A Study to Assess the Pharmacokinetics, Safety, and Tolerability of Paliperidone Palmitate in Patients With Schizophrenia
Condition: Schizophrenia
MeSH terms: Schizophrenia
Study type: Interventional
Phase: Phase 1

Summary: 
      The purpose of this study is to assess the pharmacokinetics, safety, and tolerability of a
      paliperidone palmitate 3-month formulation in patients with schizophrenia.
    

Detailed description: 
      This is a multicenter, randomized (the study drug is assigned by chance), open-label (all
      people know the identity of the intervention), parallel-group (each group of patients will be
      initiated simultaneously) study in 4 panels (A, B, C and D). Each panel will comprise 2
      single-dose treatment periods. In Period 1, all patients from the 4 panels will receive an
      intramuscular (i.m.) injection with 1 mg paliperidone as an immediate release (IR) solution
      to assess tolerability and allergic or hypersensitivity reactions potentially related to
      paliperidone, and to establish the relative bioavailability (the extent to which a drug or
      other substance becomes available to the body) of paliperidone palmitate versus paliperidone
      IR. Patients in Panels A and C will receive an i.m. injection with 1 mg paliperidone IR
      solution in the gluteal muscle, and patients in Panel B and D will receive an i.m. injection
      with 1 mg paliperidone IR solution in the deltoid or gluteal muscle. Patients who tolerate
      this injection and have completed all assessments on Day 5 of Period 1 will be enrolled in
      Period 2. In Period 2, patients will receive a single dose of 3-month paliperidone palmitate
      i.m. injection at the dosages defined for each panel. The study drug injection will be
      followed by a 96-hour observation period in Period 1, and a 364-day or 544-day observation
      period in Period 2. Successive study drug administrations will be separated by a washout
      period (period when receiving no treatment) of at least 7 and no more than 21 days. The total
      study length for all patients is from 53 weeks to a maximum of 58 weeks. Patients in Panel B,
      if consented, and Panel D will participate in the extension period of approximately 26 weeks
      in order to obtain additional assessments to be able to characterize the pharmacokinetics
      (PK) profile. Pharmacokinetics explores how the drug is absorbed in the body, distributed
      within the body, and how it is removed from the body over time. Therefore, for those who
      participate in the extension period, the total study duration will be approximately 84 weeks.
    

Intervention name(s): Paliperidone IR (Period 1); Paliperidone palmitate F015 (Panel A: treatment group 1); Paliperidone palmitate F015 (Panel A: treatment group 2); Paliperidone palmitate F015 (Panel B: treatment group 1); Paliperidone palmitate F015 (Panel B: treatment group 2); Paliperidone palmitate F015 (Panel B: treatment group 3); Paliperidone palmitate F015 (Panel B: treatment group 4); Paliperidone palmitate F015 (Panel B: treatment group 5); Paliperidone palmitate F016; Paliperidone palmitate F015 (Panel D: treatment group 1); Paliperidone palmitate F015 (Panel D: treatment group 2); Paliperidone palmitate F015 (Panel D: treatment group 3); Paliperidone palmitate F015 (Panel D: treatment group 4)
Intervention type(s): Drug; Drug; Drug; Drug; Drug; Drug; Drug; Drug; Drug; Drug; Drug; Drug; Drug
Intervention description(s): Type= exact number, unit= mg, number=1, form= injection, route= intramuscular use. Single injection with 1 mg paliperidone IR in the gluteal or deltoid muscle.; Type= exact number, unit= mg, number=300, form= injection, route= intramuscular use. Single injection with 300 mg eq. 3-month formulation paliperidone palmitate F015 manufactured by milling technique A, in the gluteal muscle.; Type= exact number, unit= mg, number=300, form= injection, route= intramuscular use. Single injection with 300 mg eq. 3-month formulation paliperidone palmitate F015 manufactured by milling technique B, in the gluteal muscle.; Type= exact number, unit= mg, number= 75, form= injection, route= intramuscular use. Single injection with 75 mg eq. 3-month formulation paliperidone palmitate F015 in the gluteal muscle.; Type= exact number, unit= mg, number=150, form= injection, route= intramuscular use. Single injection with 150 mg eq. 3-month formulation paliperidone palmitate F015 in the gluteal muscle.; Type= exact number, unit= mg, number=450, form= injection, route= intramuscular use. Single injection with 450 mg eq. 3-month formulation paliperidone palmitate F015 in the gluteal muscle.; Type= exact number, unit= mg, number=300, form= injection, route= intramuscular use. Single injection with 300 mg eq. 3-month formulation paliperidone palmitate F015 in the deltoid muscle.; Type= exact number, unit= mg, number=450, form= injection, route= intramuscular use. Single injection with 450 mg eq. 3-month formulation paliperidone palmitate F015 in the deltoid muscle.; Type= exact number, unit= mg, number=150, form= injection, route= intramuscular use. Single injection with 150 mg eq. 3-month formulation paliperidone palmitate F016 in the gluteal muscle.; Type= exact number, unit= mg, number=525, form= injection, route= intramuscular use. Single injection with 525 mg eq. 3-month formulation paliperidone palmitate F015 in the gluteal muscle.; Type= exact number, unit= mg, number=525, form= injection, route= intramuscular use. Single injection with 525 mg eq. 3-month formulation paliperidone palmitate F015 in the deltoid muscle.; Type= exact number, unit= mg, number=350, form= injection, route= intramuscular use. Single injection with 350 mg eq. 3-month formulation paliperidone palmitate F015 in the gluteal muscle.; Type= exact number, unit= mg, number=175, form= injection, route= intramuscular use. Single injection with 175 mg eq. 3-month formulation paliperidone palmitate F015 in the deltoid muscle.
Intervention MeSH terms: Paliperidone Palmitate
Allocation: Randomized
Intervention model: Parallel Assignment
Masking: None (Open Label)
Primary purpose: Treatment
Keywords: Schizophrenia; Paliperidone palmitate; R092670; Paliperidone; 3-month formulation; Pharmacokinetics