Abstract: Abstract　At present, lung cancer is one of the malignant tumors with the highest morbidity and mortality rates. In China, lung cancer ranks first in terms of mortality from malignant tumors. In addition, the incidence of non-small-cell lung cancer (NSCLC) is over 80% among all lung cancers. Most NSCLC cases are diagnosed in the advanced stage, so medical treatment remains the primary therapy for NSCLC. Over the past 10 years, however, chemotherapy, as a first-line therapy, has failed to progress in terms of curative effects against NSCLC. Since the 1990s, with intensified studies on molecular-targeted therapy for lung cancer, where epidermal growth factor receptor (EGFR) and tumor angiogenesis became therapeutic targets, some drugs have shown satisfactory clinical effects in the treatment of advanced NSCLC. In the 21st century, research on molecular-targeted therapy has greatly developed, and studies on several novel targeted therapies have provided new modes of treatment for NSCLC. In the present article, the progress in targeted therapy for NSCLC is introduced based on three aspects: drugs that target EGFR, tumor angiogenesis, and multi-target antitumor drugs.