Brief Summary

Skip to Participation Criteria

Official Title: "An Open-label Positron Emission Tomography Study to Evaluate Use of Histamine H3 Receptor Radioligand [11C]AZ12807110 and to Determine Histamine H3 Receptor Occupancy of AZD5213 After Oral Administration to Healthy Volunteers"

The purpose of this study is to investigate features of radioligand [11C]AZ12807110 and how much AZD5213 displaces radioligand from histamine receptors when given together.

• Study Type: Interventional
• Study Design: Allocation: Randomized, Endpoint Classification: Pharmacokinetics/Dynamics Study, Intervention Model: Single Group Assignment, Masking: Single Blind (Subject), Primary Purpose: Basic Science
• Study Primary Completion Date: June 2011

Interventions Used in this Clinical Trial

• Other: [11C]AZ12807110
  • Radioligand
• Drug: AZD5213

Arms, Groups and Cohorts in this Clinical Trial

• Experimental: Pilot panel
  • [11C]AZ12807110 distribution and kinetics
• Experimental: Main panel
  • Histamine receptor occupancy reached by AZD5213

Outcome Measures for this Clinical Trial

Primary Measures

• Distribution volume (VT)
  • Time Frame: Venous blood samples for determination of concentrations of AZD5213 in plasma will be taken on many occasions from pre-dose until 48 h post-dose. Single PET measurement will take maximum 2 hours.
    Safety Issue?: No
• Estimation of the plasma concentration resulting in 50% receptor occupancy (Ki, pl).
  • Time Frame: Venous blood samples for determination of concentrations of AZD5213 in plasma will be taken on many occasions from pre-dose until 48 h post-dose.
    Safety Issue?: No

Secondary Measures

• Adverse events
  • Time Frame: Collected from Day 1 to follow-up
    Safety Issue?: Yes
• Vital signs (body temperature, BP and pulse)
  • Time Frame: Measured at screening, study days -1 to day 3 and at follow-up
    Safety Issue?: Yes

Criteria for Participation in this Clinical Trial

Inclusion Criteria

• Healthy male and/or female volunteers between 20 to 45 years with suitable veins for cannulation or repeated venipuncture (pilot panel)
• Female must be of non-child bearing potential (pilot panel)
• BMI between 18 to 30 30 kg/m2
• Normal MRI scan
• Provision of signed, written and dated informed consent

Exclusion Criteria

• History of any clinically significant disease or disorder
• History or presence of gastrointestinal, hepatic or renal disease
• Prolonged QTcF >450 ms or shortened QTcF <340 ms or family history of long QT syndrome
• History of severe allergy or hypersensitivity or ongoing allergy or hypersensitivity
• Healthy volunteer suffers from claustrophobia

Gender Eligibility for this Clinical Trial: Female

Minimum Age for this Clinical Trial: 20 Years

Maximum Age for this Clinical Trial: 45 Years

Are Healthy Volunteers Accepted for this Clinical Trial: Accepts Healthy Volunteers

Clinical Trial Investigator Information

• Lead Sponsor
  • AstraZeneca
• Provider of Information About this Clinical Study
  • Medical Science Director, AstraZeneca
• Overall Official(s)
  • Björn Paulsson, MD, Study Director, AstraZeneca
  • Wolfgang Kühn, MD, Principal Investigator, Quintiles AB, Uppsala