title: 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.
authors.affiliation: Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China.
authors.forename: Jingjing
authors.initials: J
authors.lastname: Wu
authors.affiliation: Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China.
authors.forename: Mingzhi
authors.initials: M
authors.lastname: Zhang
authors.affiliation: Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China. Delong_liu@nymc.edu.
authors.forename: Delong
authors.initials: D
authors.lastname: Liu
mesh_terms: D000077329:Agammaglobulinaemia Tyrosine Kinase; D000818:Animals; D001549:Benzamides / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D019337:Hematologic Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000473:pathology; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011719:Pyrazines / Q000627:therapeutic use*; D016896:Treatment Outcome; D023041:Xenograft Model Antitumor Assays
chemical_list: D001549:Benzamides; D047428:Protein Kinase Inhibitors; D011719:Pyrazines; D011505:Protein-Tyrosine Kinases; D000077329:Agammaglobulinaemia Tyrosine Kinase; C000625949:BTK protein, human; C000604908:acalabrutinib