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12:00 AM
 | 
Jul 19, 2004
 |  BioCentury  |  Product Development

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.

Clinical resistance to Gleevec is a result of point mutations in the ATP-binding domain of the Abl gene that interfere...

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