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Evaluation of Histamine H3 Receptor Radioligand [11C]AZ12807110 and Histamine H3 Receptor Occupancy of AZD5213 After Oral Administration

This study has been completed.
Sponsor:
Information provided by:
AstraZeneca
ClinicalTrials.gov Identifier:
NCT01194986
First received: September 2, 2010
Last updated: July 12, 2011
Last verified: July 2011
History of Changes
  Purpose

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.


Condition Intervention Phase
Brain Distribution of [11C]AZ12807110 and AZD5213
 Other: [11C]AZ12807110
Drug: AZD5213
 Phase 1

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
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

Resource links provided by NLM:

U.S. FDA Resources

Further study details as provided by AstraZeneca:

Primary Outcome 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. ] [ Designated as 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. ] [ Designated as safety issue: No ]
    Each healthy volunteer in the main panel will complete 3 PET measurements using radioligand; one at baseline and 2 after treatment with AZD5213.


Secondary Outcome Measures:
  • Adverse events [ Time Frame: Collected from Day 1 to follow-up ] [ Designated as 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 ] [ Designated as safety issue: Yes ]

Estimated Enrollment: 13
Study Start Date: November 2010
Study Completion Date: June 2011
Primary Completion Date: June 2011 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Pilot panel
[11C]AZ12807110 distribution and kinetics
 Other: [11C]AZ12807110
Radioligand
Experimental: Main panel
Histamine receptor occupancy reached by AZD5213
 Other: [11C]AZ12807110
Radioligand
Drug: AZD5213

  Eligibility

Ages Eligible for Study:   20 Years to 45 Years
Genders Eligible for Study:   Female
Accepts Healthy Volunteers:   Yes
Criteria

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
  Contacts and Locations
Please refer to this study by its ClinicalTrials.gov identifier: NCT01194986

Locations
Sweden
Research Site
Uppsala, Sweden
Sponsors and Collaborators
AstraZeneca
Investigators
Study Director: Björn Paulsson, MD AstraZeneca
Principal Investigator: Wolfgang Kühn, MD Quintiles AB, Uppsala
  More Information

No publications provided

Responsible Party: Medical Science Director, AstraZeneca
ClinicalTrials.gov Identifier: NCT01194986     History of Changes
Other Study ID Numbers: D3030C00003, 2009-010702-11
Study First Received: September 2, 2010
Last Updated: July 12, 2011
Health Authority: Sweden: Medical Products Agency

Keywords provided by AstraZeneca:
Receptor binding
Histamine H3 receptor
binding
radioligand

Additional relevant MeSH terms:
Histamine
Histamine phosphate
Histamine Agonists
Histamine Agents
 Neurotransmitter Agents
Molecular Mechanisms of Pharmacological Action
Pharmacologic Actions
Physiological Effects of Drugs

ClinicalTrials.gov processed this record on May 23, 2013