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Review
. 2013 Nov;163(4):436-43.
doi: 10.1111/bjh.12573. Epub 2013 Sep 24.

Bruton tyrosine kinase inhibitors: a promising novel targeted treatment for B cell lymphomas

Amin Aalipour  1 , Ranjana H Advani
Affiliations
Review

Bruton tyrosine kinase inhibitors: a promising novel targeted treatment for B cell lymphomas

Amin Aalipour et al. Br J Haematol. 2013 Nov.

Abstract

Constitutive or aberrant signalling of the B cell receptor signalling cascade has been implicated in the propagation and maintenance of a variety of B cell malignancies. Small molecule inhibitors of Bruton tyrosine kinase (BTK), a protein early in this cascade and specifically expressed in B cells, have emerged as a new class of targeted agents. There are several BTK inhibitors, including ONO-WG-307, LFM-A13, dasatinib, CC-292, and PCI-32765 (ibrutinib), in preclinical and/or clinical development of which ibrutinib is currently in phase III trials. Recent clinical data suggest significant activity of ibrutinib as a first in class oral inhibitor of BTK. This review provides an overview of ongoing clinical studies of BTK inhibitors.

Keywords: B cell receptor signalling; Bruton tyrosine kinase; CC-292; ibrutinib; refractory non-Hodgkin lymphoma.

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Conflict of interest statement

Disclosures

Amin Aalipour declares no conflict of interests. Ranjana H. Advani has received research funding from Pharmacyclics, Inc. and Janssen Pharmaceuticals, Inc.

Figures

Fig 1
Fig 1
The BCR signalling cascade. Antigen binding to the B cell receptor initiates kinase-mediated signal transduction resulting in activation of secondary messengers and, ultimately, transcription factors that regulate cell fate.
See this image and copyright information in PMC

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References

    1. Advani RH, Buggy JJ, Sharman JP, Smith SM, Boyd TE, Grant B, Kolibaba KS, Furman RR, Rodriguez S, Chang BY, Sukbuntherng J, Izumi R, Hamdy A, Hedrick E, Fowler NH. Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies. Journal of Clinical Oncology. 2013;31:88–94. - PMC - PubMed
    1. Amrein PC, Attar EC, Takvorian T, Hochberg EP, Ballen KK, Leahy KM, Fisher DC, LaCasce AS, Jacobsen ED, Armand P, Hasserjian RP, Werner L, Neuberg D, Brown JR. Phase II study of dasatinib in relapsed or refractory chronic lymphocytic leukemia. Clinical Cancer Research. 2011;17:2977–2986. - PMC - PubMed
    1. Brown JR. Ibrutinib (PCI-32765), the first BTK (Bruton’s Tyrosine Kinase) inhibitor in clinical trials. Current Hematologic Malignancy Reports. 2012;8:1–6. - PMC - PubMed
    1. Brown JR. Ibrutinib in chronic lymphocytic leukemia and B cell malignancies. Leukemia and Lymphoma. 2013 doi: 10.3109/10428194.2013.803226. - DOI - PubMed
    1. Brown JR, Sharman JP, Harb WA, Kelly KR, Schreeder MT, Sweetenham JW, Barr PM, Foran JM, Gabrilove JL, Kipps TJ, Ma S, O’Brien SM, Evans E, Lounsbury H, Silver BA, Singh J, Stiede K, Westlin W, Witowski S, Mahadevan D. Phase Ib trial of AVL-292, a covalent inhibitor of Bruton’s tyrosine kinase (Btk), in chronic lymphocytic leukemia (CLL) and B-non-Hodgkin lymphoma (B-NHL)[abstract] Journal of Clinical Oncology (ASCO meeting abstracts) 2012a;30:8032.

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