Description
PCI-32765 is an irreversible inhibitor of Bruton’s tyrosine kinase (BTK), an enzyme that plays a significant role in B-cell receptor signaling and B-cell malignancies and autoimmune diseases such as x-linked agammaglobulinemia, chronic lymphocytic leukemia, and non-Hodgkin’s lymphoma. This compound displays anticancer chemotherapeutic, anti-metastatic, immunomodulatory, and anti-fibrotic activities. PCI-32765’s inhibition of BTK prevents IgE-mediated activation of basophils, inhibits signaling from macrophages and mast cells, and inhibits cell migration and survival in cellular and animal models of chronic lymphocytic leukemia. Additionally, PCI-32765 inhibits IL-2-inducible kinase and suppresses the development of fibrosis in pancreatic adenocarcinoma models.