The development of new systems for diagnostic and therapeutic applications is a topic of intense and growing interest. The unique optical and electronic properties exhibited by gold-based nanomaterials have proved to be valuable for a wide range of biomedical applications. Recently, great attention has been given to rod-shaped gold nanomaterials, especially because of their electronic absorption band in the near infrared region, where maximum radiation penetration through tissue occurs. This feature has allowed the use of gold nanorods for in vivo imaging, with different techniques, and photothermal therapy. Furthermore, gold nanorods can be functionalized with a wide variety of biomolecules for cancer cell targeting. Moreover, their versatility and unique properties have generated much enthusiasm in medicine. The present review aims to show the recent advances in the synthesis and applications of gold nanorods in medical areas.