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 Subjects With Chronic Stable Schizophrenia”

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

Study Type: Interventional

Study Design: Treatment, Non-Randomized, Open Label, Single Group Assignment, Pharmacokinetics Study

Study Primary Completion Date: June 2009

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, subjects will be treated with a 1 mg immediate release formulation in the first week to confirm that the subject does not develop an allergic reaction to the long acting formulation. Each subject receives a total of two injections. The first one is the immediate release formulation and the second one the new long acting formulation. Eligible subjects can stay on their previous oral medication, no tapering of drugs is needed. Whole blood samples will be collected for the determination of risperidone and 9-hydroxy-risperidone concentrations in plasma. Whole 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 2nd injection of risperidone. Safety will assessed at limited visits throughout the study by monitoring scores of the Clinical Global Impression - Severity (CGI-S), adverse events; changes in clinical laboratory results; extrapyramidal symptoms will be evaluated using the Extrapyramidal Symptom Rating Scale (ESRS); physical examinations; electrocardiograms (ECGs); and patient + 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 in Period 1 and Period 2 will be given in the buttocks muscle (upper, outer side near the hip), separated by a 7 to 14 days wash-out.

Intervention(s) in this Clinical Trial

• Drug: risperidone 4-week LAI formulation

Primary Measures

• To explore the pharmacokinetics of a 4-week LAI formulation of risperidone after single i.m. injection of 75 mg in the gluteal muscle.

Secondary Measures

• To evaluate the safety and tolerability and to explore the feasibility to define an in vitro-in vivo correlation (IVIVC).

Inclusion Criteria:

• Patients with a diagnosis of schizophrenia
• Clinically stable with no change in current antipsychotic medications
• Meet PANSS and 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

Gender Eligibility for this Clinical Trial: Both

Minimum Age for this Clinical Trial: 18 Years

Maximum Age for this Clinical Trial: 55 Years

Are Healthy Volunteers Accepted for this Clinical Trial?: No

Lead Sponsor: Johnson & Johnson Pharmaceutical Research & Development, L.L.C.

Overall Clinical Trial Officials and Contacts

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

Information obtained from ClinicalTrials.gov on February 08, 2010

Link to the current ClinicalTrials.gov record. http://clinicaltrials.gov/show/NCT00821600

Study ID Number: CR015742

ClinicalTrials.gov Identifier: NCT00821600

Health Authority: United States: Food and Drug Administration