Heptares Orphan Disease Programme awarded grant from the UK Biomedical Catalyst

25-Nov-2014 - United Kingdom

Heptares Therapeutics announced that it has been awarded a £1.5 million grant from the UK Biomedical Catalyst, a funding programme jointly operated by the UK Medical Research Council (MRC) and Innovate UK. The grant, with additional funding from Heptares, will support a three-year research project aimed at developing first-in-class, selective and orally available small molecule GLP-1 receptor antagonists for the treatment of severe hypoglycaemia (low blood glucose) in rare diseases including congenital hyperinsulinism (CHI). These, often inherited, conditions are characterized by inappropriate and unregulated insulin secretion, causing severe hypoglycaemia, and are associated with poor clinical outcomes including long-term nerve and brain damage.
 
GLP-1 is a hormone that regulates insulin production in response to blood glucose levels. The activation of its receptor is an important approach for treating diabetes with several products approved. No GLP-1 receptor antagonists are licensed for treating CHI or other related conditions, however experimental and clinical studies with an intravenous peptide antagonist strongly indicate their prospective effectiveness.
 
The support of the MRC and Innovate UK through this grant will enable Heptares to optimise a series of novel small molecule GLP-1 receptor antagonist compounds identified and developed using its GPCR structure-based development platform. Heptares, in collaboration with the University of Manchester and Great Ormond Street Hospital, London, will then carry out the preclinical development of candidates with the goal of providing novel safe, effective and orally available molecules for clinical studies for CHI with anticipated additional potential in other areas associated with intractable hypoglycaemia; including neonatal hypoglycaemia, hypoglycaemia occurring as a consequence of gastric bypass surgery and insulinoma-associated hypoglycaemia.

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