Identification
- Summary
Octreotide is a peptide drug used to treat acromegaly as well as diarrhea associated with metastatic carcinoid tumors and vasoactive intestinal peptide secreting tumors.
- Brand Names
- Bynfezia, Mycapssa, Sandostatin
- Generic Name
- Octreotide
- DrugBank Accession Number
- DB00104
- Background
Acromegaly is a disorder caused by excess growth hormone (GH), increasing the growth of body tissues and causing metabolic dysfunction.6 In most cases, it results from an anterior pituitary growth hormone-releasing tumor. Typically, the feet, hands, and face grow abnormally large; organomegaly and insulin resistance may also occur. Acromegaly is a life-threatening disease requiring life-long management.6
Octreotide is a long-acting drug with pharmacologic activities that mimic those of the natural hormone, somatostatin, which inhibits the secretion of growth hormone.8 Additionally, it is used for the treatment of acromegaly and symptoms arising from various tumors, including carcinoid tumors and vasoactive intestinal tumors (VIPomas).8 In the past, octreotide has been administered solely by injection. On June 26, 2020, the first approved delayed-release oral somatostatin analog, Mycapssa, received FDA approval for the long term maintenance treatment of acromegaly. This drug was developed by Chiasma Inc.5,7,10
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Peptides - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
- Not Available
- Synonyms
- Octreotida
- Octreotide
- Octreotidum
- Octrotide
- External IDs
- DRG-0115
- SMS 201-995
- SMS-201-995
- SMS995-AAA
Pharmacology
- Indication
Octreotide by injection is used for the treatment of acromegaly and the reduction of flushing and diarrhea symptoms related to carcinoid tumors and/or vasoactive intestinal peptide (VIPoma) tumors.8 The delayed-release oral formulation is used for the long-term treatment of acromegaly in patients who tolerate and respond adequately to injectable octreotide and lanreotide.7,13
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Acromegaly •••••••••••• ••••• ••••••••• •• ••• ••••••••• •••••••••••• •••••••• ••••••••• •••••••• ••••••• ••••••• Management of Acromegaly •••••••••••• Treatment of Acromegaly •••••••••••• •••••••• ••••••• ••••••• Treatment of Diarrhea •••••••••••• ••••••••• Symptomatic treatment of Metastatic carcinoid tumors •••••••••••• ••••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Octreotide mimics the naturally occurring hormone known as somatostatin. Like somatostatin, it demonstrates activity against growth hormone and glucagon, treating the disordered tissue growth and insulin regulation in patients with acromegaly.6,8 In addition, octreotide relieves the flushing and diarrhea associated with gastrointestinal tumors by reducing splanchnic blood flow4 and various gastrointestinal hormones associated with diarrhea.2
Product labeling warns that octreotide may reduce gallbladder contractility, bile secretion, and the release of thyroid-stimulating hormone (TSH) in healthy volunteers.8 In addition, reports of decreased vitamin B12 in patients treated with octreotide have been made. Ensure to monitor vitamin B12 levels in patients taking octreotide.10
- Mechanism of action
Octreotide binds to somatostatin receptors coupled to phospholipase C through G proteins and leads to smooth muscle contraction in the blood vessels.9 Downstream effects that stimulate phospholipase C, the production of 1, 4,5-inositol triphosphate, and action on the L-type calcium channels lead to the inhibition of growth hormone, treating the various growth-hormone and metabolic effects of acromegaly.9
Octreotide's suppression of luteinizing hormone (LH)3, reduction in splanchnic blood flow4, and inhibition of serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide provide relief for the gastrointestinal and flushing symptoms of carcinoid and/or VIPoma tumors.2
Target Actions Organism ASomatostatin receptor agonistHumans - Absorption
After a subcutaneous dose, octreotide is absorbed completely upon administration.2,8 After the administration of an oral delayed-release capsule, peak concentrations were found to be 33% lower than after subcutaneous administration.10 The Cmax was attained at 1.67–2.5 hours after oral administration versus 30 minutes for the subcutaneous route. At 20 mg twice a day in patients with acromegaly, peak concentration was 2.5 mg/nL versus 5.30 ng/mL at 40 mg twice a day.10 AUC increases in proportion with the dose, regardless of the route.2,10
- Volume of distribution
In a pharmacokinetic study, the volume of distribution was 13.6 L in healthy volunteers.10 One pharmacokinetic study revealed a volume of distribution ranging from 18.1-30.4L after intravenous administration in healthy volunteers.2
- Protein binding
Approximately 65% of the dose is bound in the plasma to lipoproteins and albumin.8,10
- Metabolism
Octreotide has been reported to be heavily metabolized in the liver.2
- Route of elimination
About 32% of an oral octreotide dose is excreted into the urine 10 and 30-40% is excreted by the liver into the feces.2. About 11% of the unchanged parent drug is found in the urine, and 2% of the unchanged parent drug can be recovered in the feces.2
- Half-life
After a subcutaneous dose, the plasma half-life is estimated to be 0.2 hours. The average elimination half-lives for subcutaneous and oral administration ranged from 2.3 - 2.7 hours and did not differ significantly.10 One pharmacokinetic study revealed a plasma half-life ranging from 72-113 minutes.2
- Clearance
The total body clearance of octreotide is 7-10 L/h.10 One pharmacokinetic study revealed a total body clearance of 11.4 L/h.2
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
There is limited information regarding cases of octreotide overdose aside from case reports of an overdose with injectable octreotide. The dose ranged from 2.4 mg/day to 6 mg/day administered by continuous infusion or subcutaneous administration of 1.5 mg three times daily. Effects of an overdose with octreotide may include hypotension, brain hypoxia, arrhythmia, cardiac arrest, lactic acidosis, pancreatitis, hepatomegaly, diarrhea, flushing, lethargy, and weakness.10
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Octreotide. Acalabrutinib The serum concentration of Acalabrutinib can be increased when it is combined with Octreotide. Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Octreotide. Acebutolol The serum concentration of the active metabolites of Octreotide can be increased when Octreotide is used in combination with Acebutolol. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Octreotide. - Food Interactions
- Take on an empty stomach. The oral capsules should be taken on an empty stomach. Food reduces oral octreotide absorption by 90%.
- Take with or without food. Octreotide injections may be taken with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Octreotide acetate 75R0U2568I 79517-01-4 XQEJFZYLWPSJOV-XJQYZYIXSA-N Octreotide pamoate MWH8YQ1AIO 135467-16-2 KFWJVABDRRDUHY-XJQYZYIXSA-N - International/Other Brands
- Sandostatin LAR (Novartis Pharmaceuticals)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image BYNFEZIA Pen Injection 2.5 mg/1mL Subcutaneous Sun Pharmaceutical Industries, Inc. 2020-04-29 Not applicable US 
Mycapssa Capsule, delayed release 20 mg/1 Oral Chiesi USA, Inc. 2020-07-06 Not applicable US Mycapssa Capsule, delayed release 20 mg/1 Oral Amryt Pharmaceuticals Designated Activity Company 2020-07-06 Not applicable US Mycapssa Capsule, delayed release 20 mg Oral Amryt Pharmaceuticals DAC 2023-02-10 Not applicable EU 
Ocphyl Solution 500 mcg / mL Intravenous; Subcutaneous Pendopharm Division Of Pharmascience Inc 2014-05-12 2018-06-14 Canada 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Octreotide Injection, solution 50 ug/1mL Intravenous; Subcutaneous Fresenius Kabi USA, LLC 2006-03-14 Not applicable US Octreotide Injection, solution 100 ug/1mL Intravenous; Subcutaneous Fresenius Kabi USA, LLC 2006-03-14 Not applicable US Octreotide Injection, solution 1000 ug/1mL Intravenous; Subcutaneous Fresenius Kabi USA, LLC 2006-03-14 Not applicable US Octreotide Injection, solution 500 ug/1mL Intravenous; Subcutaneous Fresenius Kabi USA, LLC 2006-03-14 Not applicable US Octreotide Injection, solution 200 ug/1mL Intravenous; Subcutaneous Fresenius Kabi USA, LLC 2006-03-14 Not applicable US
Categories
- ATC Codes
- H01CB02 — Octreotide
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antineoplastic Agents
- Antineoplastic Agents, Hormonal
- Bradycardia-Causing Agents
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Gastrointestinal Agents
- Hyperglycemia-Associated Agents
- Hypoglycemia-Associated Agents
- Hypothalamic Hormones
- Miscellaneous Therapeutic Agents
- P-glycoprotein substrates
- Peptides
- Peptides, Cyclic
- Pituitary and Hypothalamic Hormones and Analogues
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- Somatostatin and Analogues
- Somatostatin Receptor Agonists
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- RWM8CCW8GP
- CAS number
- 83150-76-9
References
- Synthesis Reference
Nishith Chaturvedi, "Novel process for production of the somatostatin analog, octreotide." U.S. Patent US20040225108, issued November 11, 2004.
US20040225108- General References
- Biermasz NR: New medical therapies on the horizon: oral octreotide. Pituitary. 2017 Feb;20(1):149-153. doi: 10.1007/s11102-016-0785-3. [Article]
- Battershill PE, Clissold SP: Octreotide. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in conditions associated with excessive peptide secretion. Drugs. 1989 Nov;38(5):658-702. doi: 10.2165/00003495-198938050-00002. [Article]
- Prelevic GM, Wurzburger MI, Balint-Peric L, Nesic JS: Inhibitory effect of sandostatin on secretion of luteinising hormone and ovarian steroids in polycystic ovary syndrome. Lancet. 1990 Oct 13;336(8720):900-3. doi: 10.1016/0140-6736(90)92270-r. [Article]
- Clarke DL, McKune A, Thomson SR: Octreotide lowers gastric mucosal blood flow in normal and portal hypertensive stomachs. Surg Endosc. 2003 Oct;17(10):1570-2. doi: 10.1007/s00464-002-9274-z. Epub 2003 Jul 21. [Article]
- Bioworld: Chiasma carries new oral acromegaly treatment, Mycapssa, to FDA approval [Link]
- NIH StatPearls: Acromegaly [Link]
- FDA approval letter: Mycapssa [Link]
- Product monograph: Sandostatin (octreotide acetate) injection [Link]
- NIH StatPearls: Octreotide [Link]
- FDA Approved Drug Products: Mycapssa (octreotide) delayed-release capsules for oral administration [Link]
- Cayman Chem MSDS: Octreotide acetate [Link]
- Product monograph: Octreotide injection (octreotide acetate) [Link]
- EMA Summary of Product Characteristics: Mycapssa (octreotide) gastro-resistant hard capsules for oral use (December 2022) [Link]
- FDA Approved Drug Products: Sandostatin (octreotide acetate) for subcutaneous or intravenous injection [Link]
- External Links
- KEGG Drug
- D00442
- KEGG Compound
- C07306
- PubChem Compound
- 448601
- PubChem Substance
- 46504600
- ChemSpider
- 395352
- BindingDB
- 50272772
- 7617
- ChEMBL
- CHEMBL1680
- Therapeutic Targets Database
- DAP000397
- PharmGKB
- PA450678
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Octreotide
- FDA label
- Download (69.7 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Not Available Pituitary Adenoma 1 4 Completed Prevention Diarrhea / Neoplasm 1 4 Completed Supportive Care Colonic Motility Index / Constipation 1 4 Completed Treatment Acromegaly 11 4 Completed Treatment Ascites / Cirrhosis of the Liver 1
Pharmacoeconomics
- Manufacturers
- App pharmaceuticals llc
- Bedford laboratories div ben venue laboratories inc
- Sun pharmaceutical industries ltd
- Teva parenteral medicines inc
- Novartis pharmaceuticals corp
- Packagers
- APP Pharmaceuticals
- Bachem Inc.
- Bedford Labs
- Ben Venue Laboratories Inc.
- Novartis AG
- Polfa
- Sandoz
- Sicor Pharmaceuticals
- Solvay Pharmaceuticals
- Sun Pharmaceutical Industries Ltd.
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Injection Subcutaneous 2.5 mg/1mL Solution Parenteral 1 mg Solution Parenteral 1.000 mg Injection, powder, for suspension Parenteral 10 MG/2ML Injection, powder, for suspension Parenteral 10 MG Injection, powder, for suspension Parenteral 20 MG/2ML Injection, powder, for suspension Parenteral 20 MG Injection, powder, for suspension Parenteral 30 MG/2ML Injection, powder, for suspension Parenteral 30 MG Injection, solution 100 MICROGRAMMI/ML Injection, solution 100 MICROGRAMMI/1ML Injection, solution 1000 MICROGRAMMI/5ML Injection, solution 50 MICROGRAMMI/ML Injection, solution 50 MICROGRAMMI/1ML Injection, solution 500 MICROGRAMMI/1ML Injection, solution 500 MICROGRAMMI/ML Capsule, delayed release Oral 20 mg Capsule, delayed release Oral 20 mg/1 Injection 0.1 mg Injection Injection Intravenous 1000 ug/1mL Injection Intravenous 200 ug/1mL Injection Intravenous; Subcutaneous 100 ug/1mL Injection Intravenous; Subcutaneous 1000 ug/1mL Injection Intravenous; Subcutaneous 200 ug/1mL Injection Intravenous; Subcutaneous 50 ug/1mL Injection Intravenous; Subcutaneous 500 ug/1mL Injection, solution Intravenous 200 ug/1mL Injection, solution Intravenous; Subcutaneous 100 ug/1mL Injection, solution Intravenous; Subcutaneous 1000 ug/1mL Injection, solution Intravenous; Subcutaneous 200 ug/1mL Injection, solution Intravenous; Subcutaneous 50 ug/1mL Injection, solution Intravenous; Subcutaneous 500 ug/1mL Powder Not applicable 1 g/1g Solution Intravenous; Subcutaneous 100 mcg / mL Solution Intravenous; Subcutaneous 50 mcg / mL Solution Intravenous; Subcutaneous 500 mcg / mL Injection, solution Parenteral 0.05 MG/ML Injection, solution Parenteral 0.1 MG/ML Injection, solution Parenteral 0.5 MG/ML Injection, solution Parenteral 1 MG/5ML Injection, powder, for suspension, extended release; kit Intramuscular 10 mg / vial Injection, powder, for suspension, extended release; kit Intramuscular 20 mg / vial Injection, powder, for suspension, extended release; kit Intramuscular 30 mg / vial Injection, solution Parenteral 0.2 MG/ML Injection, solution Parenteral 0.05 MG/1ML Injection, solution Parenteral 0.1 MG/1ML Injection, solution Parenteral 0.5 MG/1ML Injection, powder, for suspension, extended release Intramuscular 10 MG/vial Injection, powder, for suspension, extended release Intramuscular 20 MG/vial Injection, powder, for suspension, extended release Intramuscular 30 MG/vial Injection, powder, for suspension Injection, solution Injection Intravenous; Subcutaneous Solution Intravenous; Subcutaneous 200 mcg / mL Solution 0.1 mg/1ml Solution 0.5 mg/1ml Injection, solution 0.1 mg/ml Injection, solution Parenteral 100 Mikrogramm/ml Injection, solution Parenteral Injection, solution Parenteral 50 Mikrogramm/ml Injection, solution Parenteral 500 Mikrogramm/ml Solution Parenteral 0.05 mg Solution Parenteral 0.1 mg Injection Intravenous Injection Subcutaneous 0.05 mg/ml Injection Subcutaneous 0.1 mg/ml Injection, powder, for solution Intramuscular 10 mg Injection, powder, for solution Intramuscular 20 mg Injection, powder, for solution Intramuscular 30 mg Injection, powder, for suspension, extended release Intramuscular 10 mg / vial Injection, powder, for suspension, extended release Intramuscular 20 mg / vial Injection, powder, for suspension, extended release Intramuscular 30 mg / vial Powder 10 mg/1vial Injection, suspension 10 mg Injection, suspension 20 mg Powder 20 mg/1vial Injection Intramuscular Powder 30 mg/1vial Injection, suspension 30 mg Injection, powder, for suspension; kit Intramuscular 1.667 mg/1mL Injection, powder, for suspension; kit Intramuscular 3.33 mg/1mL Injection, powder, for suspension; kit Intramuscular 5 mg/1mL Kit Intramuscular 1.667 mg/1mL Kit Intramuscular 10 mg/1 Kit Intramuscular 20 mg/1 Kit Intramuscular 3.33 mg/1mL Kit Intramuscular 30 mg/1 Kit Intramuscular 5 mg/1mL Injection Intramuscular 10 mg Injection Intramuscular 20 mg Injection Intramuscular 30 mg Injection Parenteral 0.2 mg Solution Intravenous; Subcutaneous 0.1 mg Injection, powder, for suspension Intramuscular 30 mg Injection, powder, for suspension Intramuscular 20 mg Injection, solution 1 MG/5ML Injection, solution Parenteral 100 μg/ml Injection, solution Parenteral 500 μg/ml Solution Parenteral 0.200 mg Suspension Parenteral 20.000 mg Injection, powder, lyophilized, for solution Intravenous; Subcutaneous 200 cg Injection, solution Parenteral 200 MICROGRAMMI/ML Injection, solution Parenteral 100 MICROGRAMMI/ML Injection, solution Parenteral 500 MICROGRAMMI/ML Injection, solution 0.1 mg/1ml - Prices
Unit description Cost Unit Sandostatin lar 30 mg kit 3860.62USD kit Sandostatin lar 20 mg kit 2578.19USD kit Sandostatin lar 10 mg kit 1967.81USD kit Sandostatin 1 mg/ml vial 234.49USD ml Sandostatin 0.5 mg/ml ampul 111.48USD ml Octreotide 1000 mcg/ml vial 67.2USD ml Sandostatin 0.2 mg/ml vial 47.66USD ml Octreotide acet 500 mcg/ml vial 24.48USD ml Sandostatin 0.1 mg/ml ampul 23.11USD ml Octreotide acet 100 mcg/ml vial 15.36USD ml Octreotide acet 200 mcg/ml vial 14.4USD ml Sandostatin 0.05 mg/ml ampul 11.92USD ml Octreotide acet 50 mcg/ml vial 3.6USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5538739 No 1996-07-23 2013-07-23 US CA1328402 No 1994-04-12 2011-04-12 Canada US5922338 Yes 1999-07-13 2017-01-13 US US5922682 Yes 1999-07-13 2017-01-13 US US5728396 No 1998-03-17 2017-01-30 US US6156331 No 2000-12-05 2017-01-30 US US6375978 No 2002-04-23 2018-12-17 US US6235712 No 2001-05-22 2017-06-13 US US6113938 No 2000-09-05 2018-07-24 US US6124261 No 2000-09-26 2017-06-13 US US6395292 No 2002-05-28 2017-01-30 US US6132420 No 2000-10-17 2017-01-30 US US5985305 No 1999-11-16 2017-01-30 US US5932547 No 1999-08-03 2017-06-13 US US5753618 Yes 1998-05-19 2015-11-19 US US10342850 No 2019-07-09 2038-05-15 US US10695397 No 2020-06-30 2036-02-03 US US8535695 No 2013-09-17 2029-09-17 US US10238709 No 2019-03-26 2036-02-03 US US9566246 No 2017-02-14 2029-09-17 US US8329198 No 2012-12-11 2029-09-17 US US9265812 No 2016-02-23 2029-09-17 US US11052126 No 2021-07-06 2036-02-03 US US11141457 No 2021-10-12 2040-12-28 US US11338011 No 2016-02-03 2036-02-03 US US11510963 No 2016-02-03 2036-02-03 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 153-156 https://www.chemicalbook.com/ChemicalProductProperty_US_CB0279552.aspx boiling point (°C) 1447 https://www.chemenu.com/products/CM100710
Targets
References
- Casarini AP, Jallad RS, Pinto EM, Soares IC, Nonogaki S, Giannella-Neto D, Musolino NR, Alves VA, Bronstein MD: Acromegaly: correlation between expression of somatostatin receptor subtypes and response to octreotide-lar treatment. Pituitary. 2009;12(4):297-303. doi: 10.1007/s11102-009-0175-1. [Article]
- Mulak A, Larauche M, Biraud M, Million M, Rivier J, Tache Y: Selective agonists of somatostatin receptor subtype 1 or 2 injected peripherally induce antihyperalgesic effect in two models of visceral hypersensitivity in mice. Peptides. 2015 Jan;63:71-80. doi: 10.1016/j.peptides.2014.10.013. Epub 2014 Nov 5. [Article]
- Product monograph: Sandostatin (octreotide acetate) injection [Link]
- NIH StatPearls: Octreotide [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Peroxidase activity
- Specific Function
- Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production o...
- Gene Name
- MPO
- Uniprot ID
- P05164
- Uniprot Name
- Myeloperoxidase
- Molecular Weight
- 83867.71 Da
References
- Alatas E, Alatas O, Colak O: Octreotide inhibits myeloperoxidase activity in rat uterus. Acta Obstet Gynecol Scand. 2000 Jul;79(7):524-7. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- This enzyme action is based on limited findings of in vitro studies and the clinical relevance is unknown.
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Yilmaz B, Kemal Y, Teker F: Be careful before prescribing warfarin and octreotide together: a new drug-drug interaction report. Hippokratia. 2014 Oct-Dec;18(4):377. [Article]
- Liddle C, Goodwin BJ, George J, Tapner M, Farrell GC: Separate and interactive regulation of cytochrome P450 3A4 by triiodothyronine, dexamethasone, and growth hormone in cultured hepatocytes. J Clin Endocrinol Metab. 1998 Jul;83(7):2411-6. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Product monograph: Sandostatin (octreotide acetate) injection [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- Curator comments
- P-glycoprotein is a possible transporter of octreotide, according to the findings of various in vitro studies.
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Gutmann H, Miller DS, Droulle A, Drewe J, Fahr A, Fricker G: P-glycoprotein- and mrp2-mediated octreotide transport in renal proximal tubule. Br J Pharmacol. 2000 Jan;129(2):251-6. doi: 10.1038/sj.bjp.0703003. [Article]
- Yamada T, Kato Y, Kusuhara H, Lemaire M, Sugiyama Y: Characterization of the transport of a cationic octapeptide, octreotide, in rat bile canalicular membrane: possible involvement of P-glycoprotein. Biol Pharm Bull. 1998 Aug;21(8):874-8. doi: 10.1248/bpb.21.874. [Article]
- Dietrich CG, Geier A, Oude Elferink RP: ABC of oral bioavailability: transporters as gatekeepers in the gut. Gut. 2003 Dec;52(12):1788-95. doi: 10.1136/gut.52.12.1788. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- Curator comments
- Octreotide is a substrate and weak inhibitor of MRP2, according to various in vitro studies.
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- Gutmann H, Miller DS, Droulle A, Drewe J, Fahr A, Fricker G: P-glycoprotein- and mrp2-mediated octreotide transport in renal proximal tubule. Br J Pharmacol. 2000 Jan;129(2):251-6. doi: 10.1038/sj.bjp.0703003. [Article]
- Visentin M, Stieger B, Merz M, Kullak-Ublick GA: Octreotide inhibits the bilirubin carriers organic anion transporting polypeptides 1B1 and 1B3 and the multidrug resistance-associated protein 2. J Pharmacol Exp Ther. 2015 Nov;355(2):145-51. doi: 10.1124/jpet.115.227546. Epub 2015 Sep 1. [Article]
- Dietrich CG, Geier A, Oude Elferink RP: ABC of oral bioavailability: transporters as gatekeepers in the gut. Gut. 2003 Dec;52(12):1788-95. doi: 10.1136/gut.52.12.1788. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55