Cerenkov radiation (CR), a phenomenon where charged particles traveling through a medium exceed the speed of light, has gained increasing attention in the realm of health. CR has shown unique imaging value and therapeutic advantages in the aspect of cancer management. In diagnosis, Cerenkov luminescence imaging (CLI) via Cerenkov light (CL) induced by CR can be used for cancer accurate detection and efficacy evaluation. CLI also can provide real-time intraoperative visualization of tumor margins, facilitating complete and precise tumor resection. Additionally, CR-induced photodynamic therapy (CR-PDT) using CL as exciting light has evolved into a novel phototherapeutic strategy, which avoids the need for external aid light sources and breaks the restrictions on the application on deep tumors. Whereas, beyond these superiorities, there are challenges of the extensive use of CR still need to be addressed, such as the need for specialized equipment and the interference of ambient light, because of the low photon volume and short spectrum of CLI. Nonetheless, with further exploration and development, CR has the potential to revolutionize cancer management, improving patient outcomes and advancing the oncology field. In this review, the preclinical and clinical research advances of CR in cancer theranostics are summarized, including early diagnosis, intraoperative navigation, and treatment evaluation.