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Lutetium Lu 177-DOTA-octreotate

A radioconjugate consisting of the somatostatin analogue octreotate labelled with lutetium Lu 177 with receptor ligand, beta-emitting radioisotope, and potential antineoplastic activities. Lutetium Lu 177-DOTA-octreotate binds to somatostatin receptors (SSTRs), especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumour cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Lutetium Lu 177-DOTA-octreotate is produced by substituting the natural amino acid Thr for the alcohol Thr(ol) at the C terminus of the somatostatin analogue octreotide and chelating the octreotate to Lu 177 via dodecanetetraacetic acid (DOTA).

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