Two-dimensional (2D) nanomaterials constitute an emerging novel class of nanomaterials with sheet-like structures having larger lateral size (up to a few microns), but the thickness is much smaller like approximately less than 5 nm. These advanced 2D materials have gained lot of attention in the recent times with respect to its biomedical application. This chapter discusses about the role of advanced materials involving 2D materials for effective lung cancer therapy. The role of various 2D materials such as graphene oxide, black phosphorus, transition metal dichalcogenides, and titanium has been described. The chapter deals in detail with the synthesis, properties, and biomedical application of these materials in cancer. Emphasis has been given on the role of these nanostructures in chemotherapy and gene therapy along with alternative therapeutic strategies such as photodynamic therapy, photothermal therapy, and subcellular-targeted therapy of lung cancer.