Second-generation inhibitors of Bruton tyrosine kinase. Review uri icon

Overview

abstract

  • Bruton tyrosine kinase (BTK) is a critical effector molecule for B cell development and plays a major role in lymphoma genesis. Ibrutinib is the first-generation BTK inhibitor. Ibrutinib has off-target effects on EGFR, ITK, and Tec family kinases, which explains the untoward effects of ibrutinib. Resistance to ibrutinib was also reported. The C481S mutation in the BTK kinase domain was reported to be a major mechanism of resistance to ibrutinib. This review summarizes the clinical development of novel BTK inhibitors, ACP-196 (acalabrutinib), ONO/GS-4059, and BGB-3111.

publication date

  • September 2, 2016

Research

keywords

  • Protein Kinase Inhibitors
  • Protein-Tyrosine Kinases

Identity

PubMed Central ID

  • PMC5010774

Scopus Document Identifier

  • 84984920989

Digital Object Identifier (DOI)

  • 10.1186/s13045-016-0313-y

PubMed ID

  • 27590878

Additional Document Info

volume

  • 9

issue

  • 1