What is the mechanism of action of ibrutinib?
Ibrutinib is a kinase inhibitor used to treat adult patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL). For adult patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) with 17p deletion. For use in adult patients with Waldenströ macroglobulinemia (WM). For use in adult and pediatric patients 1 year of age and older with chronic graft-versus-host disease (cGVHD) after failure of one or more systemic therapies.
Ibrutinib is a small molecule inhibitor of Bruton tyrosine kinase (BTK). Ibrutinibforms a covalent bond with the cysteine u200bu200bresidue in the BTK active site, resulting in the inhibition of BTK enzyme activity. BTKis a signaling molecule for the Bcell antigen receptor(BCR) and cytokine receptor pathways. BTK's role in signaling through B cell surface receptors results in activation of pathways necessary for B cell trafficking, chemotaxis, and adhesion. Non-clinical studies have shown that ibrutinib inhibits malignant cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.
Ibrutinib also eliminates Btk
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