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

Jingjing Wu, Mingzhi Zhang and Delong Liu _

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Oncotarget. 2017; 8:7201-7207. https://doi.org/10.18632/oncotarget.12786

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Jingjing Wu1, Mingzhi Zhang1 and Delong Liu1

1 Department of Oncology, The first Affiliated Hospital of Zhengzhou University, Zhengzhou, China

Correspondence to:

Delong Liu, email:

Keywords: Bruton tyrosine kinase, ONO/GS-4059, ibrutinib

Received: September 20, 2016 Accepted: October 10, 2016 Published: October 20, 2016


The Bruton tyrosine kinase (BTK) inhibitor, ibrutinib, has been approved for the treatment of chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom’s macroglobulinemia. Acquired resistance to ibrutinib due to BTK C481S mutation has been reported. Mutations in PLCγ2 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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