1. Academic Validation
  2. Ibrutinib and novel BTK inhibitors in clinical development

Ibrutinib and novel BTK inhibitors in clinical development

  • J Hematol Oncol. 2013 Aug 19;6:59. doi: 10.1186/1756-8722-6-59.
Akintunde Akinleye 1 Yamei Chen Nikhil Mukhi Yongping Song Delong Liu
Affiliations

Affiliation

  • 1 Division of Hematology/Oncology, Department of Medicine, New York Medical College, Valhalla, New York 10595, USA.
Abstract

Small molecule inhibitors targeting dysregulated pathways (Ras/Raf/MEK, PI3K/Akt/mTOR, JAK/STAT) have significantly improved clinical outcomes in Cancer patients. Recently Bruton's tyrosine kinase (Btk), a crucial terminal kinase Enzyme in the B-cell antigen receptor (BCR) signaling pathway, has emerged as an attractive target for therapeutic intervention in human malignancies and autoimmune disorders. Ibrutinib, a novel first-in-human BTK-inhibitor, has demonstrated clinical effectiveness and tolerability in early clinical trials and has progressed into phase III trials. However, additional research is necessary to identify the optimal dosing schedule, as well as patients most likely to benefit from Btk inhibition. This review summarizes preclinical and clinical development of ibrutinib and other novel Btk inhibitors (GDC-0834, CGI-560, CGI-1746, HM-71224, CC-292, and ONO-4059, CNX-774, LFM-A13) in the treatment of B-cell malignancies and autoimmune disorders.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-13943
    99.92%, Btk Inhibitor
    Btk