A Study of Plasma Concentrations, Metabolism and Excretion of 14C-paliperidone After a Single Oral Dose

• Status: Completed
• Trial end date: 2003-07-01
• Target enrollment: 0
• Participant gender: Male

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.

• Phase: Phase 1
• Accepts Healthy Volunteers?: Accepts Healthy Volunteers

Details

• Lead Sponsor: Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
• Treatments: Paliperidone Palmitate

Criteria

Inclusion Criteria:

• Dextromethorphan metabolic ratio of >0.345 (poor metabolizer) or <0.0255 (extensive metabolizer)

• Body Mass Index: (weight [kg]/height [m]2) between 20 and 28 kg/m2, inclusive

• Volunteers must have signed an informed consent document indicating that they understand the purpose of and procedures required for the study and are willing to participate in the study

• Healthy based on a prestudy physical examination, medical history, ECG, the results of hematology and serum chemistry tests, and a urinalysis carried out within the 3 weeks prior to administration of study drug. If the results of the hematology tests, serum chemistry tests (except for liver enzymes and serum creatinine), or the urinalysis are not within the laboratory's reference ranges, the volunteer can be included only on the condition that the investigator judges that the deviations are not clinically significant.

Exclusion Criteria:

• Relevant history of cardiac arrhythmias, bronchospastic or cardiovascular disease (e.g., history of ischemic heart disease or cerebrovascular accident)

• respiratory, neuropsychiatric, renal, hepatic, gastrointestinal (including surgeries, and malabsorption problems), endocrine (including diabetes mellitus and thyrotoxicosis), or immunologic diseases

• parkinsonism

• or drug allergy

• History of any cancer, with the exception of basal cell carcinoma

• Have received an experimental drug or used an experimental medical device within 30 days before the planned start of treatment

• History of smoking or use of nicotine-containing substances within the last 2 months, as determined by medical history and/or volunteer's verbal report

• History of alcohol or substance abuse. Positive test results for urine drug screen or alcohol breath test upon admission to the study center on Day 1

• Positive results for any of the serology tests (hepatitis B surface antigen, human immunodeficiency virus [HIV] antibody, and hepatitis C viral antibody)

• Liver function tests or serum creatinine exceeding normal limits at screening