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
>A chain
GIVEQCCTSICSLYQLENYCG
>B chain
FVNQHLCGSHLVEALYLVCGERGFFYTPKTRR
Download FASTA Format
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

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofDiabetes mellitus••• ••••••••••••••• ••••••••••• ••••••• ••• ••• ••••••• •• ••••••••••••••••••••••
Management ofDiabetes mellitus•••••••••••••••••••••• ••••••••
Management ofType 1 insulin-dependent diabetes mellitus••• ••••••••••••••••••• ••• ••••••• ••••••••••• ••••••• ••• ••• •••••••••• •• ••••••••••••••••••••••
Management ofType 1 insulin-dependent diabetes mellitus•••••••••••••••••• •••••••••••••••••• ••••••••
Management ofType 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.

TargetActionsOrganism
AInsulin receptor
agonist
Humans
UInsulin-like growth factor 1 receptor
activator
Humans
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
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Insulin glargine.
AcebutololThe therapeutic efficacy of Insulin glargine can be increased when used in combination with Acebutolol.
AcetazolamideThe risk or severity of hypoglycemia can be increased when Acetazolamide is combined with Insulin glargine.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Acetohexamide is combined with Insulin glargine.
AcetophenazineThe therapeutic efficacy of Insulin glargine can be decreased when used in combination with Acetophenazine.
Food Interactions
No interactions found.

Products

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International/Other Brands
Lantus R / Lusduna Nexvue / Optisulin / Semglee (Mylan Pharmaceuticals Inc.)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2016-09-072020-10-02EU flag
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2016-09-07Not applicableEU flag
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2016-09-07Not applicableEU flag
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2016-09-07Not applicableEU flag
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2016-09-07Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
SoliquaInsulin glargine (100 unit / mL) + Lixisenatide (33 mcg / mL)SolutionSubcutaneousSanofi Aventis2018-09-12Not applicableCanada flag
Soliqua 100/33Insulin glargine (100 U/1mL) + Lixisenatide (33 ug/1mL)Injection, solutionSubcutaneoussanofi-aventis U.S. LLC2016-11-21Not applicableUS flag
SOLİQUA SOLOSTAR 100 U/ML + 33 MCG/ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM, 3 KALEMInsulin glargine (100 U/mL) + Lixisenatide (33 mcg/mL)Injection, solutionSubcutaneousSANOFİ SAĞLIK ÜRÜNLERİ LTD. ŞTİ.2018-02-08Not applicableTurkey flag
SOLİQUA SOLOSTAR 100 U/ML + 33 MCG/ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM, 5 KALEMInsulin glargine (100 U/mL) + Lixisenatide (33 mcg/mL)Injection, solutionSubcutaneousSANOFİ SAĞLIK ÜRÜNLERİ LTD. ŞTİ.2020-08-14Not applicableTurkey flag
SOLİQUA SOLOSTAR 100 U/ML + 50 MCG/ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM, 3 KALEMInsulin glargine (100 U/mL) + Lixisenatide (50 mcg/mL)Injection, solutionSubcutaneousSANOFİ SAĞLIK ÜRÜNLERİ LTD. ŞTİ.2018-02-08Not applicableTurkey flag

Categories

ATC Codes
A10AE54 — Insulin glargine and lixisenatideA10AE04 — Insulin glargine
Drug Categories
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
  1. 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]
  2. 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]
  3. Home PD, Ashwell SG: An overview of insulin glargine. Diabetes Metab Res Rev. 2002 Sep-Oct;18 Suppl 3:S57-63. [Article]
  4. Jones R: Insulin glargine (Aventis Pharma). IDrugs. 2000 Sep;3(9):1081-7. [Article]
  5. 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]
  6. 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]
  7. 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]
  8. 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]
  9. 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]
  10. 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]
  11. FDA Approved Drug Products: Lantus (Insulin glargine) for subcutaneous injection [Link]
  12. FDA Approved Drug Products: Semglee (insulin glargine-yfgn) for subcutaneous injection [Link]
  13. FDA Press Announcement: FDA Approves First Interchangeable Biosimilar Insulin Product for Treatment of Diabetes [Link]
  14. Health Canada Approved Drug Products: LANTUS (insulin glargine, rDNA origin) solution for injection [Link]
  15. Health Canada Approved Drug Products: Semglee (insulin glargine-yfgn) solution for subcutaneous injection [Link]
KEGG Drug
D03250
PubChem Substance
46507981
RxNav
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
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentHyperglycemia / Type 2 Diabetes Mellitus1
4Active Not RecruitingTreatmentType 2 Diabetes Mellitus1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedHealth Services ResearchType 2 Diabetes Mellitus1
4CompletedPreventionCoronary Artery Disease (CAD)1

Pharmacoeconomics

Manufacturers
  • Sanofi aventis us llc
Packagers
  • Gruppo Lepetit SPA
  • Physicians Total Care Inc.
  • Sanofi-Aventis Inc.
Dosage Forms
FormRouteStrength
Injection, solutionParenteral100 IU/ML
SolutionSubcutaneous100 IU
SolutionSubcutaneous100 iu/1ml
SolutionSubcutaneous100 UI
Injection
Injection100 IU/ml
SolutionSubcutaneous3.640 mg
InjectionIntramuscular
InjectionIntramuscular100 U/mL
SolutionSubcutaneous100 IU/mL
Injection, solutionSubcutaneous300 [iU]/1mL
InjectionSubcutaneous
Injection, solutionParenteral; Subcutaneous100 U/ML
Injection, solutionParenteral; Subcutaneous100 IU/ML
Injection, solutionSubcutaneous100 [iU]/1mL
SolutionSubcutaneous100 U
SolutionSubcutaneous100 unit / mL
SolutionSubcutaneous1000 U
InjectionSubcutaneous100 iu/ml
Injection, solutionSubcutaneous100 iu/ml
Injection, solutionSubcutaneous
SolutionSubcutaneous10000000 IU
Injection, solutionSubcutaneous100 U/ML
Injection, solutionSubcutaneous100 Units/mL
Injection, solution100 Units/ml
Injection, solutionSubcutaneous100 iu/1ml
Injection, solutionSubcutaneous3.64 mg/ml
Injection, solution
SolutionSubcutaneous
Injection, solutionSubcutaneous
Injection, solutionSubcutaneous100 units/ml
Injection, solutionCutaneous; Parenteral
Injection, solutionParenteral; Subcutaneous100 UI/ML
Injection, solutionParenteral; Subcutaneous300 IU/ML
SolutionSubcutaneous300 U
Injection, solutionSubcutaneous300 U/ML
Injection, solutionSubcutaneous300 U/1mL
SolutionSubcutaneous300 unit / mL
Injection, solutionSubcutaneous300 Units/ml
SolutionSubcutaneous3.64 mg
Injection, solution100 iu/1ml
Injection, solution300 iu/1ml
Prices
Unit descriptionCostUnit
Lantus SoloStar 100 unit/ml Solution 1 Box = Five 3ml Syringes223.89USD box
Lantus 100 unit/ml Solution 10ml Vial111.88USD vial
Lantus for OptiClik 100 unit/ml Solution 3ml Cartridge44.78USD cartridge
Lantus 100 unit/ml cartridge14.35USD ml
Lantus solostar 100 unit/ml14.35USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6100376No2000-08-082009-11-06US flag
CA1339044No1997-04-012014-04-01Canada flag
US9011391No2015-04-212024-03-26US flag
US9233211No2016-01-122024-03-02US flag
US8603044No2013-12-102024-03-02US flag
US8512297No2013-08-202024-09-15US flag
US8679069No2014-03-252025-04-12US flag
US8992486No2015-03-312024-06-05US flag
US8556864No2013-10-152024-03-03US flag
US7918833Yes2011-04-052028-03-23US flag
US7713930Yes2010-05-112023-12-13US flag
US7476652Yes2009-01-132024-01-23US flag
US9561331No2017-02-072024-08-28US flag
US9623189No2017-04-182024-08-19US flag
US9610409No2017-04-042024-03-02US flag
US9526844No2016-12-272024-03-02US flag
US9604008No2017-03-282024-03-02US flag
US9533105No2017-01-032024-08-17US flag
US9408979No2016-08-092024-03-02US flag
US9604009No2017-03-282024-08-16US flag
USRE45313No2014-12-302020-07-12US flag
US9526764No2016-12-272029-10-09US flag
US9345750No2016-05-242031-05-18US flag
US9707176No2017-07-182030-11-11US flag
US9775954No2017-10-032024-03-02US flag
US9827379No2017-11-282024-03-02US flag
US9821032No2017-11-212032-05-09US flag
US9950039No2018-04-242035-12-10US flag
US9717852No2017-08-012033-04-08US flag
US10029011No2018-07-242032-08-02US flag
US10117909No2018-11-062029-10-09US flag
US10369291No2019-08-062035-09-16US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)81 °CKhachidze, D.G. et al., J. Biol. Phys. Chem. 1:64-67 (2001)
hydrophobicity0.098Not Available
isoelectric point6.88Not Available

Targets

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insights and accelerate drug research.
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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
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. 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]
  3. 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]
  4. 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
  1. 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]
  2. 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]
  3. 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
  1. 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]
  2. 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]
  3. Flockhart Table of Drug Interactions [Link]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48