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

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: PF-05212365

• Registration Number: NCT01253655
• Lead Sponsor: Pfizer

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

Detailed Description

Not available

Study Timeline

• Study Start: 2010-11
• Study First Submitted: 2010-11-02
• Study First Submitted QC: 2010-12-02
• Study First Posted: 2010-12-03
• Primary Completion: 2011-03
• Study Completion: 2011-03
• Status Verified: 2011-04
• Last Update Submitted: 2011-04-26
• Last Update Posted: 2011-04-28

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 6

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 & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
PF-05212365	PF-05212365	-

Primary Outcome Measures

Name	Time	Method
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

Name	Time	Method
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

Trial Locations

Locations (1)

Pfizer Investigational Site; 🇺🇸 New Haven, Connecticut, United States