Lung cancer (LC) remains a leading cause of mortality worldwide, and new therapeutic strategies are urgently needed. One such approach revolves around the utilization of four-stranded nucleic acid secondary structures, known as G-quadruplexes (G4), which are formed by G-rich sequences. G4 structures constitute enticing targets for therapeutic intervention. Ligands that bind selectively to G4 structures, present a promising strategy for regulating crucial cellular processes involved in the progression of LC, rendering them potent agents for lung cancer treatment. In this review, we offer a summary of the recent advancements in the development of ligands capable of targeting specific genes associated with the development and progression of lung cancer.