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

Sponsor
AstraZeneca (Industry)
Overall Status
Completed
CT.gov ID
NCT01194986
Collaborator
(none)
13
Enrollment
1
Location
2
Arms
7
Duration (Months)
1.9
Patients Per Site Per Month

Study Details

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
Phase 1

Study Design

Study Type:
Interventional
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 :
Nov 1, 2010
Actual Primary Completion Date :
Jun 1, 2011
Actual Study Completion Date :
Jun 1, 2011

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) [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). [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 [Collected from Day 1 to follow-up]

  2. Vital signs (body temperature, BP and pulse) [Measured at screening, study days -1 to day 3 and at follow-up]

Eligibility Criteria

Criteria

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

Locations

Site City State Country Postal Code
1 Research Site Uppsala Sweden

Sponsors and Collaborators

  • AstraZeneca

Investigators

  • Study Director: Björn Paulsson, MD, AstraZeneca
  • Principal Investigator: Wolfgang Kühn, MD, Quintiles AB, Uppsala

Study Documents (Full-Text)

None provided.

More Information

Additional Information:

Publications

None provided.
Responsible Party:
AstraZeneca
ClinicalTrials.gov Identifier:
NCT01194986
Other Study ID Numbers:
  • D3030C00003
  • 2009-010702-11
First Posted:
Sep 3, 2010
Last Update Posted:
Jan 28, 2015
Last Verified:
Jan 1, 2015
Keywords provided by AstraZeneca
Receptor binding
Histamine H3 receptor
binding
radioligand

Study Results

No Results Posted as of Jan 28, 2015