title: Second-generation inhibitors of Bruton tyrosine kinase.
abstract: Bruton tyrosine kinase (BTK) is a critical effector molecule for B cell development and plays a major role in lymphoma genesis. Ibrutinib is the first-generation BTK inhibitor. Ibrutinib has off-target effects on EGFR, ITK, and Tec family kinases, which explains the untoward effects of ibrutinib. Resistance to ibrutinib was also reported. The C481S mutation in the BTK kinase domain was reported to be a major mechanism of resistance to ibrutinib. This review summarizes the clinical development of novel BTK inhibitors, ACP-196 (acalabrutinib), ONO/GS-4059, and BGB-3111.
authors: Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China.
authors: Jingjing
authors: J
authors: Wu
authors: Weinberg College of Arts and Sciences, Northwestern University, Evanston, IL, 60208, USA.
authors: Christina
authors: C
authors: Liu
authors: SUNY Stony Brook University, Stony Brook, NY, 11794, USA.
authors: Stella T
authors: ST
authors: Tsui
authors: Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China. DELONG_LIU@NYMC.EDU.
authors: Delong
authors: D
authors: Liu
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives; D000077329:Agammaglobulinaemia Tyrosine Kinase; D001549:Benzamides; D019008:Drug Resistance, Neoplasm / Q000235:genetics; D006801:Humans; D007093:Imidazoles; D015451:Leukemia, Lymphocytic, Chronic, B-Cell / Q000188:drug therapy; D010880:Piperidines; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000502:physiology; D011719:Pyrazines; D011720:Pyrazoles; D011743:Pyrimidines
chemical_list: D001549:Benzamides; D007093:Imidazoles; D010880:Piperidines; D047428:Protein Kinase Inhibitors; D011719:Pyrazines; D011720:Pyrazoles; D011743:Pyrimidines; C551803:ibrutinib; D011505:Protein-Tyrosine Kinases; D000077329:Agammaglobulinaemia Tyrosine Kinase; C000625949:BTK protein, human; C000604908:acalabrutinib; D000225:Adenine; C000608238:tirabrutinib