[HTML][HTML] Bruton tyrosine kinase inhibitor ONO/GS-4059: from bench to bedside

J Wu, M Zhang, D Liu - Oncotarget, 2017 - ncbi.nlm.nih.gov
J Wu, M Zhang, D Liu
Oncotarget, 2017ncbi.nlm.nih.gov
The Bruton tyrosine kinase (BTK) inhibitor, ibrutinib, has been approved for the treatment of
chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstroms
macroglobulinemia. Acquired resistance to ibrutinib due to BTK C481S mutation has been
reported. Mutations in PLC? 2 can also mediate resistance to ibrutinib. Untoward effects due
to off-target effects are also disadvantages of ibrutinib. More selective and potent BTK
inhibitors (ACP-196, ONO/GS-4059, BGB-3111, CC-292) are being investigated. This review …
Abstract
The Bruton tyrosine kinase (BTK) inhibitor, ibrutinib, has been approved for the treatment of chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstroms macroglobulinemia. Acquired resistance to ibrutinib due to BTK C481S mutation has been reported. Mutations in PLC? 2 can also mediate resistance to ibrutinib. Untoward effects due to off-target effects are also disadvantages of ibrutinib. More selective and potent BTK inhibitors (ACP-196, ONO/GS-4059, BGB-3111, CC-292) are being investigated. This review summarized the preclinical research and clinical data of ONO/GS-4059.
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