BTK and Immunology
Bruton tyrosine kinase (BTK) is involved in both our innate and adaptive immune responses and is a critical signaling molecule in immune-mediated diseases.
Designing drug candidates to treat immune-mediated diseases using Tailored Covalency is best illustrated by our clinical-stage BTK inhibitor pipeline.
BTK is present in the signaling pathways of key cells types of the immune system. Our drug candidates inhibit BTK signaling inside these cells resulting in blockade and down-regulation of several cellular activities key to immune-mediated diseases. The inhibition of BTK rapidly blocks inflammatory immune cells and the destructive signaling associated with autoantibodies, and results in swift blockade of inflammation and tissue destruction. Furthermore, BTK inhibition modifies a key driver of many immune-mediated diseases by preventing new autoantibody production.
We believe this optimizing inhibition of BTK leads to a better risk benefit profile for patients with immune-mediated diseases. With tailored BTK inhibition able to address multiple underlying drivers of immune disorders, our drug candidates were designed for targeted, reversible and refined immune modulation compared to other current treatments of these diseases. Our oral drug candidates should avoid the long-term impact of broad, irreversible immunosuppression (like B cell depletion) as well as the inconvenience of injectable therapies and the potential for infusion reactions.

Our portfolio includes three BTK inhibitors that are specifically designed for the types of diseases they are targeted to treat.
B cells are essential to a healthy immune system
Immune-mediated diseases are characterized by a focused attack by the immune system on a particular organ resulting in significant damage to that organ. A key factor in this destructive process is the B cell, one of several connections in the immune system’s complex network. In preclinical models, autoreactive B cells depend on BTK signaling for survival and autoantibody production. In generating autoantibodies, the human immune system attacks its own body, generating antibodies against its own organs. Because BTK is a key part of the body’s natural B cell control mechanism, researchers have sought ways to inhibit BTK’s function in order to control the impact of B cells, autoantibodies and the resultant organ damage.
