Peptide Receptor Radionuclide Therapy (PRRT) is part of the broader concept of targeted radionuclide therapy. PRRT delivers destructive radiation to cancer cells through peptides labeled with radionuclides. These peptides can specifically bind to peptide receptors that are expressed at higher densities on tumor cell membranes compared to non-tumor tissues. Many G protein-coupled receptors fall into this category, where their overexpression is associated with numerous human malignancies.

Regulatory peptides that target G protein-coupled receptors provide a rich source of vectors, which can be chemically modified to transport radioactivity while maintaining their receptor affinity. PRRT is used to treat metastatic or inoperable cancers, particularly neuroendocrine tumors that occur in the pancreas, kidneys, small and large intestines, and stomach, through systemic or localized delivery.

PRRT therapy typically involves four outpatient treatments over eight months, administered every two months. It includes a pre-treatment intravenous infusion of amino acids for about four hours, followed by a 30-45 minute intravenous injection of Lutetium Lu 177 dotatate. In 2004, Steve Jobs received PRRT therapy in Switzerland for NETs pancreatic cancer, which extended his life by seven years. After years of clinical application, this therapy has become more affordable, although related drug development is still in the experimental phase in China.