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Research yields new agent for some drug-resistant non-small cell lung cancers
Date:12/23/2009

D, screened the pyrimidine agents in mice with Iressa- and Tarceva-resistant NSCLC tumors driven by EGFR T790M, and found them to be highly effective at impeding tumor growth. Dana-Farber's Michael Eck, MD, PhD, conducted crystallography studies to determine the molecular structure of the pyrimidines, providing a better picture of why they are so potent and how they target EGFR T790M cells so precisely.

"Not only did we determine that the compound WZ4002 could slow tumor growth, we also demonstrated that it is possible to selectively target the drug-resistant mutant EGFR in tumors, with relatively less effect on the normal EGFR in healthy tissues," says Wong.

Much work remains to determine if WZ4002 and its chemical cousins will be effective therapies, the authors caution, but the discovery demonstrates the power of screening specially designed compounds against cancers with certain genetic quirks.

"Obviously these are very early days with respect to the possible use of these compounds in patients we still have much to learn about their possible liabilities," Eck remarks. "But I am optimistic that our approach is correct and that it will lead to an effective treatment for the thousands of non-small cell lung cancer patients worldwide who development resistance to Iressa and Tarceva every year."


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Contact: Bill Schaller
william_schaller@dfci.harvard.edu
617-632-5357
Dana-Farber Cancer Institute
Source:Eurekalert  

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