N⁶-methyladenosine (m⁶A) modification is found the most prevalent and abundant post-transcriptional mRNA modification in eukaryotic cells. It regulates almost all stages of RNA life cycle including splicing, translocation, stability, decay and translation. As a dynamic and reversible process, m⁶A modification is catalyzed by the RNA methyltransferases ('writers'), removed by the demethylases ('erasers'), and interacts with m⁶A-binding proteins ('readers'). Recent studies have revealed that these m⁶A modification regulators are frequently expressed aberrantly in various types of cancer, and involved in cell proliferation, differentiation, metabolism, particularly, in tumorigenesis and tumor progression through diverse mechanisms. In this review, the m⁶A modification process and its regulatory functions in lung cancer are summarized. Furthermore, the research progress in the inhibitor development of m⁶A modification, and the potential of targeting m⁶A modifying proteins for clinical application are discussed.