An orally available inhibitor of Bruton tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, BGB-3111 selectively binds to and inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B-cells that overexpress BTK. BTK, a member of the TEC family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in the development, activation, signaling, proliferation and survival of B-lymphocytes. Check for active clinical trials using this agent. (NCI Thesaurus)
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