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Octreotide, sold under the brand name Sandostatin among others, is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone. It was first synthesized in 1979 and binds predominantly to the somatostatin receptors SSTR2 and SSTR5. [5]
Octreotide (brand name Sandostatin, Novartis Pharmaceuticals) is an octapeptide that mimics natural somatostatin pharmacologically, though is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone, and has a much longer half-life (about 90 minutes, compared to 2–3 minutes for somatostatin). Since it is ...
As somatostatin can cause inhibition of hormone production that uses it as a mediating hormone, it has an antiproliferative effect on cell tumors, especially in neuroendocrine tumors. [2] Somatostatin analogue therapy uses longer-acting agonists than the endogenous somatostatin to extend the antiproliferative effects. [25]
As somatostatin can cause inhibition of hormone production that uses it as a mediating hormone, it has an antiproliferative effect on cell tumors, especially in neuroendocrine tumors. [2] Somatostatin analogue therapy uses longer-acting agonists than the endogenous somatostatin to extend the antiproliferative effects. [24]
Octreotide is an analog of the peptide hormone somatostatin, which inhibits the production of the growth hormone as well as numerous peptide hormones of the gastrointestinal system, including insulin, glucagon, pancreatic polypeptide, gastric inhibitory polypeptide, and gastrin.
The natural somatostatin receptor ligand, the 14 amino acid peptide somatostatin (A), was abridged to the biologically more stable 8 amino acid peptide Octreotide (OC, B). Introduction of a tyrosine into the 3rd position of the Octreotide sequence resulted in Tyr3-Octreotide (TOC, C), which allows for iodination of the tyrosine residue with the ...
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 ...