Nanocomposites based on carbon nanomaterial particularly in graphene oxide, graphene quantum dots, and doped graphene quantum dots with improved biocompatibility have been increasing interests in the field of drug delivery, biosensor, energy, imaging and electronic. These nanomaterials as new kinds of fluorescent probes and electrochemical sensors all display ultrasmall size, good photostability, and excellent biocompatibility. In this chapter, we summarize an updated advance in the development of graphene and its related derivatives of synthesis methods and biomedical applications as nanosensors for detection of metal ions, inorganic ions, amino acids, proteins, saccharides and small molecules, drug molecules, and so on.