Ibrutinib (PCI-32765) is an irreversible BTK (Bruton’s tyrosine kinase) kinase inhibitor that has been extensively used as a tool compound to validate the role of BTK kinase in B cell related malignances. Ibrutinib has been shown in preclinical studies to inhibit the proliferation of diffuse large B-cell lymphoma cells, mantle cell lymphoma cells, chronic lymphocytic leukemia cells and multiple myeloma cells by blocking BTK kinase activity; ibrutinib was recently approved for the clinical application on mantle cell lymphoma and chronic lymphocytic leukemia cells. Ibrutinib has also exhibited anti-inflammatory effects in preclinical models. Recently, it has been reported that ibrutinib is also effective against epidermal growth factor receptor mutant-positive non-small cell lung cancers through inhibition of epidermal growth factor receptor kinase activities. In addition, there is evidence showing that BTK is also an important target for Acute Myeloid Leukemia (AML).

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