REVIEW Ibrutinib is an experimental anticancer drug recently approved for mantle cell lymphoma. It is a selective and covalent inhibitor of the enzyme Bruton''s tyrosine kinase (BTK). Ibrutinib is currently under development for other B-cell malignancies including chronic lymphocytic leukemia, diffuse large B-cell lymphoma, and multiple myeloma. It was originally synthesized as one of a series of small molecules that inactivate BTK through covalent binding to cysteine-481 near the ATP binding domain of BTK, by means of a Michael acceptor for binding to the target cysteine.
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