Open-label, SAD Study to Investigate Receptor Occupancy of HTL0014242
Research type
Research Study
Full title
An Open-label, Single Centre, Single Oral Dose Study to Investigate the Receptor Occupancy of HTL0014242 using [18F]FPEB in Healthy Male Subjects.
IRAS ID
278968
Contact name
Pablo ForteSoto
Contact email
Sponsor organisation
Heptares Therapeutics
Eudract number
2020-000602-28
Clinicaltrials.gov Identifier
Duration of Study in the UK
0 years, 5 months, 3 days
Research summary
This is an open-label, adaptive, single oral dose study with HTL0014242 in healthy male subjects. The main purpose of the study is to investigate to what extent HTL0014242 binds to receptor sites in different regions of the brain when given at different dose levels, using ionising radiation. The study will also investigate how HTL0014242 is taken up in the blood, metabolised (chemically broken down), distributed through the body, and excreted. A further aim is to look at how safe and well-tolerated HTL0014242 is. No genetic samples will be collected.
The study drug, HTL0014242 is being developed by Heptares Therapeutics Ltd. It is thought that HTL0014242 reduces the release of glutamate by selectively adjusting receptor activity in the brain and hereby reduces irregular and abnormal movement disorders caused by over-excited nerve cells. In addition, HTL0014242 may have anxiety-relieving effects. Glutamate is the most abundant excitatory neurotransmitter (chemical that nerve cells use to send signals to other cells) in the nervous system. Excessive glutamate function is associated with conditions such as Parkinson’s disease, dystonia and amyotrophic lateral sclerosis.
This is not a first-in-human clinical trial as the study drug has been given to humans before. As of the cut-off date of 03 February 2020, about 42 young healthy male and female subjects received single oral doses of HTL0014242 at dose levels ranging between 1 mg and 160 mg in a double-blind rising dose study. Reported adverse events were graded mild or moderate in severity. No serious adverse effects or any findings of clinical concern in vital signs, laboratory tests and ECGs were reported. In this study subjects will receive dose levels demonstrated as safe and well-tolerated.
This study comprises an intensive screening period, an in-house dosing period and a follow-up period. Up to 10 subjects may be included. The study will be performed at a single research centre in collaboration with an imaging site where the brain scans will be performed, both sites are located in London, UK.
REC name
London - Harrow Research Ethics Committee
REC reference
20/LO/0443
Date of REC Opinion
17 May 2020
REC opinion
Further Information Favourable Opinion