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.
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.