Fullerene is an effective free radical scavenger and antioxidant. The fullerene derivatives obtained by chemical modification of fullerene have good water solubility and biological activities. Fullerene and its derivatives have many advantages in cell protection and antioxidant properties, antibacterial activity, antiviral activity, photodynamic activity, drug delivery and anti-tumor activities, playing an important role in the field of medicine. In recent years, great progress has been made in this field. In this review, we summarized the latest research progress and applications of fullerene and its derivatives in medicine field at home and abroad from four aspects of regulating tumor microenvironment, drug delivery, photodynamic therapy and anti-oxidative stress. At last, the future development and application of fullerene and its derivatives in the domain of medicine are prospected.