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

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

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01253655

Acronym

3193A1-1103

Enrollment

Registered

2010-12-03

Start date

2010-11-30

Completion date

2011-03-31

Last updated

2011-04-28

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Keywords

Healthy Volunteers

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

Interventions

DRUGPF-05212365

Single dose of up to 30 mg PF-05212365, delivered as 1 mg, 3 mg, and/or 5 mg on study day 1.

Study design

Allocation

NON_RANDOMIZED

Intervention model

SINGLE_GROUP

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

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

Design outcomes

Primary

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

Measure	Time frame
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
Number of Participants with Adverse Events as a Measure of Safety and Tolerability	continuous, 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
Time at Cmax (Tmax) for PF-05212365 in plasma	up to 4 days

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026