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Lutetium (177 Lu) oxodotreotide or 177 Lu dotatate, brand name Lutathera, is a chelated complex of a radioisotope of the element lutetium with dotatate, used in peptide receptor radionuclide therapy. Specifically, it is used in the treatment of cancers which express somatostatin receptors. [5] It is a radiolabeled somatostatin analog. [3] [6] [7]
DOTA-TATE can be reacted with the radionuclides gallium-68 (T 1/2 = 68 min), lutetium-177 (T 1/2 = 6.65 d) and copper-64 (T 1/2 = 12.7 h) to form radiopharmaceuticals for positron emission tomography (PET) imaging or radionuclide therapy. 177 Lu DOTA-TATE therapy is a form of peptide receptor radionuclide therapy (PRRT) which targets ...
177 Lu-DOTATATE was associated with limited acute toxic effects. In neuroendocrine tumor patients with advanced well-differentiated disease and progression on somatostatin analogs, 177 Lu-DOTATATE is likely to reduce the risk of disease progression and be associated with quality-of-life benefits. [19] [20]
RNT contrasts with sealed-source therapy (brachytherapy) where the radionuclide remains in a capsule or metal wire during treatment and needs to be physically placed precisely at the treatment position. [4] When the radionuclides are ligands (such as with Lutathera and Pluvicto), the technique is also known as radioligand therapy. [5]
Lutetium-177 labelled edotreotide (177 Lu-DOTA-TOC), with the trade name Solucin, is the subject of a phase 3 clinical trial for treatment of GEP-NETs. [ 7 ] [ 8 ] It was granted orphan drug designation by the European Medicines Agency in 2014.
Forty radioisotopes have been characterized, with the most stable, besides 176 Lu, being 174 Lu with a half-life of 3.31 years, and 173 Lu with a half-life of 1.37 years. All of the remaining radioactive isotopes have half-lives that are less than 9 days, and the majority of these have half-lives that are less than half an hour.
As well as diagnosis and staging of NETs, 68 Ga DOTA conjugated peptide imaging may be used for planning and dosimetry in preparation for lutetium-177 or yttrium-90 DOTA therapy. [35] [36] In June 2016, Netspot (kit for the preparation of gallium Ga-68 dotatate injection) was approved for medical use in the United States. [37] [38]
The peptide receptor may be bound to lutetium-177, yttrium-90, indium-111 and other isotopes including alpha emitters. [90] This is a highly targeted and effective therapy with minimal side effects in tumors with high levels of somatostatin cell surface expression, because the radiation is absorbed at the sites of the tumor, or excreted in the ...