Basmisanil Positron Emission Tomography Study in Japanese Volunteers

A Single-Centre, Non-Randomised, Open Label, Positron Emission Tomography Imaging Study to Assess Occupancy of α5-Containing GABAA Receptors by RO5186582 in Healthy Volunteers of Japanese Origin

This study will evaluate the relationship between basmisanil plasma concentrations and the occupancy of Gamma-Amino Butyric Acid A (GABAA) receptor subtypes containing an alpha5 (α5) subunit in healthy Japanese volunteers. Each participant will have two post-screening imaging sessions. In the first imaging session, participants will have a baseline Positron Emission Tomography (PET) scan. In the second imaging session, participants will receive a single oral dose of basmisanil, followed by two on-treatment PET scans at about 4 and 10 hours post-dose.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteer
• Intervention / Treatment: Drug: Basmisanil

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • London, United Kingdom, W12 0NN
  • London, United Kingdom, NW10 7EW
  • London, United Kingdom, NW10 7EW
    • Hammersmith Medicines Research; Central Middlesex Hospital
  • London, United Kingdom, W12 0NN
    • Imanova Limited

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 45 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Male or female Japanese healthy volunteer, who was born in Japan, has 4 ethnically Japanese grandparents and has lived outside Japan for no longer than 5 years
• A body mass index (BMI, Quetelet index) in the range 18.0 to 32.0 kilograms per square meter (kg/m^2)
• Willingness and ability to comply with study restrictions

Exclusion Criteria:

• A history of epilepsy, convulsions or significant head injury, or other structural brain abnormality
• Pregnant or lactating or not using acceptable contraception
• Presence or history of severe adverse reaction to any drug or a history of sensitivity to basmisanil or the PET radioligand (RO15-4513)
• Significant exposure to radiation within the previous 12 months
• Any other clinically relevant abnormalities, concomitant diseases or ongoing medical conditions

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Basmisanil in Japanese Healthy Volunteers; Japanese healthy volunteers will receive a single oral dose of RO5186582 within 15 minutes after completing a standard meal.	Drug: Basmisanil; Single oral dose: Basmisanil doses between 20 milligrams (mg) and 960 mg may be used in this study. The planned doses for the first two participants are 160 mg and 480 mg, respectively. Basmisanil dose for subsequent participants will be decided by the investigator and sponsor during the study, based on on-going review of emerging data.; Other Names: RO5186582, RG1662

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Percentage of Brain α5 Subunit-Containing GABAA Receptors Occupied by Basmisanil (Receptor Occupancy) Following a Single Dose of Basmisanil in Selected Regions of Interest (ROIs) Assessed by PET Imaging	Day 1
Correlation Between Basmisanil Plasma Concentration and Occupancy of Brain α5 Subunit-Containing GABAA Receptors	Day 1

Secondary Outcome Measures

Outcome Measure	Time Frame
Brain GABAA Receptor α5 Subunit Levels in Selected ROIs Assessed by PET Imaging	Day 1
Percentage of Participants With Adverse Events	From Baseline up to 7-14 days

Collaborators and Investigators

• Sponsor: Hoffmann-La Roche

Study record dates

Study Major Dates

• Study Start: August 1, 2015
• Primary Completion (Actual): October 1, 2015
• Study Completion (Actual): November 1, 2015

Study Registration Dates

• First Submitted: August 21, 2015
• First Submitted That Met QC Criteria: August 26, 2015
• First Posted (Estimate): August 27, 2015

Study Record Updates

• Last Update Posted (Estimate): January 26, 2017
• Last Update Submitted That Met QC Criteria: January 24, 2017
• Last Verified: January 1, 2017

More Information

Terms related to this study

• Other Study ID Numbers: BP29784; 2015-001621-16 (EudraCT Number)