Clinical trial NCT01253655: To Evaluate The Relationship Between Plasma Drug Levels And Receptor Binding In Brain Using PET (Positron Emission Tomography) 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
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Keywords: Healthy Volunteers
Lead sponsor: Pfizer
Sponsor class: INDUSTRY
Collaborators: name: Yale University
First posted: 2010-12-03
Enrollment: 6
Sex: ALL
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NON_RANDOMIZED
Intervention model: SINGLE_GROUP
Primary purpose: BASIC_SCIENCE

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


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

Primary outcomes:
measure: Exposure response of 5-HT6 Receptor Occupancy (RO) of PF-05212365 in the striatum of healthy adult subjects
timeFrame: up to 4 days
Secondary outcomes:
measure: Number of Participants with Adverse Events as a Measure of Safety and Tolerability
timeFrame: continuous, up to 4 days
measure: Change from baseline in orthostatic blood pressure
timeFrame: Baseline, -5 pre-dose, and 5, 51, and 72 hrs post-dose
measure: Change from baseline in supine blood pressure
timeFrame: Baseline, -2.5, -1.5, -.5 pre-dose, and 2, 3, 4, 48, 49, 50 hrs post-dose
measure: Change from baseline in Singlet ECG
timeFrame: Baseline and 72 hrs post-dose
measure: 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).
timeFrame: Baseline and 72 hrs post-dose
measure: Abnormal findings from standard physical examination
timeFrame: Baseline and 72 hrs post-dose
measure: Maximum concentration (Cmax) for PF-05212365 in plasma
timeFrame: up to 4 days
measure: Time at Cmax (Tmax) for PF-05212365 in plasma
timeFrame: up to 4 days
measure: Area under the concentration-time profile from time zero to the time of the last quantifiableconcentration (AUClast) for PF-05212365 in plasma
timeFrame: up to 4 days
measure: Average concentration during the first post-dose PET scan (Cavg (scan 1)) for PF-05212365 in plasma
timeFrame: 2-4 hrs post-dose
measure: Average concentration during the second post-dose PET scan (Cavg (scan 2)) for PF-05212365 in plasma
timeFrame: 48-50 hrs post dose
measure: Change from baseline in orthostatic pulse rate
timeFrame: Baseline, -5 pre-dose, and 5, 51, and 72 hrs post-dose
measure: Change from baseline in supine pulse rate
timeFrame: Baseline, -2.5, -1.5, -.5 pre-dose, and 2, 3, 4, 48, 49, 50 hrs post-dose
measure: Abnormal findings from standard neurological examination
timeFrame: Baseline and 72 hrs post-dose
Other outcomes:
Locations:
city: New Haven
country: United States
facility: Pfizer Investigational Site
state: Connecticut
city: New Haven
country: United States
facility: Pfizer Investigational Site
state: Connecticut
city: New Haven
country: United States
facility: Pfizer Investigational Site
state: Connecticut
Study officials:
affiliation: Pfizer
name: Pfizer CT.gov Call Center
role: STUDY_DIRECTOR
References: