Due to its unique physical structure and chemical properties, graphene family nanomaterials (GFNs) and derived commodities have been widely used in commercial products, particularly biomedical applications, which has significantly increased the risk of human exposure. There exists significant evidence that GFNs are accumulated in a number of tissues and organs through different exposure pathways, and further cause toxicity manifested as lesions or functional impairment. Moreover, GFNs can be internalized by varing cell types and induce cytoskeletal disorders, organelle dysfunction, and interact directly with biological macromolecules such as DNA, mRNA and proteins, ultimately resulting in greater rates of cell apoptosis, necrosis and autophagic cell death. The toxicological effect of GFN is closely related to its lateral size, surface structure, functionalization, and propensity to adsorb proteins. Using major data published over the past four years, this review presents and summarizes state of current understanding of GFN toxicology and identifies current deficiencies and challenges. This review aims to help improve evaluation of the biocompatibility of GFNs and provides theoretical guidance for their safe application.