To Evaluate The Relationship Between Plasma Drug Levels And Receptor Binding In Brain Using PET (Positron Emission Tomography) In Healthy Volunteers (3193A1-1103)

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

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

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: PF-05212365

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Connecticut
    • New Haven, Connecticut, United States, 06511
      • Pfizer Investigational Site
    • New Haven, Connecticut, United States, 06519
      • Pfizer Investigational Site
    • New Haven, Connecticut, United States, 06520
      • Pfizer Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

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

Study Plan

How is the study designed?

Design Details

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

Number of Arms

1

Arms and Interventions

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

What is the study measuring?

Primary Outcome Measures

Outcome Measure	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	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

Collaborators and Investigators

• Sponsor: Pfizer
• Collaborators: Yale University

Publications and helpful links

Helpful Links

• To obtain contact information for a study center near you, click here.

Study record dates

Study Major Dates

• Study Start: November 1, 2010
• Primary Completion (Actual): March 1, 2011
• Study Completion (Actual): March 1, 2011

Study Registration Dates

• First Submitted: November 2, 2010
• First Submitted That Met QC Criteria: December 2, 2010
• First Posted (Estimate): December 3, 2010

Study Record Updates

• Last Update Posted (Estimate): April 28, 2011
• Last Update Submitted That Met QC Criteria: April 26, 2011
• Last Verified: April 1, 2011

More Information

Terms related to this study

• Keywords: Healthy Volunteers
• Other Study ID Numbers: B1961009