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

• Published in: Journal of hematology and oncology Vol. 9; no. 21; p. 21
• Main Authors: Wu, Jingjing, Zhang, Mingzhi, Liu, Delong
• Format: Journal Article
• Language: English
• Published: England BioMed Central Ltd 09.03.2016; BioMed Central; BMC
• Subjects: Agammaglobulinaemia Tyrosine Kinase; Animals; Benzamides - therapeutic use; Cancer; Care and treatment; Chemotherapy; Clinical Trials as Topic; Health aspects; Hematologic Neoplasms - drug therapy; Hematologic Neoplasms - enzymology; Hematologic Neoplasms - pathology; Humans; Influence; Lymphocytic leukemia; Monoclonal antibodies; Protein Kinase Inhibitors - therapeutic use; Protein-Tyrosine Kinases - antagonists & inhibitors; Protein-Tyrosine Kinases - metabolism; Pyrazines - therapeutic use; Review; Treatment Outcome; Tyrosine; Xenograft Model Antitumor Assays
• ISSN: 1756-8722; 1756-8722
• DOI: 10.1186/s13045-016-0250-9

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.