The unique size-dependent properties of carbon nanomaterials (CNMs)-graphene, nanotubes (CNTs) and fullerenes-make them very attractive for diagnostic and therapeutic application. This chapter presents possible application of CNMs. Graphene with extraordinary chemical and physical properties has already revealed a great number of potential applications such as environmental toxic material removal, drug delivery, tissue engineering, and fl uorescence-based biomolecular sensing. The CNT derivatives have many interesting properties which make them potentially useful in a living system as biosensors, bioelectronic devices based on enzyme-nanotube or antibody-nanotube conjugates, chemotherapeutic agents, hyperthermia therapy and immunotherapy agents, agent in treatment of central nervous system disorders, and tissue engineering agent. Fullerene C 60 derivatives have been used as: drug and gene delivery vectors, magnetic resonance imaging agents, radio protectors, antioxidants, HIV-1 protease inhibitors, antigenotoxic agents, and phototherapy agents. Fullerenols are polyhydroxylated derivatives of fullerene (C 60 (OH)n) with remarkable antioxidant, xenobiotic-protective, radioprotective, nanodrug and endohedral gadolinium carrier properties.