Selection of drug candidate from Orexin-1 programme to treat stress-related addictive disorders and entry into pre-clinical development

Rapid progression demonstrates power of C4XD technology

20 May, 2015 – C4X Discovery Holdings plc ("C4XD" or "the Company"), a leader in rational drug discovery and design, today announced that it has selected a drug candidate from its Orexin-1 programme to enter pre-clinical development prior to the initiation of clinical studies for the treatment of stress-related addictive disorders. This represents a major milestone for C4XD.

Treatment of addictions, such as alcohol, nicotine, cocaine and opiates, is an area of high unmet medical need. This market is worth around $9 billion annually and Orexin-1 represents a key molecular target for new drug development in this area. C4XD's drug candidate is a small-molecule compound discovered using the Company's unique, highly efficient conformational design technology.

Industry-leading selectivity, excellent drug-like properties in pharmacokinetic and pharmacodynamic studies and a good toxicological profile strongly support the progression of the candidate into pre-clinical development. Subject to satisfactory progression, C4XD anticipates this programme should enter clinical development in the second half of 2016.

The rapid progression of this programme demonstrates the potential of conformational design to accelerate the identification and optimisation of small molecule therapeutics. C4XD reached this milestone in less than 50% of the time typically required by industry, which targets 3 – 5 years for such projects. The Company's approach required the synthesis of fewer than 100 compounds and C4XD estimates overall project cost savings to date of up to 90% compared to standard industry approaches.

In addition to this drug candidate, C4XD is progressing additional series of Orexin-1 inhibitors with distinct profiles to enable the development of follow-up compounds for other indications within the field of addiction treatment.
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, helping to accelerate product development. Our conformational insights can be used in conjunction with existing technologies for rational drug design and can make a particularly high impact when protein crystallography is not routinely available, as is the case for GPCRs (G-protein-coupled receptors, such as orexin receptors) and ion channels.
"We are enormously excited by this significant demonstration of the power of our technology. Taking our proprietary drug candidate into preclinical development represents an important milestone," said Piers Morgan, CEO of C4XD. "Our technology has shown a speed and economic efficiency that could revolutionise the drug discovery process. The C4XD platform, centred on conformational design of small molecule therapeutics, is delivering on its promise to develop innovative treatments faster and at a fraction of the cost of conventional approaches."