Graphene is a kind of atomic crystal with two-dimensional polycyclic aromatic hydrocarbons planes, which is of great concern in various fields. This paper reviews the latest development of graphene-based materials in biomedical research fields in the recent years, including in vitro and in vivo toxicity, drug loading, targeting controlled release, as well as photodynamic therapy. These researches validate that the graphene-based materials indicate promising prospects in the application to biomedicine.