Abstract: The clinical mechanisims of micromolecular Tyrosine kinase inhibitors (Erlotinib and Gefitinib), single-dose therapy and current clinical trials of Chemotherapeutic agent are introduced. The relationship between some factors such as chemotherapy, radiotherapy, expressions and mutations of the epidermal growth factor receptors, as well as the patient's characteristics and the clinical efficacy of micromolecular Tyrosine kinase inhibitors is explored, in order to elucidated the development of micromolecular Tyrosine kinase inhibitors in treatment of non-small cell lung cancer.