Malignant tumor disease is one of the leading causes of human death in many countries. Currently, chemotherapy is considered highly efficient for cancer treatment. However, the clinical application of conventional chemotherapeutic agents is limited because of their high toxicity. With the development of nanotechnology, engineered nanomaterials have been widely and increasingly used in biomedical fields such as biomedicine. Thus, the use of engineered nanomaterials has become a promising approach to cancer treatment. Many newly fabricated nanomaterials with unique characteristics exhibit favorable therapeutic and diagnostic properties, implying their enormous potential as biomedical candidates. [Gd@C-82(OH)(22)](n) is a new type of metallofullerenol nanoparticle with high anti-tumor activity but low toxicity. In this article, the properties and biological effects of [Gd@C-82(OH)(22)](n) are summarized, and their possible mechanisms are analyzed.