Precision kinase targeting to reduce T-cell mediated inflammation.
PKCθ Inhibitor
Protein Kinase C Theta (PKCϴ), a member of the protein kinase C family of kinases, is primarily expressed in T-cells, and plays a dual role in T-cell biology. Activation of PKCϴ leads to effector T-cell activation, proliferation, and production of IL-2, while the inhibition of PKCϴ leads to an increase in both the numbers and functionality of regulatory T-cells that dampen immune response. It has been shown that mice lacking functional PKCϴ are highly resistant to inflammatory diseases. Genetic variants within the gene for PKCϴ have been associated with many inflammatory diseases.
Restoring the proper balance between effector and regulatory T-cell activity is one potential path to a potent and durable resolution of chronic inflammation.
More than 100 autoimmune diseases are associated with T-cell pathology.
PKCϴ inhibition is currently being evaluated in several areas of high unmet need:
- Psoriasis: Psoriasis is both common and chronic, affecting more than 7.5 million adults in the United States, without a known cure. An overactive immune system is the culprit that drives itching, burning, and disfiguring manifestations on the skin. Current therapies are effective for about 50 percent of patients, and despite advances in psoriasis treatment, there remains a need for faster, more effective, and longer-lasting treatments. Growing evidence suggests that dysregulation of T-cell activity in the skin plays a substantial role in the development of psoriasis.
- Inflammatory Bowel Disease: Moderate-to-severe inflammatory bowel disease (IBD) disrupts the lives of millions, in the form of either Crohn’s disease or ulcerative colitis, manifesting as chronic inflammation of the gastrointestinal tract. Current therapies may induce periods of remission, but there is no cure, and a clear need for safe and effective oral medications with good bioavailability.