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Radiolabeled Somatostatin Analogs—A Continuously Evolving Class of Radiopharmaceuticals
| Content Provider | MDPI |
|---|---|
| Author | Fani, Melpomeni Mansi, Rosalba Nicolas, Guillaume P. Wild, Damian |
| Copyright Year | 2022 |
| Description | Somatostatin receptors (SSTs) are recognized as favorable molecular targets in neuroendocrine tumors (NETs) and neuroendocrine neoplasms (NENs), with subtype 2 $(SST_{2}$) being the predominantly and most frequently expressed. PET/CT imaging with$ ^{68}$Ga-labeled SST agonists, e.g.,$ ^{68}$Ga-DOTA-TOC (SomaKit $TOC^{®}$) or$ ^{68}$Ga-DOTA-TATE $(NETSPOT^{®}$), plays an important role in staging and restaging these tumors and can identify patients who qualify and would potentially benefit from peptide receptor radionuclide therapy (PRRT) with the therapeutic counterparts$ ^{177}$Lu-DOTA-TOC or$ ^{177}$Lu-DOTA-TATE $(Lutathera^{®}$). This is an important feature of SST targeting, as it allows a personalized treatment approach (theranostic approach). Today, new developments hold promise for enhancing diagnostic accuracy and therapeutic efficacy. Among them, the use of $SST_{2}$ antagonists, such as JR11 and LM3, has shown certain advantages in improving image sensitivity and tumor radiation dose, and there is evidence that they may find application in other oncological indications beyond NETs and NENs. In addition, PRRT performed with more cytotoxic α-emitters, such as$ ^{225}$Ac, or $β^{-}$ and Auger electrons, such as$ ^{161}$Tb, presents higher efficacy. It remains to be seen if any of these new developments will overpower the established radiolabeled SST analogs and PRRT with $β^{-}$-emitters. |
| Starting Page | 1172 |
| e-ISSN | 20726694 |
| DOI | 10.3390/cancers14051172 |
| Journal | Cancers |
| Issue Number | 5 |
| Volume Number | 14 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2022-02-24 |
| Access Restriction | Open |
| Subject Keyword | Cancers Radiology, Nuclear Medicine and Imaging Somatostatin Receptors Neuroendocrine Neoplasms Neuroendocrine Tumors Agonist Antagonist Somatostatin Receptor Pet/ct Peptide Receptor Radionuclide Therapy |
| Content Type | Text |
| Resource Type | Article |