4.7 Review

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

Journal

JOURNAL OF HEMATOLOGY & ONCOLOGY
Volume 9, Issue -, Pages -

Publisher

BMC
DOI: 10.1186/s13045-016-0250-9

Keywords

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Funding

  1. Henan Provincial Grant for Overseas Research for Young Leaders of Medical Technology [2014041]
  2. Natural Science Foundation of China (NSFC) [81201793]
  3. Division of Hematology and Oncology, New York Medical College
  4. Westchester Medical Center, Valhalla, NY, USA

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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.

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