C4X Discovery Holdings PLC MALT-1 Inhibitor Programme Update (2493B)

TIDMC4XD

RNS Number : 2493B

C4X Discovery Holdings PLC

01 June 2023

C4X Discovery Holdings plc

("C4XD", "C4X Discovery" or the "Company")

MALT-1 Inhibitor Programme Update

Profiling of C4XD lead series shows no UGT1A1 liability at clinically meaningful doses

C4XD series potentially differentiated for safety profile

1 June 2023 - C4X Discovery Holdings plc (AIM: C4XD), a pioneering Drug Discovery company, provides an update on its MALT-1 inhibitor programme for cancer. C4XD has successfully completed a preclincial study demonstrating its MALT-1 lead compounds are free of UGT1A1(1) liability shown by competitor chemistries. The C4XD MALT-1 inhibitor programme is continuing to identify a shortlist of pre-clinical candidates for further development and a partnering programme has been initiated.

MALT-1 is one of the key regulators of B-cell receptor (BCR) and T-cell receptor (TCR) signalling. Mutations that lead to activation of MALT-1 are associated with aggressive forms of non-Hodgkin B-cell lymphoma, and inhibition of MALT-1 has potential therapeutic applicability as a mono therapy for MALT-1-driven cancers and in combination with BTK inhibitors across multiple haematological indications, as well as broader potential in solid tumours and inflammation.

Bilirubin is a toxic pigment produced naturally in the body as a result of the breakdown of red blood cells and is normally cleared in the bile by the enzyme UGT1A1. Excessive bilirubin (hyperbilirubinemia) has been observed clinically in patients treated with a range of tyrosine kinase inhibitors, including BTK inhibitors, and has been associated with inhibition of UGT1A1 by these drugs. BTK/MALT-1 combination therapies represent a desirable therapeutic dosing regimen and little or no activity against UGT1A1 by a MALT-1 inhibitor is essential to reduce UGT1A1 inhibition burden.

Dr Nick Ray, CSO of C4XD, said: " Yet again, our Conformetrix technology has delivered molecules that have the potential to be best-in-class. Building on promising anti-cancer activity in a preclinical xenograft study , we have now favourably observed little or no inhibition of UGT1A1 at clinically meaningful concentrations, whereas representative examples from other clinical and pre-clinical programmes showed significant UGT1A1 activities. We believe this is due to the degree of chemical differentiation in the C4XD series compared to competitors and we are confident of identifying a pre-clinical candidate shortlist with a desirable safety profile in the near future."

   1.   UDP glucuronosyltransferase 1 family, polypeptide A1 ( UGT1A1) 

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Contacts

 
 C4X Discovery Holdings 
 Mo Noonan, Communications                    [phone] 
 
 Panmure Gordon (UK) Limited (NOMAD and 
  Broker) 
 Freddy Crossley, Emma Earl (Corporate 
  Finance)                                    [phone] 
 Rupert Dearden (Corporate Broking) 
 
 C4X Discovery Media - Consilium Strategic 
  Communications 
 Mary-Jane Elliott, Chris Gardner, Matthew 
  Neal                                        [phone] 
 

Notes to Editors:

About C4X Discovery

C4X Discovery ("C4XD") is a pioneering Drug Discovery company, combining scientific expertise with cutting-edge Drug Discovery technologies to efficiently deliver world--leading medicines. We have a highly valuable and differentiated approach to Drug Discovery through our enhanced candidate molecule design and patient stratification capabilities, generating small molecule drug candidates across multiple disease areas focused on immuno-inflammation. Our commercially attractive portfolio ranges from early-stage target opportunities to late-stage Drug Discovery programmes and we have three commercially partnered programmes with one candidate in clinical development.

For more information visit us at www.c4xdiscovery.com or follow us on twitter @C4XDiscovery.

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June 01, 2023 02:00 ET (06:00 GMT)