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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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