The treatment of chronic myeloid leukemia (CML)   changed  dramatically with the emergence of the ABL tyrosine kinase  inhibitor (TKI) imatinib mesilate. However, primary and secondary  imatinib resistance has been frequently reported, particularly in  patients with advanced-stage disease. To override imatinib resistance,  three second-generation ABL TKIs, i.e., dasatinib, nilotinib and  bosutinib, were developed. Bafetinib (see structure source : Chemblink :INNO-406, NS-187) is a dual  ABL/Lyn inhibitor developed by the team at Kyoto University Hospital in  collaboration with Nippon Shinyaku. 
Bafetinib was 25-55 times more  potent than imatinib in blocking BCR/ABL autophosphorylation, while  otherwise retaining specificity for ABL and Lyn. Bafetinib had  antiproliferative effects against cells bearing wild-type or most  mutated BCR/ABL proteins, except T315I, and also inhibited  BCR/ABL-positive leukemic cell growth in the central nervous system. A  phase I study on bafetinib was completed and the agent was well  tolerated and demonstrated clinical activity across a range of doses.  Responses occurred even in the setting of a heavily pretreated  population, thus making bafetinib a viable option for CML therapy.
Recently  CytRx Corporation, announced that its drug candidate bafetinib (formerly known as INNO-406)  demonstrated statistically significant inhibition of glioblastoma  multiforme cell lines in a preclinical trial. The company believe that bafetinib could be efficacious in several hematological  cancers and  it is  preparing to begin evaluating bafetinib in a  Phase 2 proof-of-concept clinical trial in high-risk B-cell chronic  lymphocytic leukemia  (B-CLL) this quarter, as well as a Phase 2 clinical trial in advanced prostate  cancer next quarter.... 
Ref : http://www.cytrx.com/inno_406.html 
 

 
