Carbon nanomaterials (CNMs) are promising nanomaterials for technological advancement, owing to their unique properties, in particular small size, high surface area, photostability, and biocompatibility. In the last few years, several studies have shown their innumerable applications in electronic, photonics, and material science. The advances in use of CNMs in nanomedicine were also quite remarkable. This chapter gives a brief overview of the applications of CNMs in this field. We focus on fullerenes (C60), carbon nano-onions, carbon dots, carbon nanotubes, and graphene derivatives, emphasizing their potential as carriers for intracellular transport of drugs and targeted genes, bioimaging probes, diagnostic, and therapeutic agents.