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

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ClinicalTrials.gov Identifier: NCT01194986
Recruitment Status : Completed
First Posted : September 3, 2010
Last Update Posted : January 28, 2015
Sponsor:
Information provided by (Responsible Party):

Study Description
Brief Summary:
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 or disease Intervention/treatment Phase
Brain Distribution of [11C]AZ12807110 and AZD5213 Other: [11C]AZ12807110 Drug: AZD5213 Phase 1

Study Design

Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 13 participants
Allocation: Randomized
Intervention Model: Single Group Assignment
Masking: Single (Participant)
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
Study Start Date : November 2010
Primary Completion Date : June 2011
Study Completion Date : June 2011

Resource links provided by the National Library of Medicine

U.S. FDA Resources

Arms and Interventions

Arm Intervention/treatment
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


Outcome Measures

Primary Outcome Measures :
  1. 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. ]
  2. 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. ]
    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 :
  1. Adverse events [ Time Frame: Collected from Day 1 to follow-up ]
  2. Vital signs (body temperature, BP and pulse) [ Time Frame: Measured at screening, study days -1 to day 3 and at follow-up ]

Eligibility Criteria

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Ages Eligible for Study:   20 Years to 45 Years   (Adult)
Sexes 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

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its ClinicalTrials.gov identifier (NCT number): 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

Additional Information:
Publications automatically indexed to this study by ClinicalTrials.gov Identifier (NCT Number):
Responsible Party: AstraZeneca
ClinicalTrials.gov Identifier: NCT01194986     History of Changes
Other Study ID Numbers: D3030C00003
2009-010702-11 ( EudraCT Number )
First Posted: September 3, 2010    Key Record Dates
Last Update Posted: January 28, 2015
Last Verified: January 2015

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
Physiological Effects of Drugs