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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]
An octreotide scan is a type of SPECT scintigraphy used to find carcinoid, pancreatic neuroendocrine tumors, and to localize sarcoidosis. It is also called somatostatin receptor scintigraphy (SRS). Octreotide , a drug similar to somatostatin , is radiolabeled with indium-111 , [ 1 ] and is injected into a vein and travels through the bloodstream.
The US Food and Drug Administration (FDA) approved 177 Lu dotatate based primarily on evidence from one clinical trial, NETTER-1 of 229 participants with somatostatin-receptor positive midgut GEP-NETs. [15] Enrolled participants had tumors which could not be surgically removed and were worsening while receiving treatment with octreotide. [15]
Somatostatin receptor antagonists (or somatostatin inhibitors) are a class of chemical compounds that work by imitating the structure of the neuropeptide somatostatin. The somatostatin receptors are G protein-coupled receptors. Somatostatin receptor subtypes in humans are sstr1, 2A, 2 B, 3, 4 and 5. [1]
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It is a non-selective somatostatin receptor antagonist, [37] inhibiting the effects of somatostatin on target cells in the gastrointestinal tract, pancreas, hypothalamus, and central nervous system. [2] Cyclosomatostatin is used as a research chemical to investigate the effects of somatostatin on different cell types by antagonizing its ...
These cells release the peptides growth hormone-releasing hormone (GHRH or somatocrinin) and growth hormone-inhibiting hormone (GHIH or somatostatin) into the hypophyseal portal venous blood surrounding the pituitary. GH release in the pituitary is primarily determined by the balance of these two peptides, which in turn is affected by many ...
The combination of the beta emitter 177 Lu with DOTA-TATE can be used in the treatment of cancers expressing the relevant somatostatin receptors. [16] The U.S. Food and Drug Administration (FDA) considers 177 Lu-dotatate to be a first-in-class medication. [17] Alternatives to 177 Lu-DOTA-TATE include 90 Y (T 1/2 = 64.6 h) DOTA-TATE.
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