Graphene and graphene-based nanomaterials such as graphene oxide (GO), reduced graphene oxide (rGO) and graphene quantum dots (GQDs) have gained a lot of attention from diverse scienti¯c¯elds for applications in sensing, catalysis, nanoelectronics, material engineering, energy storage and biomedicine due to its unique structural, optical, electrical and mechanical properties. Graphene-based nanomaterials emerge as a novel class of nanomedicine for cancer therapy for several reasons. Firstly, its structural properties like high surface area and aromaticity enables easy loading of hydrophobic drugs. Secondly, presence of oxygen containing functional groups improve its physiological stability and also act as site for biofunctionalization. Thirdly, its optical absorption in the NIR region enable them to act as photoagents for photothermal and photodynamic therapies of cancer, both in vitro and in vivo. Finally, its intrinsic°u orescence property helps in bioimaging of cancer cells. Overall, graphene-based nanomaterials can act as agents for developing multifunctional theranostic platforms for carrying out more e±cient detection and treatment of cancers. This review provides a detailed summary of the di®erent applications of graphene-based nanomaterials in drug delivery, nucleic acid delivery, phototherapy, bioimaging and theranostics.