Abstract: Aldo-keto reductase (AKR) 1C3 is a member of the AKR superfamily. Its expression level in a variety of malignant solid tumor cells and hematologic tumor cells is higher than that in normal cells, which is closely related to the occurrence and development of cancer, as well as tumor resistance to chemotherapy/immunotherapy and resistance to radiotherapy. Studies have proved that AKR1C3 can be used both as a biomarker for screening, drug guidance and prognostic diagnosis of tumor patients, and as a new target of anti-tumor drugs for drug design and development. Anti-tumor drugs based on AKR1C3 are expected to provide novel solutions for clinical use. In this article, the research progress of anti-tumor drugs based on AKR1C3 in recent years has been reviewed, and an outlook of the research field has been provided.