At present, cancer research has entered the cellular and molecular level, and the so-called molecular targeted therapy is to target a key molecule in the process of cancer development, so as to develop drugs targeting this molecule to achieve the purpose of anti-tumor. Therefore, molecular targeted therapy has the characteristics of high specificity and low damage to normal tissues, and molecular targeted therapy is currently under development and research. Among them, Gefitinib, Troche and Kemena have better efficacy for advanced non-small cell lung cancer with EGFR mutation, with remission rate of 70% or more, and currently only ERSA and Kemena are approved by the Chinese FDA for first-line treatment of advanced non-small cell lung cancer with EGFR mutation. It is more suitable for Chinese patients, with less side effects, especially rash and diarrhea, better price, and more convenient drug delivery. Some clinical trials have demonstrated the value of these drugs in the treatment of lung cancer, and more clinical trials are underway. The current studies such as IPASS and icogen fully illustrate the important role of molecularly targeted drugs in the treatment of patients with mutated non-small cell lung cancer, and because of the creation of molecularly targeted drugs, the survival of patients can be extended to 3 years or more.