Ignite Creation Date:
2024-05-05 @ 9:02 PM
Last Modification Date:
2024-10-26 @ 9:58 AM
Study NCT ID:
NCT00796029
Status:
COMPLETED
Last Update Posted:
2011-06-08
First Post:
2008-11-20
Brief Title:
A Study of Plasma Concentrations Metabolism and Excretion of 14C-paliperidone After a Single Oral Dose
Sponsor:
Johnson Johnson Pharmaceutical Research Development LLC
Organization:
Johnson Johnson Pharmaceutical Research Development LLC
Study Overview
Official Title:
Plasma Concentrations Metabolism and Excretion of 14C-paliperidone After a Single Oral Dose in Healthy Male Subjects
Status:
COMPLETED
Status Verified Date:
2010-03
Last Known Status:
None
Delayed Posting:
No
If Stopped, Why?:
Not Stopped
Has Expanded Access:
No
If Expanded Access, NCT#:
N/A
Has Expanded Access, NCT# Status:
N/A
Acronym:
None
Brief Summary:
The purposes of this study are to investigate the metabolic pathways of paliperidone and excretion of paliperidone and its metabolites in healthy adult male volunteers both CYP2D6 poor and extensive metabolizers after administration of a single 1-mg oral dose of 14C-paliperidone to evaluate the safety and tolerability of paliperidone and to determine the relationship between genotypes CYP2D6 CYP3A4 CYP3A5 UGT1A1 and UGT1A6 and exposure to paliperidone and its metabolites
Detailed Description:
This study is designed as a single-center single-dose open-label study of the absorption metabolism and excretion of paliperidone in healthy men 3 extensive and 3 poor metabolizers based on CYP2D6 phenotype Eligible volunteers will be admitted to the study center the evening before study drug administration and will remain at the study center until 168 hours after dosing or longer if required up to a maximum of 14 days Each volunteer will receive a single oral dose of 14C-paliperidone with total radioactivity below 1000 µSv 16 mCi Blood samples for plasma pharmacokinetic profile will be obtained immediately before study drug administration and 05 1 15 3 6 12 16 36 48 72 96 120 144 and 168 hours postdose Blood samples will be obtained 2 4 8 and 24 hours postdose for determination of 14C in whole blood Samples for determination of serum creatinine will be obtained 2 4 8 and 24 hours postdose Urine will be collected immediately prior to drug administration and from 0-4 4-8 8-12 12-16 16-24 24-36 36-48 48-72 72-96 96-120 120-144 and 144-168 hours after study drug administration Fecal samples will be collected per each stool once before study drug administration and in the period from 0-168 hours after study drug administration Collections of urine and feces per 24 hours will continue beyond 168 hours to a maximum of 336 hours Day 15 for patients who excrete radioactivity slowly 2 latest 24-hour urine collections each greater than or equal to 2 of total radioactive dose or have 7 feces stool samples over the 0 to 168-hour period 14C radioactivity will be measured in plasma urine and feces Aliquots of the 0- through 24 hour urine collections will be analyzed for creatinine Plasma concentrations of paliperidone and risperidone will be determined by means of a validated LC MSMS method The 14C-labeled moiety in plasma and urine will be determined by liquid scintillation counting For all plasma samples the lower limits of quantification for paliperidone and risperidone will be 0100 ngmL For all plasma and urine samples the lower limits of quantification for 14C-paliperidone will be 72 dpmmL 20n g eqmL The rationale for the present study with a single-dose administration of 1 mg 14C-paliperidone to healthy white men is to determine the routes of excretion for paliperidone and to elucidate the metabolic pathways and structures of predominant paliperidone metabolites As such this study will result in a more complete understanding of the pharmacokinetics of paliperidone in humans Safety and tolerability will be monitored Volunteers will receive a single oral 1 mg dose of 14C-paliperidone as a solution with a specific activity of 592 kBqmg resulting in an administered radioactivity of 592 kBq or 16 µCi The total radioactive load for the subject will remain lower than 1000 µSv
Study Oversight
Has Oversight DMC:
None
Is a FDA Regulated Drug?:
None
Is a FDA Regulated Device?:
None
Is an Unapproved Device?:
None
Is a PPSD?:
None
Is a US Export?:
None
Is an FDA AA801 Violation?:
None