Healthy Volunteer
Conditions
Brief summary
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.
Interventions
DRUGBasmisanil
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.
Sponsors
Hoffmann-La Roche
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
20 Years to 45 Years
Healthy volunteers
Yes
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
Design outcomes
Primary
| 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
| 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 |
Countries
United Kingdom
Outcome results
None listed