pharmatimesDecember 14, 2018
Tag: Sosei , Neurodegeneration , HTL0014242
Sosei has announced that the first healthy subject has been dosed with HTL0014242 - a novel small molecule being tested for its ability to slow neurodegeneration.
The Phase I clinical study marks the start of a new in-house clinical programme at the firm, targeting psychiatric and neurological disorders.
An earlier study has shown that the novel mGlu5 negative allosteric modulator slowed the decline in motor function in late stages of disease progression in a mouse MND model, meaning it reduced neuroinflammation and exerted a neuroprotective effect as evidenced by a reduction in motor neuron loss compared to the control mice.
The Phase I study, which is the first double-blind, randomised, oral single ascending dose study of its kind, is being conducted in the UK and will assess safety, tolerability and pharmacokinetics of HTL0014242 in up to 48 subjects, with preliminary results expected in the second half of 2019.
Dr Malcolm Weir, executive VP and chief R&D officer, said: "The start of this new clinical programme is a result of dedicated research that leveraged all aspects of our unique SBDD approach and our development capabilities.
"HTL0014242 has been designed to be a highly selective and potent blocker of mGlu5 activity and has been optimised to overcome the potential limitations seen with other small molecules targeting this important GPCR."
He continued, "We see great potential with this candidate in a range of indications driven by altered glutamate signalling and intend to take decisions about the ultimate Phase II development pathway following the evaluation of results from this Phase I study."
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