Research update

Small molecule leads against IL-17 for inflammation and autoimmune diseases

7 October, 2015 – C4X Discovery Holdings plc (“C4XD”), a leader in rational drug discovery and design, is pleased to provide the following research update on key, highly selective small molecule leads in its programme against Interleukin-17 (IL-17), a critical and high value target in inflammation and autoimmune diseases.

Following the recently announced advances in our diabetes and inflammation programmes, we have shown again that our conformational design technology can significantly outperform conventional drug-discovery approaches when it comes to generating novel agents for challenging disease targets, in this case the member of a protein-protein interaction that has typically proved difficult to target with small-molecule drugs.

IL-17 is implicated in multiple inflammatory and autoimmune diseases and is the subject of numerous clinical studies. Current attempts to target IL-17 are largely based around monoclonal antibodies, which have the necessary size required to inhibit the IL-17/IL-17R engagement. Historically, identifying small molecules that specifically inhibit the IL-17 pathway has been extremely challenging, but our technology has identified small molecules that can selectively block the IL-17/IL-17R interaction with high potency. These are conventional, drug-like compounds, for oral and/or topical use, which would offer benefits over injectable therapies such as IL-17 antibodies. We aim to progress our IL-17 programme towards optimisation and in vivo validation over the coming months.

The first significant market to be targeted by IL-17 antibodies is psoriasis, which is estimated to be worth $6bn per annum. Other significant IL-17 market opportunities include psoriatic arthritis and ankylosing spondylitis, together estimated to be worth a further $6bn per annum.

Outlook

C4XD’s most advanced compound, an oral Orexin-1 antagonist for the treatment of addiction, is in formal pre-clinical safety and toxicity studies prior to initiation of clinical trials. C4XD expects to file for regulatory approval of Phase I studies at the end of 2016.

C4XD’s programmes against Type 2 Diabetes and Inflammation are progressing towards in vivo proof of concept data, and C4XD expects to be in a position to announce further news regarding these programmes before the end of 2015.

Piers Morgan, CEO of C4XD commented: “We continue to expand our proprietary pipeline by using C4XD’s highly effective conformational design technology, and our IL-17 programme is the latest addition. We are rapidly building a portfolio of highly attractive programmes in areas of significant unmet medical need with large target markets. Our technology can be applied broadly to generate drug candidates in a fraction of the time and cost incurred using conventional methods.”