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  • A radioconjugate consisting of the somatostatin analog octreotate labeled 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 tumor 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 analog octreotide and chelating the octreotate to Lu 177 via dodecanetetraacetic acid (DOTA). Check for \'https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C95020\' active clinical trials using this agent. (\'http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C95020\' NCI Thesaurus)
  • A radioconjugate consisting of the tyrosine-containing somatostatin analog Tyr3-octreotate (TATE) conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope lutetium Lu 177 with potential antineoplastic activities. Lutetium Lu 177 dotatate binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTR, present on the cell membranes of many types of neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Tyr3-octreotate (TATE) is an octreotide derivative in which phenylalanine at position 3 is substituted by tyrosine and position 8 threoninol is replaced with threonine. SSTRs have been shown to be present in large numbers on NET and their metastases, while most other normal tissues express low levels of SSTRs. Check for \'https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C95020\' active clinical trials using this agent. (\'http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C95020\' NCI Thesaurus)
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