Abstract: Neuroendocrine tumors(NETs) are a group of heterogeneous tumors originating from neuroendocrine cells. They can occur anywhere in the body, most commonly in the digestive tract, pancreas, and lungs. The incidence and prevalence of NET have been increasing in recent years. Early diagnosis of NET has been difficult. Somatostatin receptor(SSTR), as the most common peptide hormone receptor in NET, has become an important target in NET drug development. Radionuclide-labeled somatostatin analogs can specifically bind to SSTR over-expressed on the surface of NET cells. Therefore, such radiopharmaceuticals can be used for early diagnosis and targeted therapy of NET. So far, several SSTR-targeted radiopharmaceuticals have been approved for marketing by the U.S. Food and Drug Administration(FDA), European Medicines Agency(EMA) and other agencies, but no such radiopharmaceuticals have been marketed in China. This review first introduces the relationship between neuroendocrine tumors and SSTR, and the development history of SSTR-targeted metal-based radiopharmaceuticals, and summarizes the diagnostic and therapeutic radiopharmaceuticals that have been approved by the FDA and other drug regulatory authorities in various countries. The different characteristics of SSTR antagonists and antagonist drugs are discussed, and the related research progress of SSTR antagonists in the field of radioactive diagnosis and therapy is remarked. Metal-based radiopharmaceuticals targeting SSTR antagonists have initially shown better diagnostic and therapeutic effects than agonists, and may have good application prospects.