Fullerene derivatives with amino acids, peptides and proteins have wide perspectives in biomedical applications. Thus, development and up-scaling of synthesis procedures, as well as investigation of the physico-chemical and biological properties of these derivatives, are extremely important. The present paper systematizes the current literature data on synthesis, physico-chemical properties and application of fullerene derivatives with amino acids, peptides and proteins in biomedicine. Experimental and theoretical data presented in the review give a comprehensive overview of these substances and can be valuable for specialists in the fields of nanotechnology, nanomaterials and bionanomedicine.