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

2016; BioMed Central; Volume: 9; Issue: 1 Linguagem: Inglês

10.1186/s13045-016-0250-9

1756-8722

Jingjing Wu, Mingzhi Zhang, Delong Liu,

Immunodeficiency and Autoimmune Disorders

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.