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

AstraZeneca

Status and phase: Completed; Phase 1

Conditions: Brain Distribution of [11C]AZ12807110 and AZD5213

Treatments: Drug: AZD5213; Other: [11C]AZ12807110

Study type: Interventional

Funder types: Industry

Identifiers

NCT01194986

D3030C00003

2009-010702-11 (EudraCT Number)

Details and patient eligibility

About

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.

Enrollment: 13 patients

Sex: Female

Ages: 20 to 45 years old

Volunteers: Accepts Healthy Volunteers

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

Trial design

Primary purpose: Basic Science

Allocation: Randomized

Interventional model: Single Group Assignment

Masking: Single Blind

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13 participants in 2 patient groups

Pilot panel

Experimental group

Description:

[11C]AZ12807110 distribution and kinetics

Treatment:

Other: [11C]AZ12807110

Main panel

Experimental group

Description:

Histamine receptor occupancy reached by AZD5213

Treatment:

Drug: AZD5213

Other: [11C]AZ12807110