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
  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:


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
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

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 by AstraZeneca

Additional publications automatically indexed to this study by ClinicalTrials.gov Identifier (NCT Number):
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 July 22, 2014