Manchester and London, UK, 4 September, 2014 – C4X Discovery (C4XD), a leader in rational drug discovery and design, today announced positive initial data from its Orexin-1 programme to treat stress-related addictive disorders, and the filing of a related patent.
C4XD has the only technology in the world that can generate accurate, experimentally-derived dynamic solution 3D structures of drug molecules in just a matter of days. It can be used in conjunction with existing technologies for structure-based drug design, and can make a particularly high impact when protein crystallography is not routinely available, as is the case for GPCRs and ion channels.
C4XD used its conformational design ability to analyse the shapes and thereby identify separate features relating to activity against each of Orexin-1 and Orexin-2 receptors. Using these insights, the C4XD medicinal chemistry team was able to design multiple series of interest, including several molecules showing more than 1,000x selectivity for Orexin-1 over Orexin-2 receptors. In pre-clinical models C4XD has generated data showing effective reduction in stress-related behaviours whilst showing a beneficially differentiated profile against other behavioural endpoints compared to third party Orexin-1 receptor selective compounds.
Piers Morgan, CEO, said "This excellent result demonstrates not only C4XD's ability to accurately measure and describe the shapes of small-molecule drugs, but to then apply the principles of conformational design to solve problems which have until now resisted the pharma industry." Dr Charles Blundell, CSO added "The newly filed patent clearly demonstrates C4XD's ability to rapidly establish secure and novel IP positions for challenging programmes in highly competitive areas."