Insulin glargine
Identification
- Summary
Insulin glargine is a modified form of long-acting or basal insulin used to control hyperglycemia in diabetes mellitus.
- Brand Names
- Basaglar, Lantus, Rezvoglar, Semglee, Soliqua, Toujeo
- Generic Name
- Insulin glargine
- DrugBank Accession Number
- DB00047
- Background
Insulin glargine is a long-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Insulin is typically prescribed for the management of diabetes mellitus to mimic the activity of endogenously produced human insulin, a peptide hormone produced by beta cells of the pancreas that promotes glucose metabolism. Insulin is released from the pancreas following a meal to promote the uptake of glucose from the blood into internal organs and tissues such as the liver, fat cells, and skeletal muscle. Absorption of glucose into cells allows for its transformation into glycogen or fat for storage. Insulin also inhibits hepatic glucose production, enhances protein synthesis, and inhibits lipolysis and proteolysis.
Insulin is an important treatment in the management of Type 1 Diabetes (T1D), which is caused by an autoimmune reaction that destroys the beta cells of the pancreas, resulting in the body not being able to produce or synthesize the insulin needed to manage circulating blood sugar levels. As a result, people with T1D rely primarily on exogenous forms of insulin, such as insulin glargine, to lower glucose levels in the blood. Insulin is also used in the treatment of Type 2 Diabetes (T2D), another form of diabetes mellitus that is a slowly progressing metabolic disorder caused by a combination of genetic and lifestyle factors that promote chronically elevated blood sugar levels. Without treatment or improvement in non-pharmacological measures such as diet and exercise to lower blood glucose, high blood sugar eventually causes cellular resistance to endogenous insulin, and in the long term, damage to pancreatic islet cells. Insulin is typically prescribed later in the course of T2D, after several oral medications such as Metformin, Gliclazide, or Sitagliptin have been tried, when sufficient damage has been caused to pancreatic cells that the body is no longer able to produce insulin on its own.
Available as the brand name product Lantus, insulin glargine has a duration of action up to 24 hours allowing for once-daily dosing, typically at bedtime. Due to its duration of action, Lantus is considered "basal insulin" as it provides low concentrations of background insulin that can keep blood sugar stable between meals or overnight. Basal insulin is often combined with short-acting "bolus insulin" such as Insulin lispro, Insulin glulisine, and Insulin aspart to provide higher doses of insulin that are required following meals. Use of basal and bolus insulin together is intended to mimic the pancreas' production of endogenous insulin, with a goal of avoiding any periods of hypoglycemia.
Insulin glargine is also available as the biosimilar, or "follow-on" product, Basaglar in the US and as Abasaglar in the EU. As of 2015, insulin glargine was reformulated by Sanofi as the product Toujeo in an extra-concentrated form containing 300IU/mL (compared to 100IU/mL contained in Lantus). Use of the higher concentrated Toujeo as compared to Lantus results in slightly different pharmacokinetics, with a later onset (up to 6 hours) and duration of action (up to 30 hours). In 2021, another biosimilar, Semglee (insulin glargine-yfgn),12 became the first interchangeable (with Lantus) biosimilar insulin to receive FDA approval.13
Insulin glargine is produced by recombinant DNA technology using a non-pathogenic laboratory strain of Escherichia coli (K12) as the production organism. Insulin glargine differs from endogenous human insulin by the replacement of an asparagine residue at position A21 of the A-chain with glycine and addition of two arginines to the C-terminus (positions B31 and 32) of the B-chain. The resulting protein is soluble at pH 4 and forms microprecipitates at physiological pH 7.4 allowing for the slow release of small amounts of insulin glargine, giving the drug a long duration of action and no pronounced peak concentration.
Without an adequate supply of insulin to promote absorption of glucose from the bloodstream, blood sugar levels can climb to dangerously high levels and can result in symptoms such as fatigue, headache, blurred vision, and increased thirst. If left untreated, the body starts to break down fat, instead of glucose, for energy which results in a build-up of ketone acids in the blood and a syndrome called ketoacidosis, which is a life-threatening medical emergency. In the long term, elevated blood sugar levels increase the risk of heart attack, stroke, and diabetic neuropathy.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Hormones / Insulins - Protein Structure
- Protein Chemical Formula
- C267H404N72O78S6
- Protein Average Weight
- 6063.0 Da
- Sequences
- Synonyms
- Insulin glargine
- Insulin glargine (rDNA origin)
- Insulin glargine recombinant
- insulin glargine-yfgn
- Insulina glargina
- External IDs
- HOE 71GT
- HOE 901
- HOE-71GT
- HOE-901
- LY 2963016
- LY-2963016
- LY2963016
- MK-1293
- MYL-1501D
Pharmacology
- Indication
Insulin glargine is indicated to improve glycemic control in adults and pediatric patients with type 1 diabetes mellitus and in adults with type 2 diabetes mellitus.11,14,15
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 Diabetes mellitus ••• ••• ••••• ••••••• ••••••••••• ••••••• ••• ••• ••••••• •• ••••••••••••• ••••••••• Management of Diabetes mellitus •••••••••••• •••••••••• •••••••• Management of Type 1 insulin-dependent diabetes mellitus ••• ••• •••••••• •••••••• ••• ••••••• ••••••••••• ••••••• ••• ••• •••••••••• •• ••••••••••••• ••••••••• Management of Type 1 insulin-dependent diabetes mellitus •••••••••••• •••••• •••••••• •••••••••• •••••••• Management of Type 2 diabetes mellitus •••••••••••• ••••• •••••••••• •••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, the pancreas produces a continuous supply of low levels of basal insulin along with spikes of insulin following meals. Increased insulin secretion following meals is responsible for the metabolic changes that occur as the body transitions from a postabsorptive to absorptive state. Insulin promotes cellular uptake of glucose, particularly in muscle and adipose tissues, promotes energy storage via glycogenesis, opposes catabolism of energy stores, increases DNA replication and protein synthesis by stimulating amino acid uptake by liver, muscle and adipose tissue, and modifies the activity of numerous enzymes involved in glycogen synthesis and glycolysis. Insulin also promotes growth and is required for the actions of growth hormone (e.g. protein synthesis, cell division, DNA synthesis). Insulin glargine is a long-acting insulin analogue with a flat and predictable action profile. It is used to mimic the basal levels of insulin in diabetic individuals.
- Mechanism of action
Insulin glargine binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor autophosphorylates and phosphorylates numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. Activation of these proteins leads to the activation of downstream signalling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC), both of which play critical roles in metabolism. Insulin glargine is completely soluble at pH 4, the pH of administered solution, and has low solubility at physiological pH 7.4. Upon subcuteous injection, the solution is neutralized resulting in the formation of microprecipitates. Small amounts of insulin glargine are released from microprecipitates giving the drug a relatively constant concentration over time profile over 24 hours with no pronounced peak. This release mechanism allows the drug to mimic basal insulin levels within the body.
Target Actions Organism AInsulin receptor agonistHumans UInsulin-like growth factor 1 receptor activatorHumans - Absorption
Because of the modifications to the A and B chain, the isoelectric point shifts towards a neutral pH and insulin glargine is more stable in acidic conditions than regular insulin. As insulin glargine is less soluble at neutral pH, once injected, forms microprecipitates. Slow release of insulin glargine from microprecipitates provides a relatively constant concentration of insulin over 24 hours. Onset of action is approximately 1.1 hours.
The pharmacokinetic profiles for single 0.4, 0.6, and 0.9 U/kg doses of Toujeo in 24 patients with type 1 diabetes mellitus was evaluated in a euglycemic clamp study. The median time to maximum serum insulin concentration was 12 (8–14), 12 (12–18), and 16 (12–20) hours, respectively. Steady-state insulin concentrations are reached by at least 5 days of once-daily subcutaneous administration of 0.4 U/kg to 0.6 U/kg doses of Toujeo over 8 days in patients with type 1 diabetes mellitus.
The median time to maximum effect of Basaglar (measured by the peak rate of glucose infusion) was approximately 12.0 hours. The pharmacodynamic profile of Basaglar following subcutaneous injection demonstrated sustained glucose lowering activity over 24 hours with no pronounced peak. The mean area under the glucose infusion rate curves (measure of overall pharmacodynamic effect) and maximum glucose infusion rate were 1670 mg/kg and 2.12 mg/kg/min, respectively. On average, serum insulin concentrations declined to baseline by approximately 24 hours.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Insulin glargine is metabolized in the liver into two active metabolites with similar activity to insulin: 21a-Gly-human insulin (M1) and 21a-Gly-des-30b- threonine insulin (M2), with M1 being the predominant metabolite.
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- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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- Toxicity
Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Neuroglycopenic signs and symptoms of hypoglycemia include difficulty concentrating, lethargy/weakness, confusion, drowsiness, vision changes, difficulty speaking, headache, and dizziness. Mild hypoglycemia is characterized by the presence of autonomic symptoms. Moderate hypoglycemia is characterized by the presence of autonomic and neuroglycopenic symptoms. Individuals may become unconscious in severe cases of hypoglycemia. Other adverse events that may occur include allergic reaction, injection site reaction, lipodystrophy, pruritis, and rash.
- 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 softwareAcarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Insulin glargine. Acebutolol The therapeutic efficacy of Insulin glargine can be increased when used in combination with Acebutolol. Acetazolamide The risk or severity of hypoglycemia can be increased when Acetazolamide is combined with Insulin glargine. Acetohexamide The risk or severity of hypoglycemia can be increased when Acetohexamide is combined with Insulin glargine. Acetophenazine The therapeutic efficacy of Insulin glargine can be decreased when used in combination with Acetophenazine. - Food Interactions
- No interactions found.
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.
- International/Other Brands
- Lantus R / Lusduna Nexvue / Optisulin / Semglee (Mylan Pharmaceuticals Inc.)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Abasaglar Injection, solution 100 Units/ml Subcutaneous Eli Lilly Nederland B.V. 2016-09-07 Not applicable EU Abasaglar Injection, solution 100 Units/ml Subcutaneous Eli Lilly Nederland B.V. 2020-12-15 Not applicable EU Abasaglar Injection, solution 100 Units/ml Subcutaneous Eli Lilly Nederland B.V. 2016-09-07 Not applicable EU Abasaglar Injection, solution 100 Units/ml Subcutaneous Eli Lilly Nederland B.V. 2016-09-07 Not applicable EU Abasaglar Injection, solution 100 Units/ml Subcutaneous Eli Lilly Nederland B.V. 2016-09-07 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Soliqua Insulin glargine (100 unit / mL) + Lixisenatide (33 mcg / mL) Solution Subcutaneous Sanofi Aventis 2018-09-12 Not applicable Canada Soliqua 100/33 Insulin glargine (100 U/1mL) + Lixisenatide (33 ug/1mL) Injection, solution Subcutaneous sanofi-aventis U.S. LLC 2016-11-21 Not applicable US SOLİQUA SOLOSTAR 100 U/ML + 33 MCG/ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM, 3 KALEM Insulin glargine (100 U/mL) + Lixisenatide (33 mcg/mL) Injection, solution Subcutaneous SANOFİ SAĞLIK ÜRÜNLERİ LTD. ŞTİ. 2018-02-08 Not applicable Turkey SOLİQUA SOLOSTAR 100 U/ML + 33 MCG/ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM, 5 KALEM Insulin glargine (100 U/mL) + Lixisenatide (33 mcg/mL) Injection, solution Subcutaneous SANOFİ SAĞLIK ÜRÜNLERİ LTD. ŞTİ. 2020-08-14 Not applicable Turkey SOLİQUA SOLOSTAR 100 U/ML + 50 MCG/ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM, 3 KALEM Insulin glargine (100 U/mL) + Lixisenatide (50 mcg/mL) Injection, solution Subcutaneous SANOFİ SAĞLIK ÜRÜNLERİ LTD. ŞTİ. 2018-02-08 Not applicable Turkey
Categories
- ATC Codes
- A10AE54 — Insulin glargine and lixisenatide
- A10AE — Insulins and analogues for injection, long-acting
- A10A — INSULINS AND ANALOGUES
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Alimentary Tract and Metabolism
- Amino Acids, Peptides, and Proteins
- Antimetabolites
- Biological Products
- Blood Glucose Lowering Agents
- Complex Mixtures
- Cytochrome P-450 CYP1A2 Inducers
- Cytochrome P-450 CYP1A2 Inducers (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Drugs Used in Diabetes
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypoglycemia-Associated Agents
- Hypolipidemic Agents
- Insulin
- Insulin Analog
- Insulin, Long-Acting
- Lipid Regulating Agents
- Pancreatic Hormones
- Peptide Hormones
- Peptides
- 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
- 2ZM8CX04RZ
- CAS number
- 160337-95-1
References
- General References
- Chatterjee S, Tringham JR, Davies MJ: Insulin glargine and its place in the treatment of Types 1 and 2 diabetes mellitus. Expert Opin Pharmacother. 2006 Jul;7(10):1357-71. [Article]
- Dunn CJ, Plosker GL, Keating GM, McKeage K, Scott LJ: Insulin glargine: an updated review of its use in the management of diabetes mellitus. Drugs. 2003;63(16):1743-78. [Article]
- Home PD, Ashwell SG: An overview of insulin glargine. Diabetes Metab Res Rev. 2002 Sep-Oct;18 Suppl 3:S57-63. [Article]
- Jones R: Insulin glargine (Aventis Pharma). IDrugs. 2000 Sep;3(9):1081-7. [Article]
- Wang F, Carabino JM, Vergara CM: Insulin glargine: a systematic review of a long-acting insulin analogue. Clin Ther. 2003 Jun;25(6):1541-77, discussion 1539-40. [Article]
- Warren E, Weatherley-Jones E, Chilcott J, Beverley C: Systematic review and economic evaluation of a long-acting insulin analogue, insulin glargine. Health Technol Assess. 2004 Nov;8(45):iii, 1-57. [Article]
- Owens DR, Bolli GB: Beyond the era of NPH insulin--long-acting insulin analogs: chemistry, comparative pharmacology, and clinical application. Diabetes Technol Ther. 2008 Oct;10(5):333-49. doi: 10.1089/dia.2008.0023. [Article]
- Pettus J, Santos Cavaiola T, Tamborlane WV, Edelman S: The past, present, and future of basal insulins. Diabetes Metab Res Rev. 2016 Sep;32(6):478-96. doi: 10.1002/dmrr.2763. Epub 2015 Nov 25. [Article]
- Leto D, Saltiel AR: Regulation of glucose transport by insulin: traffic control of GLUT4. Nat Rev Mol Cell Biol. 2012 May 23;13(6):383-96. doi: 10.1038/nrm3351. [Article]
- Wiesli P, Schories M: Improved Glycemic Control with Insulin Glargine 300 U/mL (Toujeo((R))) in Patients with Type 2 Diabetes: Real-World Effectiveness in Switzerland. Diabetes Ther. 2018 Dec;9(6):2325-2334. doi: 10.1007/s13300-018-0518-x. Epub 2018 Oct 9. [Article]
- FDA Approved Drug Products: Lantus (Insulin glargine) for subcutaneous injection [Link]
- FDA Approved Drug Products: Semglee (insulin glargine-yfgn) for subcutaneous injection [Link]
- FDA Press Announcement: FDA Approves First Interchangeable Biosimilar Insulin Product for Treatment of Diabetes [Link]
- Health Canada Approved Drug Products: LANTUS (insulin glargine, rDNA origin) solution for injection [Link]
- Health Canada Approved Drug Products: Semglee (insulin glargine-yfgn) solution for subcutaneous injection [Link]
- External Links
- KEGG Drug
- D03250
- PubChem Substance
- 46507981
- 274783
- ChEMBL
- CHEMBL1201497
- Therapeutic Targets Database
- DAP001088
- PharmGKB
- PA449992
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Insulin_glargine
- FDA label
- Download (51.2 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 Active Not Recruiting Treatment Hyperglycemia / Type 2 Diabetes Mellitus 1 4 Active Not Recruiting Treatment Type 1 Diabetes Mellitus 1 4 Active Not Recruiting Treatment Type 2 Diabetes Mellitus 1 4 Completed Basic Science Type 2 Diabetes Mellitus 1 4 Completed Health Services Research Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Sanofi aventis us llc
- Packagers
- Gruppo Lepetit SPA
- Physicians Total Care Inc.
- Sanofi-Aventis Inc.
- Dosage Forms
Form Route Strength Injection, solution Parenteral 100 IU/ML Solution Subcutaneous 100 IU Solution Subcutaneous 100 iu/1ml Solution Subcutaneous 100 UI Injection Injection 100 IU/ml Solution Subcutaneous 3.640 mg Injection Intramuscular Injection Intramuscular 100 U/mL Solution Subcutaneous 100 IU/mL Injection, solution Subcutaneous 300 [iU]/1mL Injection Subcutaneous Injection, solution Parenteral; Subcutaneous 100 U/ML Injection, solution Parenteral; Subcutaneous 100 IU/ML Injection, solution Subcutaneous 100 [iU]/1mL Solution Subcutaneous 100 U Solution Subcutaneous 100 unit / mL Solution Subcutaneous 1000 U Injection Subcutaneous 100 iu/ml Injection, solution Subcutaneous 100 iu/ml Injection, solution Subcutaneous Solution Subcutaneous 10000000 IU Injection, solution Subcutaneous 100 U/ML Injection, solution Subcutaneous 100 Units/mL Injection, solution 100 Units/ml Injection, solution Subcutaneous 100 iu/1ml Injection, solution Subcutaneous 3.64 mg/ml Injection, solution Solution Subcutaneous Injection, solution Subcutaneous Injection, solution Subcutaneous 100 units/ml Injection, solution Cutaneous; Parenteral Injection, solution Parenteral; Subcutaneous 100 UI/ML Injection, solution Parenteral; Subcutaneous 300 IU/ML Solution Subcutaneous 300 U Injection, solution Subcutaneous 300 U/ML Injection, solution Subcutaneous 300 U/1mL Solution Subcutaneous 300 unit / mL Injection, solution Subcutaneous 300 Units/ml Solution Subcutaneous 3.64 mg Injection, solution 100 iu/1ml Injection, solution 300 iu/1ml - Prices
Unit description Cost Unit Lantus SoloStar 100 unit/ml Solution 1 Box = Five 3ml Syringes 223.89USD box Lantus 100 unit/ml Solution 10ml Vial 111.88USD vial Lantus for OptiClik 100 unit/ml Solution 3ml Cartridge 44.78USD cartridge Lantus 100 unit/ml cartridge 14.35USD ml Lantus solostar 100 unit/ml 14.35USD 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 US6100376 No 2000-08-08 2009-11-06 US CA1339044 No 1997-04-01 2014-04-01 Canada US9011391 No 2015-04-21 2024-03-26 US US9233211 No 2016-01-12 2024-03-02 US US8603044 No 2013-12-10 2024-03-02 US US8512297 No 2013-08-20 2024-09-15 US US8679069 No 2014-03-25 2025-04-12 US US8992486 No 2015-03-31 2024-06-05 US US8556864 No 2013-10-15 2024-03-03 US US7918833 Yes 2011-04-05 2028-03-23 US US7713930 Yes 2010-05-11 2023-12-13 US US7476652 Yes 2009-01-13 2024-01-23 US US9561331 No 2017-02-07 2024-08-28 US US9623189 No 2017-04-18 2024-08-19 US US9610409 No 2017-04-04 2024-03-02 US US9526844 No 2016-12-27 2024-03-02 US US9604008 No 2017-03-28 2024-03-02 US US9533105 No 2017-01-03 2024-08-17 US US9408979 No 2016-08-09 2024-03-02 US US9604009 No 2017-03-28 2024-08-16 US USRE45313 No 2014-12-30 2020-07-12 US US9526764 No 2016-12-27 2029-10-09 US US9345750 No 2016-05-24 2031-05-18 US US9707176 No 2017-07-18 2030-11-11 US US9775954 No 2017-10-03 2024-03-02 US US9827379 No 2017-11-28 2024-03-02 US US9821032 No 2017-11-21 2032-05-09 US US9950039 No 2018-04-24 2035-12-10 US US9717852 No 2017-08-01 2033-04-08 US US10029011 No 2018-07-24 2032-08-02 US US10117909 No 2018-11-06 2029-10-09 US US10369291 No 2019-08-06 2035-09-16 US
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 81 °C Khachidze, D.G. et al., J. Biol. Phys. Chem. 1:64-67 (2001) hydrophobicity 0.098 Not Available isoelectric point 6.88 Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor signaling protein tyrosine kinase activity
- Specific Function
- Receptor tyrosine kinase which mediates the pleiotropic actions of insulin. Binding of insulin leads to phosphorylation of several intracellular substrates, including, insulin receptor substrates (...
- Gene Name
- INSR
- Uniprot ID
- P06213
- Uniprot Name
- Insulin receptor
- Molecular Weight
- 156331.465 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Le Roith D: Insulin glargine and receptor-mediated signalling: clinical implications in treating type 2 diabetes. Diabetes Metab Res Rev. 2007 Nov;23(8):593-9. [Article]
- Sciacca L, Cassarino MF, Genua M, Pandini G, Le Moli R, Squatrito S, Vigneri R: Insulin analogues differently activate insulin receptor isoforms and post-receptor signalling. Diabetologia. 2010 Aug;53(8):1743-53. doi: 10.1007/s00125-010-1760-6. Epub 2010 Apr 28. [Article]
- Wada T, Azegami M, Sugiyama M, Tsuneki H, Sasaoka T: Characteristics of signalling properties mediated by long-acting insulin analogue glargine and detemir in target cells of insulin. Diabetes Res Clin Pract. 2008 Sep;81(3):269-77. doi: 10.1016/j.diabres.2008.05.007. Epub 2008 Jun 27. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Activator
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Receptor tyrosine kinase which mediates actions of insulin-like growth factor 1 (IGF1). Binds IGF1 with high affinity and IGF2 and insulin (INS) with a lower affinity. The activated IGF1R is involv...
- Gene Name
- IGF1R
- Uniprot ID
- P08069
- Uniprot Name
- Insulin-like growth factor 1 receptor
- Molecular Weight
- 154791.73 Da
References
- Varewijck AJ, Janssen JA: Insulin and its analogues and their affinities for the IGF1 receptor. Endocr Relat Cancer. 2012 Sep 5;19(5):F63-75. doi: 10.1530/ERC-12-0026. Print 2012 Oct. [Article]
- Ciaraldi TP, Sasaoka T: Review on the in vitro interaction of insulin glargine with the insulin/insulin-like growth factor system: potential implications for metabolic and mitogenic activities. Horm Metab Res. 2011 Jan;43(1):1-10. doi: 10.1055/s-0030-1267203. Epub 2010 Oct 11. [Article]
- Le Roith D: Insulin glargine and receptor-mediated signalling: clinical implications in treating type 2 diabetes. Diabetes Metab Res Rev. 2007 Nov;23(8):593-9. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- 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 oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Barnett CR, Wilson J, Wolf CR, Flatt PR, Ioannides C: Hyperinsulinaemia causes a preferential increase in hepatic P4501A2 activity. Biochem Pharmacol. 1992 Mar 17;43(6):1255-61. doi: 10.1016/0006-2952(92)90500-i. [Article]
- Pass GJ, Becker W, Kluge R, Linnartz K, Plum L, Giesen K, Joost HG: Effect of hyperinsulinemia and type 2 diabetes-like hyperglycemia on expression of hepatic cytochrome p450 and glutathione s-transferase isoforms in a New Zealand obese-derived mouse backcross population. J Pharmacol Exp Ther. 2002 Aug;302(2):442-50. doi: 10.1124/jpet.102.033553. [Article]
- Flockhart Table of Drug Interactions [Link]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55