Study to assess brain occupancy of σ1 receptors following MR309 dosing
Research type
Research Study
Full title
An exploratory study in healthy volunteers to assess the relationship between plasma exposure of MR309 and occupancy of Sigma 1 receptors σ1 (σ1) in the brain.
IRAS ID
226837
Contact name
Muna Albayaty
Contact email
Sponsor organisation
Mundipharma Research Ltd
Eudract number
2017-000670-11
Duration of Study in the UK
0 years, 3 months, 22 days
Research summary
This is an open-label, exploratory, step-wise design study in healthy volunteers to assess the relationship between the sigma-1 receptor occupancy and the blood levels, following single oral doses of MR309. The study will be run at a single study site based in the United Kingdom (UK) with subjects attending a separate Imaging Facility to undergo the imaging scans.\n\nUp to 8 healthy male subjects will be enrolled after attending a screening visit between 28 and 8 days before dosing. The study will consist of up to 4 cohorts of 1 to 2 subjects. Subjects will receive a single oral dose of MR309 with water. The first cohort of 2 subjects will start with an MR309 dose of 400 mg with subsequent cohort doses depending on the result of the Data Review Meeting. A stepwise design will be followed where data from preceding participants will be evaluated.\n\nEach subject will undergo one magnetic resonance imaging (MRI) scan of the brain at screening and up to 3 positron emission tomography - computed tomography (PET-CT) scans of the head. Each PET-CT scan will follow immediately an injection of [11C]SA4503, a PET radioligand selective for the sigma-1 receptor. One PET-CT scan will be conducted at baseline, while the others will be performed following an oral dose of MR309.\n\nSafety assessment will be performed throughout the study. Total duration of the study for a subject will be up to 60 days. \n\nThis is not a first-in-human study. This means that the study drug researched in this study has been given to humans before. Extensive studies in laboratory animals and previous studies in approximately 312 healthy human volunteers have suggested that MR309 should be safe given in the doses proposed in this study.
REC name
South Central - Berkshire Research Ethics Committee
REC reference
17/SC/0199
Date of REC Opinion
21 Apr 2017
REC opinion
Favourable Opinion