A Phase 1 interventional study of IR OROS paliperidone and ER OROS paliperidone in Schizophrenia, sponsored by Johnson & Johnson Pharmaceutical Research & Development, L.L.C.. Completed. Open to participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2011-06-08.
Sponsored by Johnson & Johnson Pharmaceutical Research & Development, L.L.C. · Phase 1, Interventional, and Treatment
The purpose of this study is to characterize the pharmacokinetics of paliperidone in plasma and urine after intravenous (i.v.) administration of the racemate, administration of the immediate-release (IR) racemate oral solution, administration of the ER OROS tablet, and administration of the oral solutions of the individual enantiomers R078543 (+) and R078544 (-); to determine the absolute oral bioavailability of IR and ER OROS paliperidone; to document the (+) and (-) paliperidone enantiomer ratio after i.v. and oral administration (IR and ER OROS paliperidone); to document the possible interconversion between the (+) and (-) enantiomers of paliperidone after oral treatment with the separate enantiomers; to document the possible relationship between the subject's CYP2D6 phenotype and the (+) and (-) enantiomer disposition of paliperidone (CYP2D6 genotyping was used to corroborate the phenotype). In addition, the safety and tolerability of all treatments will be evaluated.
This is a single-center, single-dose, open-label, randomized, crossover study in healthy adults, following a 5-sequence, 5-treatment, 5-period Latin square design. The study consists of a screening phase (within 21 days before the first administration of study drug), and a treatment phase consisting of 5 periods during which volunteers will receive a single dose of study drug under fasting conditions [orally with 240 mL of water or intravenously (i.v.)] in a random order. Pharmacokinetic blood and urine samples will be collected over a 96-hour period following study drug administration during each treatment period. Volunteers will be confined to the testing facility from at least 10 hours before dosing until 72 hours after dosing in each treatment period and will return for additional assessments. Each administration of study drug will be separated by a washout period of at least 7 to a maximum of 14 days. The duration of volunteer participation is maximally 12 weeks, including the 3 week screening period. CYP2D6 metabolizer status will be assessed by phenotyping and will be corroborated by genotyping of a DNA sample to be collected from volunteers who consent to this part of the study. Pharmacokinetic data are available after oral administration of immediate release and extended release formulations of paliperidone. No data are available after i.v. administration of paliperidone. The data obtained in this study for the i.v. route are important to further characterize the pharmacokinetics of paliperidone, and for future population pharmacokinetics modeling of paliperidone. For chiral substances, it is requested by regulatory authority guidelines to document the disposition of the enantiomers. Therefore, the disposition of the (+) and (-) enantiomers of paliperidone for different administration routes (i.v. and oral) and formulations (immediate release and extended release [ER OROS]) will be documented. Separate enantiomers will be administered in this study, as it is important for the full understanding of the pharmacokinetics of paliperidone to document the possible chiral interconversion. Safety and tolerability will be monitored throughout the study. 5 single doses, one each of: Treatment A, 1 mg IR paliperidone oral solution; Treatment B, 3 mg ER OROS paliperidone oral; Treatment C, 1 mg paliperidone as a 30-min i.v. infusion; Treatment D, 1 mg (+)-paliperidone (R078543) oral solution; and Treatment E, 1 mg (-)-paliperidone (R078544) oral solution.
3,471 studies on the registry are indexed under Schizophrenia; 472 are open to participants now.
This study's enrollment of 20 is below the median of 70 across 2,872 interventional studies indexed under Schizophrenia.
Browse Schizophrenia studies →Johnson & Johnson Pharmaceutical Research & Development, L.L.C. is the lead sponsor of 458 studies on the registry; none are open to participants now.
Counted across the registry records on this site, refreshed daily.
Exclusion Criteria:
To characterize and document the pharmacokinetics of paliperidone in plasma and urine;the (+) and (-) paliperidone ratio;the possible interconversion between the (+)- and (-)- enantiomers of paliperidone;the absolute oral bioavailability of paliperidone
To document the possible relationship between the volunteer's CYP2D6 phenotype and the disposition of the (+) and (-) enantiomers of paliperidone and to evaluate the safety and tolerability of the treatments in healthy volunteers
No study locations are listed for this record.
This study is completed, as verified in Mar 2010. You cannot join it, but the record below documents what was studied.
Get an email when the registry record changes — status, dates, results — or when someone posts here.
Sign in to followQuestions and observations about this study, from anyone following it. Not medical advice, and not a channel to the study team — their contact details are on the registry record.
Sign in to join the discussion. Reading takes no account; posting does. You choose a display name, and a pseudonym is the default.
Nothing here yet. If you are running this trial, taking part in it, or weighing whether to, this is the place to say so.
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.