Abstract: Polypeptide drug conjugate are an emerging tumor-targeted therapy drug with the characteristics of small molecular weight, strong tumor cell penetration, and low immunogenicity, which has received increasing attention in molecular imaging and targeted therapy of tumors. ¹⁷⁷Lu-1, 4, 7, 10-tetraazacyclododecane-1, 4, 7, 10-tetraacetic acid-D-Phe1-Tyr3-Thr8-octreotide (DOTATATE), as the most successful polypeptide drug conjugate, can specifically bind to the somatostatin receptor (SSTR) to achieve peptide receptor radionuclide therapy for tumors. The author reviews the research progress on the therapeutic efficacy, dose selection, and improvement strategies of ¹⁷⁷Lu-DOTATATE in neuroendocrine neoplasms, to provide a reference for the targated therapy of SSTR overexpression tumors.