Graphene has attracted the attention of the entire scientific community due to its unique mechanical and electrochemical, electronic, biomaterial, and chemical properties. The water-soluble derivative of graphene, graphene oxide, is highly prized and continues to be intensely investigated by scientists around the world. This review seeks to provide an overview of the currents applications of graphene oxide in nanomedicine, focusing on delivery systems, tissue engineering, cancer therapies, imaging, and cytotoxicity, together with a short discussion on the difficulties and the trends for future research regarding this amazing material.