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

Pfizer12 enrolled

Overview

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-05212377 in healthy volunteers

Study Type

INTERVENTIONAL

Allocation

NON_RANDOMIZED

Purpose

BASIC_SCIENCE

Masking

NONE

Enrollment

Conditions

Healthy

Interventions

PF-05212377DRUG

Single dose of up to 70 mg PF-05212377, delivered as .25 mg, 5 mg and/or 15 mg on study day 1

Eligibility

Sex: ALLMin age: 18 YearsMax age: 55 YearsHealthy volunteers:

Medical Language ↔ Plain English

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

Locations (3)

Pfizer Investigational Site

New Haven, Connecticut, United States

Pfizer Investigational Site

New Haven, Connecticut, United States

Pfizer Investigational Site

New Haven, Connecticut, United States

Outcomes

Primary Outcomes

To assess the central 5-HT6 receptor occupancy (RO) in the striatum in relation to systemic exposure of PF-05212377 after single oral administration in healthy adult subjects.

Time frame: up to 8 days

Secondary Outcomes

Number of Participants with Adverse Events as a Measure of Safety and Tolerability

Time frame: continuous, up to 8 days

Maximum concentration (Cmax) for PF-05212377 in plasma

Time frame: up to 8 days

Time at Cmax (Tmax) for PF-05212377 in plasma

Time frame: up to 8 days

Area under the concentration-time profile from time zero to the time of the last quantifiable concentration (AUClast) for PF-05212377 in plasma

Time frame: up to 8 days

Average concentration during the first post-dose PET scan (Cavg (scan 1)) for PF-05212377 in plasma

Time frame: approximately 4-6 hrs post-dose

Average concentration during the second post-dose PET scan (Cavg (scan 2)) for PF-05212377 in plasma

Time frame: approximately 28-30 hrs post-dose

Data from ClinicalTrials.gov

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