Simple SummaryThis article discusses the use of peptide receptor radionuclide therapy (PRRT) as a key treatment method for advanced, unresectable neuroendocrine tumors. It covers the multidisciplinary theranostic approach, treatment effectiveness, patient outcomes, and toxicity of PRRT for neuroendocrine neoplasms. We will also examine important research, and explore new radiopharmaceuticals for the treatment of these patients.AbstractNeuroendocrine neoplasms (NENs) are tumors originating from neuroendocrine cells distributed throughout the human body. With an increasing incidence over the past few decades, they represent a highly heterogeneous group of neoplasms, mostly expressing somatostatin receptors (SSTRs) on their cell surface. Peptide receptor radionuclide therapy (PRRT) has emerged as a crucial strategy for treating advanced, unresectable neuroendocrine tumors by administering radiolabeled somatostatin analogs intravenously to target SSTRs. This article will focus on the multidisciplinary theranostic approach, treatment effectiveness (such as response rates and symptom relief), patient outcomes, and toxicity profile of PRRT for NEN patients. We will review the most significant studies, such as the phase III NETTER-1 trial, and discuss promising new radiopharmaceuticals, including alpha-emitting radionuclide-labeled somatostatin analogs and SSTR antagonists.