ObjectiveTo study the latest progress of cancer therapy by using clostridium perfringens enterotoxin (CPE). MethodsRecent advances in malignant tumor treatment based on the molecular structure and function of CPE and its receptor Claudin-3, -4 was focused. ResultsCPE is cytotoxic for ovarian, breast, pancreatic, and prostate cancer cells which express its receptor Claudin-3, -4, it is also effective over the xenograft mode of those cancers. But CPE is limitted in clinics because of its side effect. Modifying the molecular structure of CPE had made some progress to reduce its toxicity. ConclusionAs the ligand of claudin protein, an important component of tight junction, CPE can attack the tumor cell. It is a potentially a chemotherapeutic drug.