Abstract: OBJECTIVE The review discussed the relationship between endothelin system and the development of tumors, showing that endothelin receptor may be a novel target of anticancer drugs, and providing new ideas on anticancer drug research. METHODS The domestic and foreign data, regarding endothelin system in tumor development and endothelin receptor antagonist in tumor treatment from 2000 to 2010, were retrieved, and the relationship between endothelin system and the development/treatment of tumor was reviewed. RESULTS Endothelin receptor is a novel target of anticancer drugs．CONCLUSION Endothelin receptor antagonist will be a promising agent in the treatment of cancer.