Positron Emission Tomography (PET) Study With (11C) Flumazenil to Determine Central GABAA Receptor Occupancy of AZD6280

NCT00681746 | Completed Phase 1

• 2 other identifiers: D0850C00011EudractCT 2007-006683-29
• Study Type: interventional
• Target: 8
• Locations: 1 country
• Sites: 1

Brief Summary

The study is carried out in order to determine the relationship between the dose of AZD6280 and the blood concentration of AZD6280, and to investigate to which extent AZD6280 binds to GABAA receptors

Conditions

Anxiety

Keywords

Anxiety; GABA receptors; Positron Emission Tomography; PET; phase I

Outcome Measures

Primary Outcomes (1)

• Positron emission tomography using the radioligand (11C) flumazenil

  4 times per subject

Secondary Outcomes (2)

• To assess safety of AZD7325 by assessment of adverse events, vital signs, ECGs, psychometric tests and laboratory variables.

  6 visits with tests for the 2 subjects in the first group (Panel 1). 4 visits with tests for the 6 remaining subjects. Some tests will be done several times per visit. All tests will not be done at every visit.

• Investigate the pharmacokinetics of AZD6280 following single doses of AZD6280 by assessment of drug concentration in plasma.

  3 times for the 2 subjects in the first group (Panel 1). Once for the 6 remaining subjects. Up to 48 hours at each time.

Study Arms (1)

1

EXPERIMENTAL

Drug: AZD6280; Drug: (11C) flumazenil

Interventions

AZD6280 DRUG

Single dose of oral solution or capsule(s). 3 times for the 2 subjects in Panel 1. Once for the 6 remaining subjects.

1

(11C) flumazenil DRUG

Single dose of intravenous solution. 4 times for 2 subjects in Panel 1. 2 times for the remaining 6 subjects. (once together with AZD6280)

1

Eligibility Criteria

• Age: 20 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Body Mass Index (BMI) of 18-30 kg/m2 and weight of 60-100 kg
• Clinically normal physical findings, medical history and laboratory values.

You may not qualify if:

• Clinically significant illness or clinical relevant trauma within 2 weeks before the study start.
• History of clinically significant heart arrythmias or heart disease/problems.
• Previous participation in a PET study within the past 12 months. Suffer from claustrophobia and would be unable to undergo MRI (magnetic resonance imaging) or PET scanning.

Sponsors & Collaborators

• AstraZeneca: lead

Study Sites (1)

Research Site

Stockholm, Sweden

Location

Related Publications (1)

• Jucaite A, Cselenyi Z, Lappalainen J, McCarthy DJ, Lee CM, Nyberg S, Varnas K, Stenkrona P, Halldin C, Cross A, Farde L. GABAA receptor occupancy by subtype selective GABAAalpha2,3 modulators: PET studies in humans. Psychopharmacology (Berl). 2017 Feb;234(4):707-716. doi: 10.1007/s00213-016-4506-4. Epub 2016 Dec 24.

  PMID: 28013354 DERIVED

MeSH Terms

Conditions

Anxiety Disorders

Interventions

4-amino-8-(2,5-dimethoxyphenyl)-N-propylcinnoline-3-carboxamide; Flumazenil

Condition Hierarchy (Ancestors)

Mental Disorders

Intervention Hierarchy (Ancestors)

Benzodiazepinones; Benzodiazepines; Benzazepines; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds

Study Officials

• Bo Fransson

  AstraZeneca Clinical Pharmacology Unit, Stockholm, Sweden

  PRINCIPAL INVESTIGATOR

• Eva Taavo

  AstraZeneca R&D, Study Delivery, Clinical Development, Södertälje, Sweden

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY

Study Record Dates

• First Submitted: May 16, 2008
• First Posted: May 21, 2008
• Study Start: February 1, 2008
• Primary Completion: September 1, 2008
• Study Completion: September 1, 2008
• Last Updated: December 10, 2010

Record last verified: 2008-11

Locations

SE (1)