A safer imatinib for treating GIST

Researchers from Rice University, the University of Texas M.D. Anderson Cancer Center and colleagues reported in the Journal of Clinical Oncology that a reengineered variant of Gleevec imatinib demonstrated decreased cardiotoxicity compared to the marketed drug in mouse models of gastrointestinal stromal tumors (GIST). The methylated variant, designated WBZ_4, showed substantially higher inhibition of the GIST target c-kit kinase than did imatinib. WBZ_4 also had reduced inhibition of Bcr-Abl tyrosine kinase and increased inhibition of c-jun N-terminal kinase (JNK) compared with imatinib, with a consequent reduction in cardiotoxicity. ...