Lung Cancer and Gefitinib Lung cancer statistics in

Lung Cancer and Gefitinib · Lung cancer statistics in the United States · Estimated cases in 2004: ~174, 000 · Estimated deaths in 2004: ~160, 000 · Gefitinib (Iressa ™) · Developed by Astra. Zeneca · Used to treat Nonsmall Cell Lung Cancer (NSCLC) · Accounts for 85% of all lung cancers · 90% of patients did not respond to drug · But, 10% responded incredibly well © 2005 Prentice Hall Inc. / A Pearson Education Company / Upper Saddle River, New Jersey 07458

EGFR and Gefitinib Efficacy · Mutated protein kinases implicated in cancer · Gefitinib targets Epidermal Growth Factor Receptor (EGFR), a kinase · Gefitinib only effective in patients with mutated EGFR From Figure 3 A in Paez, J. G. et al. (2004) “EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy” Science 304: 1497 -1500. © 2005 Prentice Hall Inc. / A Pearson Education Company / Upper Saddle River, New Jersey 07458

Mutations Accounting for Positive Drug Response · Mutations indicative of good gefitinib response EGFR kinase domain · Segregated in areas implicated in autoregulation of kinases · P-loop · Activation loop From Figure 2 in Paez, J. G. et al. (2004) “EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy” Science 304: 1497 -1500. © 2005 Prentice Hall Inc. / A Pearson Education Company / Upper Saddle River, New Jersey 07458