During the last years, molecular targeted agents generated a small revolution within the various treatment options for malignant tumors. Preclinical data showed that activation of the epidermal growth factor receptor (EGFR)-depending downstream pathways, plays a major role in tumor growth and development. Small molecules, like the tyrosine kinase inhibitors (TKIs), proved their capacity to inhibit the trigger event of this oncogenic activation. Of paramount importance was the fact that this effect has been efficiently translated from preclinical models into clinical practice. Erlotinib is a major representative of this category of drugs. This review will address the current status of the treatment with erlotinib and other TKIs in pancreatic and non-small cell lung cancer (NSCLC), along with the most debated issues regarding the clinical and molecular criteria for patient selection for this kind of targeted therapy.

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