Peptide Receptor Radionuclide Therapy of Neuroendocrine Tumors Expressing Somatostatin Receptors

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Therapeutic Nuclear Medicine

Part of the book series: Medical Radiology ((Med Radiol Radiat Oncol))

Abstract

Peptide receptor radionuclide therapy (PRRT) refers to the administration of radiolabeled synthetic peptides binding specifically to receptors on tumor cells with high affinity. Therapeutic radionuclides enable irradiation of tumors and their metastases ultimately by way of internalization through the receptor, over-expressed on the tumor cell membrane. Though the primary treatment of neuroendocrine tumors (NETs) is surgery with curative intent or debulking of the tumor mass, treatment with radiolabeled somatostatin (SST) analogs specifically targeting the SST-receptor 2A (SSTR 2A), is effective for the management of patients with inoperable or metastasized NETs. Objective responses are well-documented, which also benefits survival. PRRT of NETs using the agonists like DOTATOC ([DOTA0, Tyr3, Thr8]-octreotide) or DOTATATE ([DOTA0, Tyr3]-octreotate) labeled with beta-emitting radionuclides like 177Lu and 90Y or alpha-emitting radionuclides like 213Bi, has paved the way to molecular radiotherapy. As these peptides are reabsorbed by the kidneys, there is a potential risk of renal toxicity over the long term. Radiation dose to the bone marrow should also be taken into account for conceivable side effects. However, PRRT can be safely administered with renoprotective measures and a personalized approach, including individualized dosimetry to ensure that the dose to normal organs is not exceeded.

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Baum, R.P., Kulkarni, H.R. (2014). Peptide Receptor Radionuclide Therapy of Neuroendocrine Tumors Expressing Somatostatin Receptors. In: Baum, R. (eds) Therapeutic Nuclear Medicine. Medical Radiology(). Springer, Berlin, Heidelberg. https://doi.org/10.1007/174_2013_945

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