Oxodotreotide
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IUPAC name
Oxodotreotide
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Other names
DOTA3-Tyr3-octreotate, Lutathera
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E number | Lua error in Module:Wikidata at line 879: attempt to index field 'wikibase' (a nil value). |
PubChem CID
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CompTox Dashboard (EPA)
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Properties | |
C65H87Lu3N14O19S2 | |
Molar mass | 1609.554 g/mol |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
Infobox references | |
Oxodotreotide[edit]
Oxodotreotide, also known as dotatate, or DOTA3-Tyr3-octreotate, is a ligand-linked somatostatin peptide analog. The peptide was invented by Jack Erion, and Ananthachari Srinivasan and others in the mid-90’s[1].
Oxodotreotide is closely related to the peptide, edotreotide, in that both molecules are identical, except at the C-terminus, where edotreotide contains a threoninol residue, and oxodotreotide contains L-threonine.[2].
Currently, the oxodotreotide name is only used in context with the radiopharmaceutical, lutetium (177Lu) oxodotreotide, which is the international nonproprietary name (INN) assigned by WHO[3].
Another radiopharmaceutical with the INN, gallium (68Ga) dotatate, is composed of the same chemical entity as lutetium (177Lu) oxodotreotide (DOTA3-Tyr3-octreotate) except that the DOTA moiety of the molecule in one case is complexed with the radionuclide, lutetium-177, and in the other case is complexed with gallium-68. The products are used to diagnose and treat patients with neuroendocrine tumors that over-express somatostatin receptors. The gallium-68 radiolabeled peptide is used as a diagnostic PET (Positron emission tomography) imaging agent, and the lutetium-177 radiolabeled peptide is used as a radiotherapeutic agent.
Both products have been developed by Advanced Accelerator Applications[4][5]
Gallium (68Ga) dotatate is approved for use in the United States for the diagnosis of neuroendocrine tumors and is marketed under the brand name, NETSPOT®®.[4]. Lutetium (177Lu) oxodotreotide has marketing approval in the EU, and also the USA [5][4]. The brand name for the product is LUTATHERA®[5]
References[edit]
- ↑ US 5830431, "Radiolabeled peptide compositions for site-specific targeting", assigned to Mallinckrodt Medical, Inc
- ↑ De Jong M, Breeman WAP, Bakker WH, Kooij PM, Bernard BF, Hofland LJ, Visser TJ, Srinivasan A, Schmidt MA, Erion JL, Bugaj JE (1998). Comparison of 111In-labeled somatostatin analogues for tumor scintigraphy and radionuclide therapy. Cancer Research, 58: 437-441 PMID 9458086
- ↑ https://www.whocc.no/ddd/lists_of_new_atc_ddds_and_altera/new_atc/?order_by=0&d=DESC
- ↑ 4.0 4.1 4.2 http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm504524.htm
- ↑ 5.0 5.1 5.2 http://www.adacap.com/wp-content/uploads/2017/09/2017-09-29-PR-EMA-Approval-Lutathera-ENG.pdf
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