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Description: Octreotide is the acetate salt of a cyclic octapeptide. It is a long-acting octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin.
Drug Type: Biotech; Approved; Investigational
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, 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.
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.
Indication: For treatment of acromegaly and reduction of side effects from cancer chemotherapy
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Data Correlations | 1 study

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Genes category icon Genes
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SSTR1 100 100
SSTR2 96 96
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Peptide GPCRs 100 100
Rhodopsin Like 98 98
Neuroactive Ligand Receptor Interac… 98 98
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    Homo sapiens Homo sapiens | Therapeutic   Therapeutic

    The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information.

    Authors: David S Wishart, Craig Knox, An Chi Guo et al.

    Organization: Department of Computing Science, Univers…
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Thought leaders and organizations working on research involving octreotide.

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  • Tullio Florio
  • Marcelo Paez-Pereda
  • Marily Theodoropoulou
  • H A Schmid
  • Marion de Jong
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  • Novartis
  • Novartis Pharmaceuticals
  • North Central Cancer Treatment Group
  • Endo Pharmaceuticals Solutions Inc.
  • Sandoz Inc.
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  • Max Planck Institute of Psychiatry
  • Utrecht University
  • Technische Universität München
  • University of Milan
  • University of Texas M.D. Anderson Cancer Center

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