Novel Indications for Bruton’s Tyrosine Kinase Inhibitors, beyond Hematological Malignancies

Journal of Clinical Medicine

卷:7

Robert Campbell¹  Geoffrey Chong¹  Eliza A. Hawkes¹ 

[1] Department of Medical Oncology and Clinical Haematology, Olivia Newton-John Cancer Research Institute, Austin Health, Heidelberg, VIC 3084, Australia;

关键词: ibrutinib;    Bruton’s tyrosine kinase;    solid tumors;   

DOI  :  10.3390/jcm7040062

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown