According to World Health Organization estimations, there are 2.3 million women diagnosed with breast cancer in 2020, with 6,85,000 deaths worldwide and 7.8 million women alive who have been diagnosed with breast cancer in the previous 5 years, making it the world's most prevalent cancer. Breast cancer is a diverse illness on a molecular level. Several critical unsolved clinical and scientific issues persist despite great advancements in the detection and treatment of breast cancer. Graphene‐based materials have shown tremendous relevance for detecting/imaging, quality/drug conveyance, malignant growth treatment/finding, and tissue designing/regenerative medication. Indeed, graphene (G) and graphene oxide (GO)-based nano-structures are promising candidates for applications in cancer therapy due to their large surface area, ease of functionalization, high drug loading capacity, and reactive oxygen species induction potentials. For the application of graphene and graphene oxide-based nanosystems in cancer therapy, significant obstacles, recent advancements, and perspectives for the future are discussed.