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Heptares Initiates Clinical Study With First Selective Muscarinic M1 Receptor Agonist for Improving Cognition in Patients With Alzheimer's Disease
Date:12/9/2013

LONDON and BOSTON, December 9, 2013 /PRNewswire/ --

First Human Trial of Novel Small Molecule Drug Derived From Heptares GPCR-Focused Structure-Based Drug Design Platform

Heptares Therapeutics, the leading GPCR structure-guided drug discovery and development company, announces that it has initiated a Phase 1 clinical study of HTL9936, the first fully selective muscarinic M1 receptor agonist to enter clinical development. HTL9936 is an orally available, small molecule drug candidate discovered using the Heptares GPCR structure-based drug design (SBDD) platform. Heptares plans to develop HTL9936 as a novel treatment for improving cognitive function (memory and thinking abilities) in patients with Alzheimer's disease and other diseases associated with dementia and cognitive impairment.

"We are excited to initiate clinical development of HTL9936, a first-in-class agent with the potential to become an important new medicine for improving cognitive function in patients with Alzheimer's disease and other potential indications including schizophrenia and Lewy body dementia," said Malcolm Weir, CEO of Heptares. "In addition, the initiation of this clinical trial with HTL9936 marks an important milestone for Heptares, as we evolve into a clinical-stage business with a rich portfolio of novel GPCR-targeted agents advancing through Phase 1 and 2a clinical trials in the near-term."

M1 receptor agonism is a well-validated mechanism of action for treating cognitive impairment and a valuable pharmacological profile that the pharmaceutical industry has endeavored to create for decades. The principal challenge has been to engineer selective compounds that activate the M1 receptor subtype without also activating the M2 or M3 receptors, which are associated with undesirable side effects. All previous compounds have been d
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SOURCE Heptares Therapeutics
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