Somatostatin analogues labeled with copper radioisotopes: current status
نویسندگان
چکیده
Peptide receptor radionuclide therapy (PRRT) is a promising way to treat patients with inoperable tumors or metastatic neuroendocrine tumors. This therapeutic strategy is using radiolabeled peptides, which are capable of selective biding to receptors overexpressed in the cancer cells. One of the group of receptor-avid peptide used in the PRRT are the analogues of somatostatin (SST) connected to the complexes of radionuclides (e.g. 90Y, 177Lu or 111In). Many studies have shown that radiopharmaceuticals based on Cu radioisotopes are promising for the diagnosis and treatment of various cancers. This mini-review focuses on recent developments and summarises the results of multiple studies addressing SST agonists and antagonists radiolabeled to Cu radioisotopes.
منابع مشابه
Positron Emission Tomographic Imaging of Copper 64- and Gallium 68-Labeled Chelator Conjugates of the Somatostatin Agonist Tyr3-Octreotate.
The bifunctional chelator and radiometal have been shown to have a direct effect on the pharmacokinetics of somatostatin receptor (SSTR)-targeted imaging agents. We evaluated three Y3-TATE analogues conjugated to NOTA-based chelators for radiolabeling with 64Cu and 68Ga for small-animal positron emission tomographic/computed tomograhic (PET/CT) imaging. Two commercially available NOTA analogues...
متن کاملPET/CT in diagnosis and management of neuroendocrine tumors compared to current FDA approved imaging modalities: a review of literature
Neuroendocrine tumors (NETs) are rare group of neoplasms arising from nervous and endocrine systems. Somatostatin analogue imaging is a functional imaging modality of choice for evaluating the NETs. Recent availability of positron emitting radioisotope labeled somatostatin analogues to image neuroendocrine cancers, has raised the interests to use this new imaging modality in management of patie...
متن کاملPET imaging of tumours with a 64Cu labeled macrobicyclic cage amine ligand tethered to Tyr3-octreotate.
The use of copper radioisotopes in cancer diagnosis and radionuclide therapy is possible using chelators that are capable of binding Cu(II) with sufficient stability in vivo to provide high tumour-to-background contrast. Here we report the design and synthesis of a new bifunctional chelator, 5-(8-methyl-3,6,10,13,16,19-hexaaza-bicyclo[6.6.6]icosan-1-ylamino)-5-oxopentanoic acid (MeCOSar), that ...
متن کاملSynthesis, labeling, formulation and quality control of 99mTc-Tricine-HYNIC-Tyr³-Octreotide, a peptide radiopharmaceutical for imaging Somatostatin receptor positive tumors [Persian]
Somatostatin analoges labeled with different radionuclides are able used for imaging and treatment of somatostatin receptor positive tumors. In this study Tyr³-Octreotide protected at lysine as an analoge of somatostatin was conjugated with bifunctional chelating agent 6-BOC-hydrazinopyridine-3-carboxylic acid (BOC-HYNIC) and after deprotecting of conjugate, purification was performed wit...
متن کاملPeptide receptor radionuclide therapy.
On their plasma membranes, cells express receptor proteins with high affinity for regulatory peptides, such as somatostatin. Changes in the density of these receptors during disease, for example, overexpression in many tumors, provide the basis for new imaging methods. The first peptide analogues successfully applied for visualization of receptor-positive tumors were radiolabeled somatostatin a...
متن کامل