Following two decades of research on the biology of cancer and in particular of lung cancer, we have now a large number of molecular targets that can be utilized to create specific medicines against these cancers. Non-small cell lung cancer represents numerically the most important solid tumor in Western world, and is poorly affected by current therapies, where surgery represents almost the only curative therapy for about 25% of patients who are resectable at diagnosis. An abundant number of targeted therapies are being investigated in NSCLC. Among them are the metalloproteinase inhibitors, several tyrosine kinase inhibitors and several attempts of gene replacement have also been made. Promising results have so far been obtained with some of these approaches, and the outcome of large randomized studies is awaited. Small cell lung cancer (SCLC) represents about 20% of lung carcinomas, and several of the novel approaches that are being attempted for NSCLC, are also being investigated for SCLC. All these novel therapies open a new era of anticancer treatment that will likely complement the currently available therapies in the near future.