3193A1-1103: To Evaluate The Relationship Between Plasma Drug Levels And Receptor Binding In Brain Using PET (Positron Emission Tomography) In Healthy Volunteers
Study Details
Study Description
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
| Condition or Disease | Intervention/Treatment | Phase |
|---|---|---|
| Phase 1 |
Study Design
Arms and Interventions
| 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:
|
Outcome Measures
Primary Outcome Measures
- 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
- 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]
Eligibility Criteria
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
Contacts and Locations
Locations
| Site | City | State | Country | Postal Code | |
|---|---|---|---|---|---|
| 1 | Pfizer Investigational Site | New Haven | Connecticut | United States | 06511 |
| 2 | Pfizer Investigational Site | New Haven | Connecticut | United States | 06519 |
| 3 | Pfizer Investigational Site | New Haven | Connecticut | United States | 06520 |
Sponsors and Collaborators
- Pfizer
- Yale University
Investigators
- Study Director: Pfizer CT.gov Call Center, Pfizer
Study Documents (Full-Text)
None provided.More Information
Additional Information:
Publications
None provided.- B1961009