mass index (BMI) between 18 and 35 kilogram (kg)/meter (m)2
If a woman, is postmenopausal surgically sterile, abstinent, or, if sexually active, is practicing before entry into the study and agrees to practice throughout the study an effective method of birth control
If a man, agrees to use an adequate contraception method as deemed appropriate by the investigator

Exclusion Criteria:

Alcohol or substance dependence, with the exception of nicotine or caffeine dependence
Involuntarily-committed or unable to provide an informed consent
Has tardive dyskinesia, History of Neuroleptic Malignant Syndrome
History of or current clinically significant medical illness
Treatment with any protocol disallowed therapies
Clinically significant result from screening laboratory or ECG

Contacts and Locations

Locations

	City	State	Country
1	Cerritos	California	United States
2	Santa Ana	California	United States
3	Atlanta	Georgia	United States

Sponsors and Collaborators

Johnson & Johnson Pharmaceutical Research & Development, L.L.C.

Investigators

Study Director: Johnson & Johnson Pharmaceutical Research & Development, L.L. C. Clinical Trial, Johnson & Johnson Pharmaceutical Research & Development, L.L.C.