Company investigating selective orexin-1 receptor inhibitors
Manchester, UK, December 17 2012 – Conformetrix Ltd, a leader in optimising drug discovery and design, is pleased to announce progress in its lead proprietary programme, focused on selective inhibition of the orexin-1 receptor (OX1R). The company has generated a series of potent antagonists, which it plans to evaluate and progress to drug leads. Orexin is a neurotransmitter believed to play a role in a broad range of behavioural conditions, from sleep disorders to addiction.
While there are two receptors for orexin, OXR1 and OXR2, emerging preclinical data supports the use of selective OXR1 antagonists in the treatment of disorders specifically associated with panic, anxiety and compulsive behaviours. Using its proprietary NMR-based technology for structural determination, Conformetrix has built a universal 3D (or "pharmacophore") map of existing OXR1 and OXR2 binders. The company was able to use this to design low nanomolar inhibitors with substantial selectivity for OXR1 over OXR2 in just a few months.
Dr Clive Dix, Chairman of Conformetrix, said, 'Our ability to rapidly design these antagonists highlights the disruptive nature of Conformetrix's technology and its potential to significantly increase the efficiency of the drug discovery process. Orexin represents the first of several therapeutically important targets to which Conformetrix is applying its technology, about which we intend to make similar announcements over the course of 2013.'