AbstractCancer is prevailing around the world and so does its mortality rates. Conventionally used therapies have some adverse effects as they are not entirely accurate, leading researchers and investigators to explore new ways and materials. They are constantly looking into ways that can effectively cure this malicious disease and in this effort, they came across new smart materials labeled as nanoparticles (NPs). In between various sorts of nanoparticles, only graphene‐based nanomaterials (GBNMs) shine because of their particular chemical structure and properties. They have high drug loading capacity, can easily target specific tissues, and can be easily functionalized according to the stage and other factors for a patient. Several researches and trials have been executed on animal models to check the potency of these nanoparticles proving them revolutionary in the medical domain, especially for combating cancer. Through this review, we evaluate the experiments conducted by scientists in an effort to devise a platform based on graphene nanoparticles for curing cancer efficiently by using single or multiple therapeutic approaches.