Lung cancer remains the leading cause of cancer-related mortality in the western world. Non-small-cell lung cancer (NSCLC) accounts for approximately 80% of these thoracic malignancies, with 1.2 million new cases diagnosed worldwide each year. The vast majority of NSCLC patients present with disease that is beyond the scope of surgical cure and are, therefore, candidates for palliative chemotherapy, which has been the subject of intensive investigation in recent years. Although platinum-based therapies modestly improve survival and palliate some tumour-related symptoms in patients with locally advanced or metastatic NSCLC, at times the chemotherapy-related side effects outweigh the benefits. Consequently, the identification of new regimens that maintain the same level of efficacy as platinum-based combinations but offer a better toxicity profile is a key goal in this important area of medicine.