Lung cancer, primarily non-small cell lung cancer (NSCLC), is a leading cause of morbidity and mortality globally. Targeted therapies have emerged as a preferred first-line treatment for NSCLC patients with oncogenic driver mutations, such as EGFR, ALK, ROS1, BRAF, MET, RET, FGFR, and NTRK. These therapies, including small-molecule drugs and monoclonal antibodies, have shown superior efficacy compared to traditional chemotherapy and immunotherapy, particularly in specific molecular subtypes. Challenges remain in drug resistance, adverse effects, and determining optimal treatment sequences. Continued research is essential for advancing precision medicine in lung cancer treatment.