Chasing the path of Gleevec resistance

By any definition, Gleevec imatinib from Novartis AG has been a success as a treatment for chronic myeloid leukemia. However, while the drug has shown minimal toxicity, increased resistance is being encountered. Bristol-Myers Squibb Co. is developing a next-generation version that has been active in Gleevec-resistant models of CML.

Gleevec, which Novartis (NVS; SWX:NOVN, Basel, Switzerland) markets as Glivec in Europe, is a small molecule inhibitor of the Bcr-Abl tyrosine kinase, a mutated protein that is permanently activated in CML. The drug prevents overexpression of Abl by attaching to the ATP-binding site, thus inactivating the protein...