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Ther Adv Hematol. 2014 Aug;5(4):121-33. doi: 10.1177/2040620714539906.

Bruton's tyrosine kinase inhibitors and their clinical potential in the treatment of B-cell malignancies: focus on ibrutinib.

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Stanford University Medical Center, Stanford, CA, USA.
Stanford University Medical Center, 875 Blake Wilbur Dr, Suite CC-2338, Stanford, CA 94305-5821, USA.


Aberrant signaling of the B-cell receptor pathway has been linked to the development and maintenance of B-cell malignancies. Bruton's tyrosine kinase (BTK), a protein early in this pathway, has emerged as a new therapeutic target in a variety of such malignancies. Ibrutinib, the most clinically advanced small molecule inhibitor of BTK, has demonstrated impressive tolerability and activity in a range of B-cell lymphomas which led to its recent approval for relapsed mantle cell lymphoma and chronic lymphocytic leukemia. This review focuses on the preclinical and clinical development of ibrutinib and discusses its therapeutic potential.


B-cell receptor signaling; Bruton’s tyrosine kinase; chronic lymphocytic leukemia; ibrutinib; mantle cell lymphoma; refractory non-Hodgkin’s lymphoma

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