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

NCT01258751 | Completed Phase 1

• 1 other identifier: B2081007
• Study Type: interventional
• Target: 12
• Locations: 1 country
• Sites: 3

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-05212377 in healthy volunteers

Conditions

Healthy

Keywords

Healthy Volunteers

Outcome Measures

Primary Outcomes (1)

• 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.

  up to 8 days

Secondary Outcomes (6)

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

  continuous, up to 8 days

• Maximum concentration (Cmax) for PF-05212377 in plasma

  up to 8 days

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

  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

  up to 8 days

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

  approximately 4-6 hrs post-dose

Study Arms (1)

PF-05212377

EXPERIMENTAL

Drug: PF-05212377

Interventions

PF-05212377 DRUG

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

Also known as: SAM-760

PF-05212377

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male and/or female subjects of nonchildbearing potential between the ages of 18 and 55 years, inclusive

You may not qualify if:

• 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

Sponsors & Collaborators

• Pfizer: lead
• Yale University: collaborator

Study Sites (3)

Pfizer Investigational Site

New Haven, Connecticut, 06511, United States

Location

Pfizer Investigational Site

New Haven, Connecticut, 06519, United States

Location

Pfizer Investigational Site

New Haven, Connecticut, 06520, United States

Location

Related Publications (1)

• Sawant-Basak A, Chen L, Lockwood P, Boyden T, Doran AC, Mancuso J, Zasadny K, McCarthy T, Morris ED, Carson RE, Esterlis I, Huang Y, Nabulsi N, Planeta B, Fullerton T. Investigating CNS distribution of PF-05212377, a P-glycoprotein substrate, by translation of 5-HT6 receptor occupancy from non-human primates to humans. Biopharm Drug Dispos. 2023 Feb;44(1):48-59. doi: 10.1002/bdd.2351. Epub 2023 Mar 13.

  PMID: 36825693 DERIVED

Related Links

• To obtain contact information for a study center near you, click here.

MeSH Terms

Interventions

SAM-760

Study Officials

• Pfizer CT.gov Call Center

  Pfizer

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY

Study Record Dates

• First Submitted: December 9, 2010
• First Posted: December 13, 2010
• Study Start: December 1, 2010
• Primary Completion: May 1, 2011
• Study Completion: May 1, 2011
• Last Updated: July 6, 2011

Record last verified: 2011-07

Locations

US (3)