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Ibrutinib is a recent Food and Drug Administration-approved drug for the treatment of lymphoid malignancies: mantle cell lymphoma and chronic lymphocytic leukemia (CLL). It is a Bruton's tyrosine kinase (BTK) inhibitor which increases the apoptotic susceptibility of malignant lymphocytes and also causes tissue redistribution of lymphocytes. Strong biological rationale makes BTK an ideal target for therapy of CLL and other B-cell malignancies. We are presenting a comprehensive review of this promising drug, highlighting its metabolism, safety profile, trials, and approved uses.
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