title: Ibrutinib (PCI-32765) in chronic lymphocytic leukemia.
abstract: B-cell receptor (BCR) signaling is essential for chronic lymphocytic leukemia (CLL) cell survival. Many kinases in the BCR signaling pathway are being studied as potential therapeutic targets. Ibrutinib (PCI-32765) is a novel first-in-class selective inhibitor of Bruton tyrosine kinase. Preclinical evidence suggests that ibrutinib inhibits CLL cell survival and proliferation and affects CLL cell migration and homing. Early clinical data in patients with CLL and non-Hodgkin lymphoma is encouraging. It is likely that ibrutinib and other drugs targeting the BCR pathway will become an integral component of CLL therapy.
authors.affiliation: Department of Leukemia, MD Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA.
authors.forename: Nitin
authors.initials: N
authors.lastname: Jain
authors.forename: Susan
authors.initials: S
authors.lastname: O'Brien
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives; D000077329:Agammaglobulinaemia Tyrosine Kinase; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D006801:Humans; D015451:Leukemia, Lymphocytic, Chronic, B-Cell / Q000188:drug therapy*; D010880:Piperidines; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage / Q000627:therapeutic use*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D011720:Pyrazoles / Q000008:administration & dosage / Q000627:therapeutic use*; D011743:Pyrimidines / Q000008:administration & dosage / Q000627:therapeutic use*; D016896:Treatment Outcome
chemical_list: D000970:Antineoplastic Agents; D010880:Piperidines; D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011743:Pyrimidines; C551803:ibrutinib; D011505:Protein-Tyrosine Kinases; D000077329:Agammaglobulinaemia Tyrosine Kinase; D000225:Adenine
keywords: B-cell receptor inhibitor; Bruton tyrosine kinase inhibitor; Chronic lymphocytic leukemia; Ibrutinib; PCI-32765
references.citation: J Clin Invest. 2005 Feb;115(2):369-78
references.pmid: 15650771
references.citation: Blood. 2011 Jan 13;117(2):563-74
references.pmid: 20940416
references.citation: Lancet Oncol. 2011 Dec;12(13):1204-13
references.pmid: 21992852
references.citation: N Engl J Med. 2000 Dec 28;343(26):1910-6
references.pmid: 11136261
references.citation: Blood. 2004 Jun 15;103(12):4389-95
references.pmid: 14962897
references.citation: ChemMedChem. 2007 Jan;2(1):58-61
references.pmid: 17154430
references.citation: Blood. 2012 Aug 9;120(6):1175-84
references.pmid: 22715122
references.citation: Blood. 2008 Jun 1;111(11):5291-7
references.pmid: 18334676
references.citation: Annu Rev Immunol. 2003;21:841-94
references.pmid: 12615894
references.citation: Blood. 2012 Feb 2;119(5):1182-9
references.pmid: 22180443
references.citation: J Immunol. 1994 Jan 15;152(2):557-65
references.pmid: 8283037
references.citation: J Exp Med. 2001 Dec 3;194(11):1639-47
references.pmid: 11733578
references.citation: Blood. 2011 Sep 29;118(13):3489-98
references.pmid: 21725050
references.citation: Leukemia. 2012 Jul;26(7):1576-83
references.pmid: 22362000
references.citation: J Clin Oncol. 2012 Sep 10;30(26):3209-16
references.pmid: 22869884
references.citation: Blood. 2012 Dec 6;120(24):4684-91
references.pmid: 22875912
references.citation: Blood. 2011 Sep 29;118(13):3603-12
references.pmid: 21803855
references.citation: Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80
references.pmid: 20615965
references.citation: Blood. 2011 Jun 16;117(24):6450-8
references.pmid: 21498674
references.citation: Immunol Rev. 2000 Jun;175:120-7
references.pmid: 10933597
references.citation: Blood. 2010 Jun 3;115(22):4497-506
references.pmid: 20335218
references.citation: J Clin Oncol. 2011 Feb 10;29(5):544-50
references.pmid: 21220603
references.citation: Blood. 2011 Jan 13;117(2):591-4
references.pmid: 20959606
references.citation: Nature. 2010 Jan 7;463(7277):88-92
references.pmid: 20054396
references.citation: Eur J Immunol. 1994 Dec;24(12):3100-5
references.pmid: 7805739
references.citation: Cancer. 2003 Dec 15;98(12):2657-63
references.pmid: 14669286
references.citation: Hematology Am Soc Hematol Educ Program. 2011;2011:96-103
references.pmid: 22160019
references.citation: Immunol Res. 2001;23(2-3):147-56
references.pmid: 11444380
references.citation: Blood. 2010 Sep 23;116(12):2078-88
references.pmid: 20522708
references.citation: Blood. 2011 Jun 9;117(23):6287-96
references.pmid: 21422473
references.citation: Blood. 2002 Dec 15;100(13):4609-14
references.pmid: 12393534
references.citation: J Clin Oncol. 2011 Sep 10;29(26):3559-66
references.pmid: 21844497
references.citation: Blood. 2008 Aug 15;112(4):975-80
references.pmid: 18411418
references.citation: Annu Rev Immunol. 2009;27:199-227
references.pmid: 19302039
references.citation: Blood. 2010 Apr 1;115(13):2578-85
references.pmid: 19965662