Abstract: Anisotropic gold nanorods have been widely used in biomedical field due to their unique optical properties and excellent biocompatibility. This paper provides a systematic review on the surface modification and functionalization of gold nanorods including the modification with inorganics materials，surfactants，organic small molecules，organic macromolecules，metallic materials and their functionalization. Applications of gold nanorods in the fields of biorecognition，biological imaging，cancer diagnosis and photothermal therapy are also discussed.