An increased understanding of the biology of lung cancer has identified biological targets for rationally designed novel therapies. Most of these targets are components of signalling pathways or metabolic processes. EGFR-tyrosinkinase inhibitors have become standard in second- and thirdline therapy of NSCLC, the anti-VEGF-antibody Avastin combined with first-line chemotherapy showed a significant survival benefit over chemotherapy alone. There are ongoing studies with targeted therapies in all stages of lung cancer. Major advances of these new drugs are their low toxicity and, in part, the oral application.