Evaluation of Histamine H3 Receptor Radioligand [11C]AZ12807110 and Histamine H3 Receptor Occupancy of AZD5213 After Oral Administration
Phase 1
Completed
- Conditions
- Brain Distribution of [11C]AZ12807110 and AZD5213
- Interventions
- Other: [11C]AZ12807110
- Registration Number
- NCT01194986
- Lead Sponsor
- AstraZeneca
- 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.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- Female
- Target Recruitment
- 13
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
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- SINGLE_GROUP
- Arm && Interventions
Group Intervention Description Pilot panel [11C]AZ12807110 \[11C\]AZ12807110 distribution and kinetics Main panel [11C]AZ12807110 Histamine receptor occupancy reached by AZD5213 Main panel AZD5213 Histamine receptor occupancy reached by AZD5213
- Primary Outcome Measures
Name Time Method 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.
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.
- Secondary Outcome Measures
Name Time Method Adverse events Collected from Day 1 to follow-up Vital signs (body temperature, BP and pulse) Measured at screening, study days -1 to day 3 and at follow-up
Trial Locations
- Locations (1)
Research Site
🇸🇪Uppsala, Sweden