A Drug Interaction Study of Valproic Acid and Single-dose Paliperidone Extended-Release (ER) in Healthy Men

This study has been completed.
Information provided by (Responsible Party):
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
ClinicalTrials.gov Identifier:
First received: January 29, 2010
Last updated: December 21, 2012
Last verified: December 2012
The purpose of this study is to evaluate the effect of valproic acid (VPA) on the pharmacokinetics (blood levels) of a single oral dose of an extended-release formulation of paliperidone in healthy male volunteers.

Condition Intervention Phase
Drug: paliperidone ER
Drug: divalproex sodium ER
Phase 1

Study Type: Interventional
Study Design: Endpoint Classification: Pharmacokinetics Study
Intervention Model: Single Group Assignment
Masking: Open Label
Official Title: An Open-Label, Drug-Drug Interaction Study Between Steady-State Valproic Acid and Single-Dose Paliperidone Extended-Release in Healthy Men

Resource links provided by NLM:

Further study details as provided by Johnson & Johnson Pharmaceutical Research & Development, L.L.C.:

Primary Outcome Measures:
  • To evaluate the pharmacokinetics of a single dose of orally administered paliperidone ER before and during the administration of VPA at steady-state [ Time Frame: Blood samples taken within 2 hours before dosing on Day 1, and during 96 hours after dosing on Day 15 with paliperidone ER ] [ Designated as safety issue: No ]

Secondary Outcome Measures:
  • To determine the effect of a single dose of paliperidone ER on steady-state VPA plasma concentrations [ Time Frame: Predose on Days 12 to 16, and 19 ] [ Designated as safety issue: No ]
  • To evaluate safety and tolerability of the 12-mg tablet of paliperidone ER administered with and without divalproex sodium ER [ Time Frame: Day -1 through the last study assessment on Day 19. ] [ Designated as safety issue: No ]

Enrollment: 24
Study Start Date: January 2009
Study Completion Date: February 2009
Arms Assigned Interventions
paliperidone ER 1 tablet of 500 mg once daily on Day 1 and Day 15
Drug: paliperidone ER
1 tablet of 500 mg once daily on Day 1 and Day 15
divalproex sodium ER 2 tablets of 500 mg once daily from Days 5 through 18
Drug: divalproex sodium ER
2 tablets of 500 mg once daily from Days 5 through 18

  Show Detailed Description


Ages Eligible for Study:   18 Years to 55 Years
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Signed informed consent obtained indicating an understanding of the purpose of and procedures required for the study and willingness to participate in the study
  • Agree to use an adequate contraception method as deemed appropriate by the study physician (for example, vasectomy, double-barrier, partner using effective contraception) and to not donate sperm during the study and for 3 months after receiving the last dose of study drug
  • Have a body mass index (BMI, weight [kg]/height2 [m]2) between 18 and 30 kg/m2 (inclusive) and body weight not less than 50 kg
  • Have a systolic blood pressure between 90 and 140 mm Hg and a diastolic blood pressure between 50 and 90 mm Hg
  • Habitually smokes no more than 10 cigarettes, or 2 cigars, or 2 pipes of tobacco per day for at least 6 months before first study drug administration

Exclusion Criteria:

  • History of or current clinically significant medical illness including (but not limited to) drug or alcohol abuse within the past 5 years, cancer with exception of basal cell carcinoma, epilepsy, suspected urea cycle disorder, any severe pre-existing gastrointestinal narrowing or malabsorption problems, cardiac arrhythmias or other cardiac disease, hematologic disease, coagulation disorders (including any abnormal bleeding or blood dyscrasias), lipid abnormalities, significant pulmonary disease, including bronchospastic respiratory disease, diabetes mellitus, renal or hepatic insufficiency, thyroid disease, neurologic or psychiatric disease, infection, or any other illness that the study physician considers should exclude the healthy volunteer or that could interfere with the interpretation of the study results
  • Known allergy or intolerance to study drugs including paliperidone, valproic acid (VPA), sodium valproate, or divalproex sodium or any of the excipients (inactive substances) of the drugs (such as lactose)
  • Donated blood or blood products or had substantial loss of blood (more than 500 mL) within 3 months before the first administration of study drug or intention to donate blood or blood products during the study or within 1 month after the completion of the study
  • Unable to swallow solid, oral dosage forms whole with the aid of water (participants may not chew, divide, dissolve, or crush the study drugs)
  • Preplanned surgery or procedures that would interfere with the conduct of the study
  Contacts and Locations
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT01060228

Sponsors and Collaborators
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
Study Director: Johnson & Johnson Pharmaceutical Research & Development, L.L. C. Clinical Trial Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
  More Information

Additional Information:
Responsible Party: Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
ClinicalTrials.gov Identifier: NCT01060228     History of Changes
Other Study ID Numbers: CR015802  R076477BIM1003 
Study First Received: January 29, 2010
Last Updated: December 21, 2012
Health Authority: United States: Food and Drug Administration

Keywords provided by Johnson & Johnson Pharmaceutical Research & Development, L.L.C.:
Paliperidone ER
Divalproex sodium
Depakote ER
Valproic Acid
Human Experimentation

Additional relevant MeSH terms:
Paliperidone Palmitate
Valproic Acid
Antimanic Agents
Antipsychotic Agents
Central Nervous System Depressants
Dopamine Agents
Dopamine Antagonists
Dopamine D2 Receptor Antagonists
Enzyme Inhibitors
GABA Agents
Molecular Mechanisms of Pharmacological Action
Neurotransmitter Agents
Physiological Effects of Drugs
Psychotropic Drugs
Serotonin 5-HT2 Receptor Antagonists
Serotonin Agents
Serotonin Antagonists
Tranquilizing Agents

ClinicalTrials.gov processed this record on May 25, 2016