Lung cancer is the second leading cause of the mortality related to the cancer. So, it is very necessary to explore the novel strategies to eradicate it. Currently, gold based medicinal compounds have emerged as remarkable anticancer agents and expressed strong potential against the lung cancer cell lines. This review provides a comprehensive overview of the history, advancements, and recent state of gold complexes in the treatment of the lung cancer. We discuss the biological evaluation in relation with the chemical structures of numerous gold complexes, including those featuring thiosemicarbazone, N-heterocyclic imine, N-heterocyclic carbenes, steroidyl NHC, CAACs, carbamates, and diphosphanes as ligands. Gold complexes’ cytotoxicity has been assessed and contrasted with that of standard drugs such as auranofin and cisplatin, with a special focus on IC50 values for evaluating potency. This review targets to deliver a detailed understanding of the potential of the gold complexes in lung cancer therapies, paving way for the future research and clinical applications.