DT-Web

DB00104 - Octreotide


Identification
Name Octreotide
Accession Number DB00104 (BIOD00088, BTD00088)
Type small molecule
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.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 1019.239
Groups approved
Monoisotopic Weight 1018.440479762
Pharmacology
Indication For treatment of acromegaly and reduction of side effects from cancer chemotherapy
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.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination About 32% of the dose is excreted unchanged into the urine.
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Cyclosporine Octreotide decreases the effect of cyclosporine
Dihydrocodeine Concurrent use may enhance the analgesic effect of dihydrocodeine. It is recommended to monitor therapy, and reduce the dose of dihydrocodeine as appropriate.
Insulin Lispro Concomitant therapy with somatostatin analogs may increase the blood-glucose-lowering effect of insulin lispro and thus the chance of hypoglycemia should be monitored closely.
Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Quinupristin This combination presents an increased risk of toxicity
Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
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.
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.
Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Food Interactions Not Available

Targets


Somatostatin receptor type 1
Name Somatostatin receptor type 1
Gene Name SSTR1
Pharmacological action yes
Actions Not Available
References
  • Wang ZZ, Qu W, Wang F, Li Y, Wang SK, Wang JQ: [Expression of somatostatin receptor reporter gene and its correlation with targeted imaging in vivo for detection of pancreas carcinoma] Zhonghua Zhong Liu Za Zhi. 2005 Nov;27(11):663-6. - Pubmed
  • Matrone C, Pivonello R, Colao A, Cappabianca P, Cavallo LM, Del Basso De Caro ML, Taylor JE, Culler MD, Lombardi G, Di Renzo GF, Annunziato L: Expression and function of somatostatin receptor subtype 1 in human growth hormone secreting pituitary tumors deriving from patients partially responsive or resistant to long-term treatment with somatostatin analogs. Neuroendocrinology. 2004 Mar;79(3):142-8. Epub 2004 Apr 16. - Pubmed
  • Jaquet P, Gunz G, Saveanu A, Barlier A, Dufour H, Taylor J, Dong J, Kim S, Moreau JP, Culler MD: BIM-23A760, a chimeric molecule directed towards somatostatin and dopamine receptors, vs universal somatostatin receptors ligands in GH-secreting pituitary adenomas partial responders to octreotide. J Endocrinol Invest. 2005;28(11 Suppl International):21-7. - Pubmed
  • Schmid HA, Silva AP: Short- and long-term effects of octreotide and SOM230 on GH, IGF-I, ACTH, corticosterone and ghrelin in rats. J Endocrinol Invest. 2005;28(11 Suppl International):28-35. - Pubmed
  • Ruan W, Fahlbusch F, Clemmons DR, Monaco ME, Walden PD, Silva AP, Schmid HA, Kleinberg DL: SOM230 inhibits insulin-like growth factor-I action in mammary gland development by pituitary independent mechanism: mediated through somatostatin subtype receptor 3? Mol Endocrinol. 2006 Feb;20(2):426-36. Epub 2005 Oct 13. - Pubmed
DTHybrid score 1.0393
Somatostatin receptor type 5
Name Somatostatin receptor type 5
Gene Name SSTR5
Pharmacological action yes
Actions Not Available
References
  • Bronstein MD: Acromegaly: molecular expression of somatostatin receptor subtypes and treatment outcome. Front Horm Res. 2006;35:129-34. - Pubmed
  • Xie Y, Tang CW, Wang CH: [Effect of HBV X gene transfection on octreotide-inhibited growth of hepatocellular carcinoma cell line HepG2] Ai Zheng. 2005 Aug;24(8):965-9. - Pubmed
  • Wang ZZ, Qu W, Wang F, Li Y, Wang SK, Wang JQ: [Expression of somatostatin receptor reporter gene and its correlation with targeted imaging in vivo for detection of pancreas carcinoma] Zhonghua Zhong Liu Za Zhi. 2005 Nov;27(11):663-6. - Pubmed
  • Jaquet P, Gunz G, Saveanu A, Barlier A, Dufour H, Taylor J, Dong J, Kim S, Moreau JP, Culler MD: BIM-23A760, a chimeric molecule directed towards somatostatin and dopamine receptors, vs universal somatostatin receptors ligands in GH-secreting pituitary adenomas partial responders to octreotide. J Endocrinol Invest. 2005;28(11 Suppl International):21-7. - Pubmed
  • Schmid HA, Silva AP: Short- and long-term effects of octreotide and SOM230 on GH, IGF-I, ACTH, corticosterone and ghrelin in rats. J Endocrinol Invest. 2005;28(11 Suppl International):28-35. - Pubmed
DTHybrid score 1.3503
Somatostatin receptor type 2
Name Somatostatin receptor type 2
Gene Name SSTR2
Pharmacological action yes
Actions binder
References
  • Yim CB, Boerman OC, de Visser M, de Jong M, Dechesne AC, Rijkers DT, Liskamp RM: Versatile conjugation of octreotide to dendrimers by cycloaddition ( - click
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 1.3525

Enzymes


Myeloperoxidase
Name Myeloperoxidase
Gene Name MPO
Actions inhibitor
References
  • Alatas E, Alatas O, Colak O: Octreotide inhibits myeloperoxidase activity in rat uterus. Acta Obstet Gynecol Scand. 2000 Jul;79(7):524-7. - Pubmed
  • Alatas E, Gunal O, Alatas O, Colak O: Octreotide prevents postoperative adhesion formation by suppressing peritoneal myeloperoxidase activity. Hepatogastroenterology. 2000 Jul-Aug;47(34):1034-6. - Pubmed
DTHybrid score 0.5249

Predictions


Id Partner name Gene Name Score
6009 Somatostatin receptor type 3 SSTR3 0.5516
427 Substance-P receptor TACR1 0.277
290 Prostaglandin G/H synthase 2 PTGS2 0.0391
1736 Somatostatin SST 0.0311
4186 Neuropeptide Y receptor type 2 NPY2R 0.0311
20 Prostaglandin G/H synthase 1 PTGS1 0.0268
309 Antithrombin-III SERPINC1 0.0251
3997 Cytochrome P450 24A1, mitochondrial CYP24A1 0.0239
563 Thyroid peroxidase TPO 0.0238
153 Dopamine beta-hydroxylase DBH 0.0238
275 Arachidonate 5-lipoxygenase ALOX5 0.0215
723 Cytosolic phospholipase A2 PLA2G4A 0.021
3866 Serum amyloid A protein SAA1 0.0209
1932 Apolipoprotein E APOE 0.0208
1200 AMBP protein AMBP 0.0208
54 Prothrombin F2 0.0207
61 2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinase folK 0.0201
2644 2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinase folK 0.0201
2710 2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinase folK 0.0201
1974 Oligopeptide transporter, kidney isoform SLC15A2 0.019
856 Vitamin D3 receptor VDR 0.0189
6020 Aldehyde oxidase AOX1 0.0188
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0183
239 Coagulation factor X F10 0.0167
115 Penicillin-binding protein 2 mrdA 0.016
6069 Penicillin-binding protein 2 mrdA 0.016
6118 Penicillin-binding protein 2 penA 0.016
6187 Penicillin-binding protein 2 pbpA 0.016
6686 Penicillin-binding protein 2 pbp2 0.016
6939 Penicillin-binding protein 2 mrdA 0.016
7163 Penicillin-binding protein 2 pbpA 0.016
867 Penicillin-binding protein 3 pbpC 0.016
6119 Penicillin-binding protein 3 pbp3 0.016
7154 Penicillin-binding protein 3 pbp3 0.016
7157 Penicillin-binding protein 3 LMHCC_2184 0.016
7162 Penicillin-binding protein 3 pbpB 0.016
7172 Penicillin-binding protein 3 pbp3 0.016
6012 Tryptophan 2,3-dioxygenase TDO2 0.0155
4200 Cytochrome P450 1A2 CYP1A2 0.0146
4757 Cytochrome P450 2C9 CYP2C9 0.0132
6165 Copper-transporting ATPase 1 ATP7A 0.0132
6163 Copper-transporting ATPase 2 ATP7B 0.0132
633 Penicillin-binding proteins 1A/1B pbpA 0.0132
6146 High affinity copper uptake protein 1 SLC31A1 0.0125
4152 Superoxide dismutase [Cu-Zn] SOD1 0.0121
6270 Group IIE secretory phospholipase A2 PLA2G2E 0.0121
908 Glutathione S-transferase theta-1 GSTT1 0.0119
2038 Inhibitor of nuclear factor kappa-B kinase subunit beta IKBKB 0.0119
896 Glutathione S-transferase Mu 1 GSTM1 0.0105
118 Organic cation/carnitine transporter 2 SLC22A5 0.0103
3947 Xanthine dehydrogenase/oxidase XDH 0.0099
2157 NAD(P)H dehydrogenase [quinone] 1 NQO1 0.0099
6161 Probable low affinity copper uptake protein 2 SLC31A2 0.0098
904 Glutathione S-transferase P GSTP1 0.0094
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0083
713 Sodium-dependent dopamine transporter SLC6A3 0.008
3941 Amine oxidase [flavin-containing] A MAOA 0.008
238 Peroxisome proliferator-activated receptor gamma PPARG 0.008
3939 Amine oxidase [flavin-containing] B MAOB 0.008
6024 Cytochrome P450 1A1 CYP1A1 0.0079
6013 Cytochrome P450 2E1 CYP2E1 0.0078
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0076
1729 Solute carrier family 22 member 6 SLC22A6 0.0075
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0075
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0071
6016 Cytochrome P450 2C19 CYP2C19 0.007
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0069
109 Mitochondrial carnitine/acylcarnitine carrier protein CACL SLC25A29 0.0067
636 Mitochondrial carnitine/acylcarnitine carrier protein SLC25A20 0.0067
3601 Dihydropteroate synthase 1 folP1 0.0065
3807 Dihydropteroate synthase 1 folP1 0.0065
3808 Dihydropteroate synthase 2 folP2 0.0065
122 P2Y purinoceptor 12 P2RY12 0.0062
6036 Eosinophil peroxidase EPX 0.0059
6168 Solute carrier family 22 member 16 SLC22A16 0.0058
200 Carnitine O-palmitoyltransferase 2, mitochondrial CPT2 0.0058
451 Carnitine O-palmitoyltransferase I, liver isoform CPT1A 0.0058
3830 Calreticulin CALR 0.0057
412 Peroxisomal carnitine O-octanoyltransferase CROT 0.0057
551 Carnitine O-acetyltransferase CRAT 0.0057
6034 Hydroxyindole O-methyltransferase ASMT 0.0055
6035 Nuclear receptor ROR-beta RORB 0.0055
4924 Cytochrome P450 2C8 CYP2C8 0.0054
1898 Cytochrome P450 1B1 CYP1B1 0.0053
6142 Solute carrier family 22 member 8 SLC22A8 0.0051
6030 Cytochrome P450 2B6 CYP2B6 0.0049
765 Indoleamine 2,3-dioxygenase IDO1 0.0047
6102 Arylamine N-acetyltransferase 2 NAT2 0.0045
362 Melatonin receptor type 1B MTNR1B 0.0045
571 Melatonin receptor type 1A MTNR1A 0.0045
4512 Cytochrome P450 3A4 CYP3A4 0.0043
6144 Solute carrier family 22 member 2 SLC22A2 0.0042
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0041
4604 Liver carboxylesterase 1 CES1 0.0037
833 Organic cation/carnitine transporter 1 SLC22A4 0.0035
243 Ribosyldihydronicotinamide dehydrogenase [quinone] NQO2 0.0033
6106 Cytochrome P450 2C18 CYP2C18 0.0033
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.003
465 Calmodulin CALM1 0.0029
4119 Cytochrome P450 2D6 CYP2D6 0.0028
6147 Solute carrier family 22 member 3 SLC22A3 0.0027
468 Cytochrome P450 4A11 CYP4A11 0.0026
6137 Multidrug resistance-associated protein 6 ABCC6 0.0026
3811 Cytochrome P450 19A1 CYP19A1 0.0026
6107 Cytochrome P450 3A7 CYP3A7 0.0024
136 Estrogen receptor ESR1 0.0024
6136 Multidrug resistance-associated protein 5 ABCC5 0.0024
4118 Cytochrome P450 3A5 CYP3A5 0.0023
6145 Solute carrier family 22 member 1 SLC22A1 0.0023
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.0021
3923 Cholinesterase BCHE 0.0018
1588 Multidrug resistance protein 1 ABCB1 0.0013
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