INTRODUCTION: In the last few years, several tyrosine kinase inhibitors (TKIs) 
have been synthesized and become available for preclinical studies and clinical 
trials. This article summarizes recent achievements in the mechanism of action, 
pharmacological properties, and clinical activity and toxicity, as well as the 
emerging role of TKIs in lymphoid malignancies, allergic diseases, and 
autoimmune disorders.
AREAS COVERED: A literature review was conducted of the MEDLINE database PubMed 
for articles in English. Publications from 2000 through January 2012 were 
scrutinized. The search terms used were Bruton's tyrosine kinase (Btk) 
inhibitors, PCI-32765, GDC-0834, LFM-A13, AVL-101, AVL-292, spleen tyrosine 
kinase (Syk) inhibitors, R343, R406, R112, R788, fostamatinib, BAY-61-3606, 
C-61, piceatannol, Lyn, imatinib, nilotinib, bafetinib, dasatinib, GDC-0834, 
PP2, SU6656 in conjunction with lymphoid malignancy, NHL, CLL, autoimmune 
disease, allergic disease, asthma, and rheumatoid arthritis. Conference 
proceedings from the previous 5 years of the American Society of Hematology, 
European Hematology Association, American Society of Clinical Oncology, and 
ACR/ARHP Annual Scientific Meetings were searched manually. Additional relevant 
publications were obtained by reviewing the references from the chosen articles.
EXPERT OPINION: The use of TKIs, especially inhibitors of Btk, Syk, and Lyn, is 
a promising new strategy for targeted treatment of B-cell lymphoid malignancies, 
autoimmune disorders and allergic diseases. However, definitive data from 
ongoing and future clinical trials will aid in better defining the status of 
TKIs in the treatment of these disorders.