The purpose of this study is to evaluate the pharmacokinetics (study of what the body does to a drug) and safety of paliperidone palmitate ranging from 75 to 150 milligram equivalents in repeated doses (4 injections) administered in the deltoid muscle (muscle in the shoulder) or gluteal muscle (group of muscles present in the buttocks) in participants with schizophrenia.
This is a multicenter (study conducted at multiple sites), open label (all people know the identity of the intervention), randomized (the study medication is assigned by chance), parallel-group (each group of participants will be treated at the same time) study. Approximately, 60 participants will be enrolled in the study. This study will consist of a screening phase (maximum 14 days), an observation phase (92 days), and a follow-up phase (98 days). Participants will be randomly assigned to treatment group A, B, or C. During the observation phase, participants will receive injections of paliperidone palmitate of concentration ranging from 75 to 150 milligram equivalents in the deltoid muscle or gluteal muscle as applicable on Days 1, 8, 36, and 64 alternating between sides (left/right). Safety evaluations will include assessment of adverse events, clinical laboratory tests, electrocardiogram, vital signs, physical examination, injection site reaction, drug-induced extrapyramidal symptoms scale, and visual analog scale which will be evaluated throughout the study. The total study duration for each participant will be approximately 190 days.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
76
Participants will receive 4 injections of paliperidone palmitate of concentration ranging from 75 to 150 milligram equivalents in deltoid or gluteal muscle as randomized to treatment group A, B, or C on Days 1, 8, 36, and 64.
Plasma concentration of unchanged drug (Paliperidone palmitate)
Time frame: Days 1 to 190
Plasma concentration of active metabolite (paliperidone)
Time frame: Days 1 to 190
Plasma concentration of enantiomer of paliperidone palmitate (R078543)
Time frame: Days 1 to 190
Plasma concentration of enantiomer paliperidone palmitate (R078544)
Time frame: Days 1 to 190
Maximum Observed Plasma Concentration (Cmax) of paliperidone palmitate
The Plasma Concentration (Cmax) is defined as maximum observed analyte concentration.
Time frame: Days 1 to 190
Time to Reach Maximum Observed Plasma Concentration (Tmax) of paliperidone palmitate
The Tmax is defined as actual sampling time to reach maximum observed analyte concentration.
Time frame: Days 1 to 190
Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of paliperidone palmitate
The Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) is a measure of the plasma paliperidone concentration from time zero to end of dosing interval. It is used to characterize drug absorption.
Time frame: Days 1 to 190
Number of participants with adverse events
Time frame: Up to Day 190
Change from baseline in Positive and Negative Syndrome Scale for Schizophrenia (PANSS)
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The PANSS is a medical scale that assesses various symptoms of schizophrenia. The symptoms are rated on a 7-point scale from 1 (absent) to 7 (extreme psychopathology). The total score is the sum of all 30 PANSS items, with a range of 30 (absent) to 210 (extreme ill). Higher scores indicate worsening.
Time frame: Screening, Baseline (Day 1), Days 8, 36, 64, and 92
Change From Baseline in Clinical Global Impression Severity (CGI-S) Scale Score
The CGI-S rating scale is a 7 point global assessment that measures the clinician's impression of the severity of illness exhibited by a participant. A rating of 1 is equivalent to "Normal, not at all ill" and a rating of 7 is equivalent to "Among the most extremely ill participants". Higher scores indicate worsening.
Time frame: Screening, Baseline (Day 1), Days 8, 36, 64, and 92