Pharmacokinetics, Effect of Food, Safety and Tolerability of a New Tablet Formulation of GSK1144814 in Healthy Subjects
Condition: Schizophrenia
MeSH terms: Schizophrenia
Study type: Interventional
Phase: Phase 1

Summary: 
      GSK1144814 is a potent, insurmountable antagonist at human neurokinin-1 (NK1) and
      neurokinin-3 (NK3) receptors with the potential to treat multiple symptom domains of
      schizophrenia and be an efficacious antidepressant.

      This study will be an open label, randomised, three-way cross-over study to evaluate the
      safety, tolerability and pharmacokinetics of a new tablet formulation of GSK1144814 and to
      evaluate the effect of food on single oral doses of GSK1144814 in healthy male and female
      subjects.
    

Detailed description: 
      GSK1144814 is a potent, insurmountable antagonist at human neurokinin-1 (NK1) and
      neurokinin-3 (NK3) receptors with the potential to treat multiple symptom domains of
      schizophrenia and be an efficacious antidepressant.

      This study will be an open label, randomised, three-way cross-over study to evaluate the
      safety, tolerability and pharmacokinetics of a new tablet formulation of GSK1144814 and to
      evaluate the effect of food on single oral doses of GSK1144814 in healthy male and female
      (non-child bearing potential) subjects.

      The study will consist of a Screening visit (up to 30 days before the first dosing session),
      three dosing sessions each separated by a maximum of at least 6 days washout, and a Follow up
      visit (7 to 14 days after the last dose of study medication). Each subject's participation in
      the study will be approximately 12 weeks Sixteen subjects will be enrolled to provide a
      minimum number of 12 evaluable subjects. The doses to be administered will be 100 mg and
      200mg in the fasted state, and 100mg following a high fat breakfast.

      Subjects will be admitted to the unit on Day 1 of each dosing session and will remain in the
      unit until 48 hours after dosing. Pharmacokinetic samples will be taken for up to 72 hours
      post dose. The duration of both in patient stay and PK sampling may be subject to change
      depending on emerging safety and PK results. Dosing will be in the morning approximately the
      same time for all sessions.

      The objectives of the study are to evaluate the pharmacokinetics, safety and tolerability of
      GSK1144814. Pharmacokinetic objectives are to evaluate the pharmacokinetic parameters of
      single oral doses of GSK1144814 administered as a tablet formulation in healthy male and
      female subjects and to evaluate the effect of a high-fat meal on the pharmacokinetics of
      GSK1144814 tablet following single dose administration of GSK1144814 to healthy male and
      female subjects.

      The safety and tolerability objectives are to evaluate the safety and tolerability of single
      oral doses of GSK1144814 tablet formulation in fed and fasted states.
    

Intervention name(s): GSK1144814
Intervention type(s): Drug
Intervention description(s): This study is an open label, randomised, three-way cross-over study to evaluate the pharmacokinetics, effect of food, safety and tolerability of a new tablet formulation of GSK1144814 in healthy male and female (non-child bearing potential) subjects. Sixteen subjects will be enrolled to provide a minimum number of 12 evaluable subjects. The doses to be administered will be 100 mg and 200mg in the fasted state, and 100mg following a high fat breakfast.
Allocation: Randomized
Intervention model: Crossover Assignment
Masking: None (Open Label)
Primary purpose: Treatment
Keywords: schizophrenia; GSK1144814; effect of food; healthy subjects; depressive disorder; pharmacokinetics