Lung cancer is one of the types of human tumors, that is characterized by a high rate of incidence and prevalence. The major type of cancer in men is lung cancer, as it has the highest rate of incidence and death due to carcinogenesis, it also has the second rate of death among women and the third rate of incidence, worldwide. The epidermal growth factor receptor (EGFR), which is a transmembrane protein and a subclass of receptor tyrosine kinase, has a major role in the carcinogenesis and metastasis of lung tumors. Therefore, the study of EGFR signaling pathways and their activity is crucial for the development of cytotoxic drugs that could provide high response rates with minimum range of side effects. Drugs that inhibit the activity of EGFR could be divided into first-generation, second-generation, and third-generation EGFR inhibitors. The three classes of EGFR differ in their affinity of selectivity and binding to their receptor. This review aims to discuss the role of EGFR in the process of lung carcinogenesis, and the effectiveness of EGFR inhibitors in the treatment of lung cancer patients.