Novel Indications for Bruton’s Tyrosine Kinase Inhibitors, beyond Hematological Malignancies
1
Department of Medical Oncology and Clinical Haematology, Olivia Newton-John Cancer Research Institute, Austin Health, Heidelberg, VIC 3084, Australia
2
Bendigo Cancer Centre, Bendigo Health, Bendigo, VIC 3084, Australia
3
Department of Oncology, Northern Hospital, Melbourne, VIC 3084, Australia
4
Department of Medical Oncology, Ballarat Health Services, Ballarat, VIC 3084, Australia
5
Department of Medical Oncology, Eastern Health, Melbourne, VIC 3084, Australia
6
Eastern Health, Monash University Clinical School, Melbourne, VIC 3084, Australia
*
Author to whom correspondence should be addressed.
J. Clin. Med. 2018, 7(4), 62; https://doi.org/10.3390/jcm7040062
Received: 31 December 2017 / Revised: 18 February 2018 / Accepted: 6 March 2018 / Published: 21 March 2018
(This article belongs to the Section Hematology)
Bruton’s tyrosine kinase (BTK) is a critical terminal enzyme in the B-cell antigen receptor (BCR) pathway. BTK activation has been implicated in the pathogenesis of certain B-cell malignancies. Targeting this pathway has emerged as a novel target in B-cell malignancies, of which ibrutinib is the first-in-class agent. A few other BTK inhibitors (BTKi) are also under development (e.g., acalabrutinib). While the predominant action of BTKi is the blockade of B-cell receptor pathway within malignant B-cells, increasing the knowledge of off-target effects as well as a potential role for B-cells in proliferation of solid malignancies is expanding the indication of BTKi into non-hematological malignancies. In addition to the expansion of the role of BTKi monotherapy, combination therapy strategies utilizing ibrutinib with established regimens and combination with modern immunotherapy compounds are being explored.
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Keywords:
ibrutinib; Bruton’s tyrosine kinase; solid tumors
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MDPI and ACS Style
Campbell, R.; Chong, G.; Hawkes, E.A. Novel Indications for Bruton’s Tyrosine Kinase Inhibitors, beyond Hematological Malignancies. J. Clin. Med. 2018, 7, 62.
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