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Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor.


ABSTRACT: More and more targeted agents become available for B cell malignancies with increasing precision and potency. The first-in-class Bruton's tyrosine kinase (BTK) inhibitor, ibrutinib, has been in clinical use for the treatment of chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom's macroglobulinemia. More selective BTK inhibitors (ACP-196, ONO/GS-4059, BGB-3111, CC-292) are being explored. Acalabrutinib (ACP-196) is a novel irreversible second-generation BTK inhibitor that was shown to be more potent and selective than ibrutinib. This review summarized the preclinical research and clinical data of acalabrutinib.

SUBMITTER: Wu J 

PROVIDER: S-EPMC4784459 | biostudies-literature | 2016 Mar

REPOSITORIES: biostudies-literature

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Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor.

Wu Jingjing J   Zhang Mingzhi M   Liu Delong D  

Journal of hematology & oncology 20160309


More and more targeted agents become available for B cell malignancies with increasing precision and potency. The first-in-class Bruton's tyrosine kinase (BTK) inhibitor, ibrutinib, has been in clinical use for the treatment of chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom's macroglobulinemia. More selective BTK inhibitors (ACP-196, ONO/GS-4059, BGB-3111, CC-292) are being explored. Acalabrutinib (ACP-196) is a novel irreversible second-generation BTK inhibitor that was sho  ...[more]

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