To Evaluate The Relationship Between Plasma Drug Levels And Receptor Binding In Brain Using PET (Positron Emission Tomography) In Healthy Volunteers

Study Overview
=================
Brief Summary
-----------------
The purpose of this study is to evaluate the relationship between plasma drug levels and receptor binding in brain using PET; and to evaluate safety and tolerability after a single administration of PF-05212365 in healthy volunteers

Official Title
-----------------
A Phase 1, Open-Label Study To Evaluate 5-HT6 Receptor Occupancy As Measured By Positron Emission Tomography (PET) With Ligand [11C]PF-04171252 Following Single Oral Dose Administration Of PF-05212365 (SAM-531) In Healthy Subjects

Conditions
-----------------
Healthy

Intervention / Treatment
-----------------
* Drug: PF-05212365


Participation Criteria
=================
Eligibility Criteria
-----------------
Inclusion Criteria: Healthy male and/or female subjects of nonchildbearing potential between the ages of 18 and 55 years, inclusive Exclusion Criteria: Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease. History of regular alcohol consumption exceeding 7 drinks/week for females or 14 drinks/week for males (1 drink = 5 ounces (150 mL) of wine or 12 ounces (360 mL) of beer or 1.5 ounces (45 mL) of hard liquor) within 6 months of screening Fulfillment of any of the MRI contraindications on the standard radiography screening questionnaire

Ages Eligible for Study
-----------------
Minimum Age: 18 Years
Maximum Age: 55 Years

Sexes Eligible for Study
-----------------
All

Accepts Healthy Volunteers
-----------------
Accepts Healthy Volunteers

Study Plan
=================
How is the study designed?
-----------------

Design Details

Primary Purpose: Basic Science
Allocation: Non-Randomized
Intervention Model: Single Group Assignment
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: PF-05212365<br> | Drug: PF-05212365<br>* Single dose of up to 30 mg PF-05212365, delivered as 1 mg, 3 mg, and/or 5 mg on study day 1.<br>* Other names: SAM-531;|

What is the study measuring?
-----------------
Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Exposure response of 5-HT6 Receptor Occupancy (RO) of PF-05212365 in the striatum of healthy adult subjects |  | up to 4 days | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Number of Participants with Adverse Events as a Measure of Safety and Tolerability |  | continuous, up to 4 days | 
| Change from baseline in orthostatic blood pressure |  | Baseline, -5 pre-dose, and 5, 51, and 72 hrs post-dose | 
| Change from baseline in supine blood pressure |  | Baseline, -2.5, -1.5, -.5 pre-dose, and 2, 3, 4, 48, 49, 50 hrs post-dose | 
| Change from baseline in Singlet ECG |  | Baseline and 72 hrs post-dose | 
| Clinically relevant levels of standard hemotology (e.g. Hemoglobin, Hematocrit RBC count), chemistry (e.g. BUN, Creatinine, fasting Glucose), and urinalysis (e.g. pH Glucose, Protein). |  | Baseline and 72 hrs post-dose | 
| Abnormal findings from standard physical examination |  | Baseline and 72 hrs post-dose | 
| Maximum concentration (Cmax) for PF-05212365 in plasma |  | up to 4 days | 
| Time at Cmax (Tmax) for PF-05212365 in plasma |  | up to 4 days | 
| Area under the concentration-time profile from time zero to the time of the last quantifiableconcentration (AUClast) for PF-05212365 in plasma |  | up to 4 days | 
| Average concentration during the first post-dose PET scan (Cavg (scan 1)) for PF-05212365 in plasma |  | 2-4 hrs post-dose | 
| Average concentration during the second post-dose PET scan (Cavg (scan 2)) for PF-05212365 in plasma |  | 48-50 hrs post dose | 
| Change from baseline in orthostatic pulse rate |  | Baseline, -5 pre-dose, and 5, 51, and 72 hrs post-dose | 
| Change from baseline in supine pulse rate |  | Baseline, -2.5, -1.5, -.5 pre-dose, and 2, 3, 4, 48, 49, 50 hrs post-dose | 
| Abnormal findings from standard neurological examination |  | Baseline and 72 hrs post-dose | 

 Terms related to the study
=================
Keywords Provided by Centre Hospitalier Valida
-----------------
Healthy Volunteers