Lung cancer is one of the leading causes of cancer-related deaths worldwide. Non-small cell lung cancer (NSCLC) accounts for at least 87% of all lung cancers and most cases present at an advanced stage, with metastatic, locally advanced or recurrent disease. With a greater understanding of tumour biology, a number of targeted agents have been investigated for the treatment of advanced NSCLC. These include insulin-like growth factor inhibitors, c-MET inhibitors, poly(adenosine diphosphate-ribose) polymerase inhibitors, histone deacetylase inhibitors, proapoptotic agents, epidermal growth factor receptor inhibitors, vaccines, immunotherapy and hedgehog inhibitors. This article aims to provide an overview of some of the emerging molecules for NSCLC that have demonstrated interesting results in the past couple of years, including descriptions of the molecular pathways of these drugs and their main location of action.