First Study in Humans With GSK206136

Study Overview
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Brief Summary
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This is the first study in humans with GSK206136 to evaluate what effects: good or bad, the drug has on human health (safety and tolerability) and the amount of drug which gets into the bloodstream and is eliminated from the body (pharmacokinetics). Also the study aims to investigate the penetration of the drug in the human brain by using PET (Positron Emission Tomography) imaging technology

Official Title
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A Single Blind, Randomised, Placebo Controlled, Single Ascending Dose Study to Evaluate the Safety, Tolerability and Pharmacokinetics of GSK206136 in Healthy Male Subjects and an Open Label Positron Emission Tomography Study to Evaluate the Serotonin Transporter and Neurokinin-1 Receptor Occupancy

Conditions
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Depressive Disorder and Anxiety Disorders

Intervention / Treatment
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* Drug: GSK206136
* Drug: PLACEBO
* Radiation: PET


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Healthy males aged 18-45 years, limited to 25-40 years of age for PET section Exclusion Criteria: The subject has a positive: drug/alcohol, Hepatitis, HIV screen.. The subject has a history of psychiatric illness suicidal attempts or behaviour. Abuse of alcohol. Clinically significant laboratory, ECG abnormality; The subject has recently received an investigational. Use of prescription or non-prescription drugs, History or presence of allergy to the study drug or drugs of this class, Donation of more than 500 mL blood within the 90 days before dosing. An unwillingness of male subjects to comply with contraceptive requirements Average daily caffeine intake exceeding Protocol requirements.

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 45 Years

Sexes Eligible for Study
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Male

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Basic Science
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: Double


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: Active<br>GSK206136 once daily | Drug: GSK206136<br>* GSK206136 2mg, 10mg, 50mg, 100mg capsule<br>Radiation: PET<br>* Each subject will undergo 3 PET Scans ; one at Baseline and the others following dosing with GSK206136 at approximately 2 hours post-dose and 24 hours post-dose<br>|
| Placebo Comparator: Placebo<br>Placebo once daily | Drug: PLACEBO<br>* Placebo to match 206136 2mg, 10mg, 50mg, 100mg capsule<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Adverse event monitoring, vital signs (blood pressure, heart rate, ECGs, clinical laboratory assessments (standard laboratory parameters); pharmacokinetics parameters: AUC, Cmax, t1/2 |  | 12 weeks | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Brain receptor occupancy |  | 2 weeks | 

 Terms related to the study
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Keywords Provided by Centre Hospitalier Valida
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Nk1 Antagonist and SSRI, Safety, First Time in Humans, Healthy Subjects