Identification

Name
Insulin Glargine
Accession Number
DB00047  (BTD00045, BIOD00045, DB01308)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Hormones / Insulins
Description

Insulin glargine is produced by recombinant DNA technology using a non-pathogenic laboratory strain of Escherichia coli (K12) as the production organism. It is an analogue of human insulin made by replacing the asparagine residue at position A21 of the A-chain with glycine and adding 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. Small amounts of insulin glargine are slowly released from microprecipitates giving the drug a long duration of action (up to 24 hours) and no pronounced peak concentration.

Protein structure
Db00047
Protein chemical formula
C267H404N72O78S6
Protein average weight
6063.0 Da
Sequences
>A chain
GIVEQCCTSICSLYQLENYCG
>B chain
FVNQHLCGSHLVEALYLVCGERGFFYTPKTRR
Download FASTA Format
Synonyms
  • Insulin Glargine (rDNA origin)
  • Insulin glargine recombinant
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
AbasaglarInjection, solution100 Units/mlSubcutaneousEli Lilly Nederland B.V.2014-09-09Not applicableEu
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Soliqua 100/33Insulin Glargine (100 U/1mL) + Lixisenatide (33 ug/1mL)Injection, solutionSubcutaneousSanofi Aventis2016-11-21Not applicableUs
International/Other Brands
Lantus OptiSet
Categories
UNII
2ZM8CX04RZ
CAS number
160337-95-1

Pharmacology

Indication

For the treatment of Type 1 or 2 diabetes mellitus in patients over 17 years old who require a long-acting (basal) insulin for the control of hyperglycemia. May be used in pediatric patients with Type 1 diabetes mellitus who require a long-acting (basal) insulin for glycemic control.

Associated Conditions
Pharmacodynamics

Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, a basal level of insulin is supplemented with insulin spikes 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. The onset of action of insulin glargine is approximately 90 minutes and its duration of action is up to 24 hours. The action profile of insulin glargine is peakless. The significance of this finding is that insulin glargine has a lower chance of nocturnal hypoglycemia.

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 signaling 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
Human
UInsulin-like growth factor 1 receptor
agonist
Human
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.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Partly metabolized to two active metabolites with similar in vitro activity to insulin: A21-Gly-insulin and A21-Gly-des-B30-Thr-insulin.

Route of elimination
Not Available
Half life

Not reported in humans; 30 hours in vitro in mammalian reticulocytes.

Clearance
Not Available
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.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,4-thiazolidinedione2,4-thiazolidinedione may increase the hypoglycemic activities of Insulin Glargine.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Insulin Glargine can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
AcarboseAcarbose may increase the hypoglycemic activities of Insulin Glargine.
AcebutololAcebutolol may increase the hypoglycemic activities of Insulin Glargine.
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Insulin Glargine.
Acetyl sulfisoxazoleThe therapeutic efficacy of Insulin Glargine can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Insulin Glargine.
AICA ribonucleotideAICA ribonucleotide may increase the hypoglycemic activities of Insulin Glargine.
AlaproclateAlaproclate may increase the hypoglycemic activities of Insulin Glargine.
AlbiglutideAlbiglutide may increase the hypoglycemic activities of Insulin Glargine.
Food Interactions
Not Available

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. [PubMed:16805721]
  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. [PubMed:12904090]
  3. Home PD, Ashwell SG: An overview of insulin glargine. Diabetes Metab Res Rev. 2002 Sep-Oct;18 Suppl 3:S57-63. [PubMed:12324987]
  4. Jones R: Insulin glargine (Aventis Pharma). IDrugs. 2000 Sep;3(9):1081-7. [PubMed:16049868]
  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. [PubMed:12860485]
  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. [PubMed:15525480]
  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. [PubMed:18715209]
External Links
KEGG Drug
D03250
PubChem Substance
46507981
ChEMBL
CHEMBL1201497
Therapeutic Targets Database
DAP001088
PharmGKB
PA449992
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
ATC Codes
A10AE04 — Insulin glargine
AHFS Codes
  • 68:20.08 — Insulins
FDA label
Download (51.2 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingPreventionRetinopathy, Diabetic1
0RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
1CompletedNot AvailableDiabetes Mellitus (DM)1
1CompletedNot AvailableDiabetes, Diabetes Mellitus Type 12
1CompletedBasic ScienceDiabetes, Diabetes Mellitus Type 14
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceType 2 Diabetes Mellitus2
1CompletedTreatmentDelivery Systems / Diabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
1CompletedTreatmentDiabetes Mellitus (DM)2
1CompletedTreatmentDiabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 19
1CompletedTreatmentDiabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 1 / Healthy Volunteers2
1CompletedTreatmentDiabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 1 / Type 2 Diabetes Mellitus1
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers2
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers / Type 2 Diabetes Mellitus2
1CompletedTreatmentDiabetes Mellitus (DM) / Hyperglycemias1
1CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus3
1CompletedTreatmentDiabetes, Diabetes Mellitus Type 14
1CompletedTreatmentType 2 Diabetes Mellitus5
1Not Yet RecruitingBasic ScienceHealthy Volunteers1
1RecruitingBasic ScienceType 2 Diabetes Mellitus1
1TerminatedBasic ScienceHealthy Volunteers1
2CompletedNot AvailableDiabetes, Diabetes Mellitus Type 11
2CompletedTreatmentDiabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 11
2CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus3
2CompletedTreatmentDiabetes, Diabetes Mellitus Type 13
2CompletedTreatmentNonalcoholic Fatty Liver Disease / Nonalcoholic Steatohepatitis / Type 2 Diabetes Mellitus1
2CompletedTreatmentType 2 Diabetes Mellitus6
2RecruitingTreatmentDiabetes Mellitus (DM)1
2TerminatedTreatmentType 2 Diabetes Mellitus1
2, 3CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
3Active Not RecruitingTreatmentComparative Effectiveness of Glycemia-lowering Medications / Type 2 Diabetes Mellitus1
3Active Not RecruitingTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus2
3Active Not RecruitingTreatmentDiabetes, Diabetes Mellitus Type 13
3Active Not RecruitingTreatmentType 2 Diabetes Mellitus5
3CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Blood Cholesterol Level / High Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
3CompletedTreatmentCardiovascular Disease (CVD) / Hyperglycemias / Myocardial Infarction1
3CompletedTreatmentChronic Kidney Disease (CKD) / Type 2 Diabetes Mellitus1
3CompletedTreatmentDawn Phenomenon / Diabetes, Diabetes Mellitus Type 11
3CompletedTreatmentDiabetes Mellitus (DM)4
3CompletedTreatmentDiabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 16
3CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus27
3CompletedTreatmentDiabetes Mellitus, Insulin-Dependent1
3CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent1
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 112
3CompletedTreatmentPoor Glycemic Control1
3CompletedTreatmentType 2 Diabetes Mellitus60
3RecruitingTreatmentDiabetes, Diabetes Mellitus Type 13
3RecruitingTreatmentHyperglycemias / Stroke, Acute1
3RecruitingTreatmentType 1 Diabetes Mellitus-Type 2 Diabetes Mellitus1
3RecruitingTreatmentType 2 Diabetes Mellitus8
3TerminatedTreatmentAMI1
3TerminatedTreatmentDiabetes, Diabetes Mellitus Type 11
3TerminatedTreatmentHyperglycemias1
3TerminatedTreatmentLeukemias / Malignant Lymphomas1
3TerminatedTreatmentType 2 Diabetes Mellitus2
3Unknown StatusTreatmentCystic Fibrosis (CF) / Glucose tolerance impaired1
3Unknown StatusTreatmentType I Diabetes1
3WithdrawnSupportive CareHyperglycemias / Leukemias1
3WithdrawnTreatmentType 2 Diabetes Mellitus1
4Active Not RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
4Active Not RecruitingTreatmentDiabetes, Diabetes Mellitus Type 1 / Nocturnal Hypoglycemia / Recurrent Severe Hypoglycaemia1
4Active Not RecruitingTreatmentType2 Diabetes1
4CompletedNot AvailableType 2 Diabetes Mellitus1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedPreventionCoronary Artery Disease1
4CompletedPreventionHyperglycemias1
4CompletedScreeningDiabetes Mellitus (DM)1
4CompletedTreatmentAcute Myocardial Infarction (AMI) / Type 2 Diabetes Mellitus1
4CompletedTreatmentCardiovascular Disease (CVD) / Endothelial Dysfunction / Type 2 Diabetes Mellitus1
4CompletedTreatmentCongestive Heart Failure (CHF) / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus (DM)12
4CompletedTreatmentDiabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 11
4CompletedTreatmentDiabetes Mellitus (DM) / General Surgery1
4CompletedTreatmentDiabetes Mellitus (DM) / Hyperglycemias2
4CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus6
4CompletedTreatmentDiabetes, Diabetes Mellitus Type 110
4CompletedTreatmentHospitalization / Hyperglycemias / Type 2 Diabetes Mellitus1
4CompletedTreatmentHyperglycemias1
4CompletedTreatmentHyperglycemias / Type 2 Diabetes Mellitus1
4CompletedTreatmentHypoglycemia / Type 2 Diabetes Mellitus1
4CompletedTreatmentImpaired Renal Function / Type 2 Diabetes Mellitus1
4CompletedTreatmentInpatient Hyperglycemia / Type 2 Diabetes Mellitus1
4CompletedTreatmentNon-Alcoholic Fatty Liver Disease (NAFLD)1
4CompletedTreatmentSecondary Drug Failure / Type 2 Diabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus73
4Not Yet RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
4Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
4Not Yet RecruitingTreatmentType2 Diabetes1
4Not Yet RecruitingTreatmentType2 Diabetes Mellitus1
4RecruitingHealth Services ResearchType 2 Diabetes Mellitus1
4RecruitingPreventionHyperglycemias1
4RecruitingTreatmentDiabetes, Diabetes Mellitus Type 13
4RecruitingTreatmentDiabetes, Diabetes Mellitus Type 1 / Ketoacidosis, Diabetic1
4RecruitingTreatmentHyperglycemia Steroid-induced / Insulin Resistance, Diabetes1
4RecruitingTreatmentNon-Alcoholic Fatty Liver Disease (NAFLD) / Type 2 Diabetes Mellitus1
4RecruitingTreatmentType 2 Diabetes Mellitus6
4RecruitingTreatmentType 2 Diabetes Patients1
4TerminatedTreatmentDiabetes Mellitus (DM)1
4TerminatedTreatmentPost-Transplant Glucocorticoid Induced Diabetes1
4TerminatedTreatmentType 2 Diabetes Mellitus7
4Unknown StatusPreventionType 2 Diabetes Mellitus1
4Unknown StatusTreatmentCoronary Artery Disease / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentDiabetes Mellitus (DM)1
4Unknown StatusTreatmentDiabetes, Diabetes Mellitus Type 12
4Unknown StatusTreatmentInsulin-requiring Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentLiver Cirrhosis / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentType 2 Diabetes Mellitus1
4WithdrawnTreatmentType 2 Diabetes Mellitus1
Not AvailableActive Not RecruitingNot AvailableDiabetes Mellitus (DM)1
Not AvailableCompletedNot AvailableBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableDiabetes Mellitus (DM)1
Not AvailableCompletedBasic ScienceDiabetes Mellitus (DM)1
Not AvailableCompletedOtherDiabetes Mellitus (DM)1
Not AvailableCompletedTreatmentBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentDiabetes Mellitus (DM)2
Not AvailableCompletedTreatmentDiabetes Mellitus (DM) / Hyperglycemias1
Not AvailableCompletedTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableCompletedTreatmentDiabetic Peripheral Neuropathy (DPN) / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentKetoacidosis, Diabetic1
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus6
Not AvailableRecruitingTreatmentDiabetes, Diabetes Mellitus Type 1 / Ketoacidosis, Diabetic1
Not AvailableRecruitingTreatmentType 2 Diabetes Mellitus2
Not AvailableTerminatedTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableUnknown StatusPreventionPre-Diabetic1
Not AvailableUnknown StatusTreatmentDiabetes Mellitus (DM)1
Not AvailableUnknown StatusTreatmentDiabetes, Diabetes Mellitus Type 1 / Hypoglycemia1
Not AvailableWithdrawnTreatmentType 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
  • Sanofi aventis us llc
Packagers
  • Gruppo Lepetit SPA
  • Physicians Total Care Inc.
  • Sanofi-Aventis Inc.
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous100 Units/ml
Injection, solutionSubcutaneous100 [iU]/1mL
SolutionSubcutaneous100 unit
Injection, solutionSubcutaneous
Injection, solutionSubcutaneous300 U/1mL
Injection, solutionSubcutaneous300 units/ml
SolutionSubcutaneous300 unit
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)
US6100376No1992-11-062009-11-06Us
CA1339044No1997-04-012014-04-01Canada
US9011391No2004-03-262024-03-26Us
US9233211No2004-03-022024-03-02Us
US8603044No2004-03-022024-03-02Us
US8512297No2004-09-152024-09-15Us
US8679069No2005-04-122025-04-12Us
US8992486No2004-06-052024-06-05Us
US8556864No2004-03-032024-03-03Us
US7918833Yes2008-03-232028-03-23Us
US7713930Yes2003-12-132023-12-13Us
US7476652Yes2004-01-232024-01-23Us
US9561331No2004-08-282024-08-28Us
US9623189No2004-08-192024-08-19Us
US9610409No2004-03-022024-03-02Us
US9526844No2004-03-022024-03-02Us
US9604008No2004-03-022024-03-02Us
US9533105No2004-08-172024-08-17Us
US9408979No2004-03-022024-03-02Us
US9604009No2004-08-162024-08-16Us
USRE45313No2000-07-122020-07-12Us
US9526764No2009-10-092029-10-09Us
US9345750No2011-05-182031-05-18Us
US9707176No2010-11-112030-11-11Us
US9775954No2004-03-022024-03-02Us
US9827379No2004-03-022024-03-02Us
US9821032No2012-05-092032-05-09Us
US9950039No2015-12-102035-12-10Us
US9717852No2013-04-082033-04-08Us
US10029011No2012-08-022032-08-02Us

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

Taxonomy

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

Targets

Kind
Protein
Organism
Human
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. [PubMed:11752352]
  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. [PubMed:17922476]
  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. [PubMed:20424816]
  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. [PubMed:18585815]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
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. Smith TJ: Insulin-like growth factor-I regulation of immune function: a potential therapeutic target in autoimmune diseases? Pharmacol Rev. 2010 Jun;62(2):199-236. doi: 10.1124/pr.109.002469. Epub 2010 Apr 14. [PubMed:20392809]

Enzymes

Kind
Protein
Organism
Human
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Drug created on June 13, 2005 07:24 / Updated on September 22, 2018 22:18