RE: RNS6 Dec 2016 10:03
Dave,
B cells form part of your immune system - they produce antibodies to fight disease. Blood cancers such as leukaemia and lymphoma can be due to mutations which result in abnormal B cells. They basically go bonkers, become overactive and grow uncontrollably.
Bruton’s tyrosine kinase (BTK) is a protein which forms a key part of the B-cell receptor (BCR) pathway - this is the signalling process which triggers the B cell abnormalities. So in simple terms, BTK inhibitors are designed to block or inhibit the pathways and thus the signals that cause the uncontrolled B cell growth. Imbruvica (ibrutinib) is an irreversible BTK inhibitor sold by Abbvie and has been hugely successful but patients become resistant to treatment.
Redx's RXC005 is a reversible BTK inhibitor targeting both natural and mutated BTK. The various graphs on the poster demonstrate preclinical results - that RXC005 does bind to the required BTK targets but not other unintended targets, that it does inhibit the BCR signalling, the length of time it stays active in the body, safety etc.
The most interesting graphs are on the right hand side where you will see two different doses of RXC005 are compared with ibrutinib in mice. You can see that although all 3 were effective, RXC005 at both doses was more effective than ibrutinib in terms of both tumour volume and regrowth delay.