Scientists have re-engineered the blockbuster oncology drug Gleevec to eliminate a serious cardiovascular risk, taking a new approach that could offer a significant improvement for "hundreds" of other drugs as well. Gleevec works by targeting the tyrosine kinases involved in cell reproduction, interfering with a key step in the development of cancer. But the drug also interferes with tyrosine kinases in the ABL family, triggering heart problems in some patients. By adding a methyl group to the drug's structure, it will now only affect cell reproduction. Novartis' drug earned $2.6 billion last year.
The scientist Thomas Force told Chemistry World: "The biggest message of this paper is that a cardiotoxic cause can be identified and steered away from. There are hundreds of agents in development that could benefit from this research."
- see the release on Gleevec
- check out the article from Chemistry World