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CompletedNCT01194986Updated Jan 28, 2015

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

A Phase 1 interventional study of [11C]AZ12807110 and AZD5213 in Brain Distribution of [11C]AZ12807110 and AZD5213, sponsored by AstraZeneca. Completed at 1 site in Sweden. Open to female participants aged 20 Years to 45 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2015-01-28.

Sponsored by AstraZeneca · Phase 1, Interventional, and Basic science

Phase
Phase 1
Study type
Interventional
Enrollment
13
Allocation
Randomized
Ages
20 Years to 45 Years
Sex
Female
01

Study 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.

02

Conditions studied

  • Brain Distribution of [11C]AZ12807110 and AZD5213

Keywords

  • Receptor binding
  • Histamine H3 receptor
  • binding
  • radioligand
03

In context

Lead sponsor

AstraZeneca is the lead sponsor of 3,429 studies on the registry; 270 are open to participants now.

Of its 357 completed or terminated interventional studies of FDA-regulated products, 173 (48%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
20 Years to 45 Years
Sexes eligible
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

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
05

Study design

Phase
Phase 1
Primary purpose
Basic science
Allocation
Randomized
Intervention model
Single group
Masking
Single (Participant)
Enrollment
13 participants (actual)

Study arms

  • Experimental
    Pilot panel

    \[11C\]AZ12807110 distribution and kinetics

    Other: [11C]AZ12807110

  • Experimental
    Main panel

    Histamine receptor occupancy reached by AZD5213

    Other: [11C]AZ12807110 · Drug: AZD5213

Interventions

  • Other[11C]AZ12807110

    Radioligand

  • DrugAZD5213
06

What researchers measure

Primary outcomes

  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).

    Each healthy volunteer in the main panel will complete 3 PET measurements using radioligand; one at baseline and 2 after treatment with AZD5213.

    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.

Secondary outcomes

  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

07

Study locations

1 site
  • Research Site
    Uppsala, Sweden
08

References and documents

Publications

  • Jucaite A, Takano A, Bostrom E, Jostell KG, Stenkrona P, Halldin C, Segerdahl M, Nyberg S. AZD5213: a novel histamine H3 receptor antagonist permitting high daytime and low nocturnal H3 receptor occupancy, a PET study in human subjects. Int J Neuropsychopharmacol. 2013 Jul;16(6):1231-9. doi: 10.1017/S1461145712001411. Epub 2012 Dec 10. PubMed 23217964 ↗
09

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Jan 28, 2015, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
10

Registry details

Key details

Study ID
NCT01194986
Lead sponsor
AstraZeneca
Responsible party
Sponsor
First posted
Sep 3, 2010
Start date
Nov 2010
Primary completion
Jun 2011
Completion
Jun 2011
Last update
Jan 28, 2015

Study contacts

Björn Paulsson, MD
study director · AstraZeneca
Wolfgang Kühn, MD
principal investigator · Quintiles AB, Uppsala

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

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