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QuickView for Octreotide (compound)

Summary
General Info

PubChem

PubChem Compound 383413

PubChem Compound 383413

Name:	Octreotide
PubChem Compound ID:	383413
Description:	A potent, long-acting synthetic SOMATOSTATIN octapeptide analog that inhibits secretion of GROWTH HORMONE and is used to treat hormone-secreting tumors; DIABETES MELLITUS; HYPOTENSION, ORTHOSTATIC; HYPERINSULINISM; hypergastrinemia; and small bowel fistula.
Molecular formula:	C₅₁H₇₀N₁₀O₁₂S₂
Molecular weight:	1079.29 g/mol
Synonyms:	Sandostatin (TN); NSC671663; 79517-01-4; D02250; AIDS161129; 10-(4-Aminobutyl)-19-((2-amino-3-phenylpropanoyl)amino)-16-benzyl-7-(1-hydroxyethyl)-N-(2-hydroxy-1-(hydroxymethyl)propyl)-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaatzacycloicosane-4-carboxamide acetate; Octreotide acetate; AIDS-161129; D-phenylalanyl-L-hemicystyl-L-phenylalanyl-D-trytophyl-L-lysyl-L-t hreonyl-L-hemicystyl-L-threoninol, acetate; Sandostatin LAR. show more » Sandostatin (TN); NSC671663; 79517-01-4; D02250; AIDS161129; 10-(4-Aminobutyl)-19-((2-amino-3-phenylpropanoyl)amino)-16-benzyl-7-(1-hydroxyethyl)-N-(2-hydroxy-1-(hydroxymethyl)propyl)-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaatzacycloicosane-4-carboxamide acetate; Octreotide acetate; AIDS-161129; D-phenylalanyl-L-hemicystyl-L-phenylalanyl-D-trytophyl-L-lysyl-L-t hreonyl-L-hemicystyl-L-threoninol, acetate; Sandostatin LAR; Sandostatin; NSC672461; Octreotide acetate (JAN/USAN) show less «

DrugBank

Identification

Name:	Octreotide
Name (isomeric):	DB00104
Drug Type:	biotech
Description:	A potent, long-acting synthetic SOMATOSTATIN octapeptide analog that inhibits secretion of GROWTH HORMONE and is used to treat hormone-secreting tumors; DIABETES MELLITUS; HYPOTENSION, ORTHOSTATIC; HYPERINSULINISM; hypergastrinemia; and small bowel fistula.
Synonyms:	Octrotide; Octreotide acetate; Octreotidum [Latin]; Octreotida [Spanish]
Brand:	Atrigel, Sandostatin LAR (Novartis), Sandostatin LAR, Longastatin, Sandostatin
Category:	Anabolic Agents, Antineoplastic Agents, Hormonal, Gastrointestinal Agents, Hormone Replacement Agents
CAS number:	83150-76-9

Pharmacology

Indication:	For treatment of acromegaly and reduction of side effects from cancer chemotherapy
Pharmacology:	Octreotide exerts pharmacologic actions similar to the natural hormone, somatostatin. It is an even more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Like somatostatin, it also suppresses leuteinizing hormone (LH) response to GnRH, decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, vasoactiv... show more » Octreotide exerts pharmacologic actions similar to the natural hormone, somatostatin. It is an even more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Like somatostatin, it also suppresses leuteinizing hormone (LH) response to GnRH, decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide. Octreotide has been used to treat the symptoms associated with metastatic carcinoid tumors (flushing and diarrhea), and Vasoactive Intestinal Peptide (VIP) secreting adenomas (watery diarrhea). Octreotide substantially reduces and in many cases can normalize growth hormone and/or IGF-1 (somatomedin C) levels in patients with acromegaly. show less «
Mechanism of Action:	Octreotide binds to somatostatin receptors. These receptors are coupled via pertussis toxin sensitive G proteins which lead to inhibition of adenylyl cyclase. Octreotide binding to these receptors also stimulates phosphotyrosine phosphatase and activation of the Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins.
Route of elimination:	About 32% of the dose is excreted unchanged into the urine.
Clearance:	7 – 10 L/hr [healthy after 100-mcg SC injection] 18 L/hr [patients with acromegaly after 100-mcg SC injection] 8.8 L/hr [mild renal impairment after 100-mcg SC injection] 7.3 L/hr [moderate renal impairment after 100-mcg SC injection] 7.6 L/hr [severe renal impairment after 100-mcg SC injection] 4.5 L/hr [severe renal failure requiring dialysis after 100-mcg SC injection] 5.9 L/hr [Patients with liver cirrhosis after 100-mcg SC injection] 8.2 L/hr [patients with fatty liver disease after 100-mcg SC injection]
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Tacrolimus	Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Lumefantrine	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Thiothixene	May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Toremifene	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.

Targets

Somatostatin receptor type 1

Somatostatin receptor type 5

Somatostatin receptor type 2