Identification

Name
Insulin lispro
Accession Number
DB00046
Description

Insulin lispro is a rapid-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Insulin is 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 among many other functions.

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 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 lispro, 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 cause 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, and when sufficient damage has been caused to pancreatic cells that the body is no longer able to produce insulin on its own.

Marketed as the brand name product Humalog, insulin lispro begins to exert its effects within 15 minutes of subcutaneous administration, while peak levels occur 30 to 90 minutes after administration. Due to its duration of action of around 5 hours, Humalog is considered "bolus insulin" as it provides high levels of insulin in a short period of time to mimic the release of endogenous insulin from the pancreas after meals. Bolus insulin is often combined with once daily, long-acting "basal insulin" such as Insulin detemir, Insulin degludec, or Insulin glargine to provide low concentrations of background insulin that can keep blood sugar stable between meals or overnight. 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 lispro is produced by recombinant DNA technology utilizing a non-pathogenic laboratory strain of Escherichia coli and was the first commercially available insulin analog. Formerly called LYSPRO from the chemical nomenclature [LYS(B28), PRO(B29)], insulin lispro differs from human insulin in that the amino acid proline at position B28 is replaced by lysine and the lysine in position B29 is replaced by proline. These biochemical changes result in a reduced tendency for self-association resulting in dissolution to a dimer and then to a monomer that is absorbed more rapidly after subcutaneous injection compared to endogenous human insulin.

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
Db00046
Protein Chemical Formula
C257H387N65O76S6
Protein Average Weight
5808.0 Da
Sequences
>A chain
GIVEQCCTSICSLYQLENYCN
>B chain
FVNQHLCGSHLVEALYLVCGERGFFYTKPT
Download FASTA Format
Synonyms
  • Insulin lispro (genetical recombination)
  • Insulin lispro (rDNA origin)
  • Insulin lispro protamine
  • Insulin lispro protamine recombinant
  • Insulin lispro recombinant
  • insulin lispro-aabc
  • Insulin,lispro,human/rDNA
  • Insulin,lispro,protamine/rDNA
  • Insulina lispro
External IDs
  • LY-275585
  • LY275585
  • SAR-342434
  • SAR342434

Pharmacology

Indication

Insulin lispro is indicated to improve glycemic control in adults and children with diabetes mellitus.

Associated Conditions
Contraindications & Blackbox Warnings
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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 lispro is a rapid-acting insulin analogue used to mimic postprandial insulin spikes in diabetic individuals. The onset of action of insulin lispro is 10-15 minutes. Its activity peaks 60 minutes following subcutaneous injection and its duration of action is 4-5 hours. Compared to regular human insulin, insulin lispro has a more rapid onset of action and a shorter duration of action. Insulin lispro is also shown to be equipotent to human insulin on a molar basis.

Mechanism of action

Insulin lispro 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 and catabolism. In humans, insulin is stored in the form of hexamers; however, only insulin monomers are able to interact with IR. Reversal of the proline and lysine residues at positions B28 and B29 of native insulin eliminates hydrophobic interactions and weakens some of the hydrogen bonds that contribute to the stability of the insulin dimers that comprise insulin hexamers. Hexamers of insulin lispro are produced in the presence of zinc and m-cresol. These weakly associated hexamers quickly dissociate upon subcutaneous injection and are absorbed as monomers through vascular endothelial cells. These properties give insulin lispro its fast-acting properties.

TargetActionsOrganism
AInsulin receptor
agonist
Humans
UInsulin-like growth factor 1 receptorNot AvailableHumans
Absorption

Insulin lispro is rapidly absorbed following subcutaneous administration. It is also absorbed more quickly than regular human insulin. Peak serum levels occur 30-90 minutes after injection in healthy subjects. Absorption also differs depending on the site of injection. After insulin lispro was administered in the abdomen, serum drug levels were higher and the duration of action was slightly shorter than after deltoid or thigh administration. The absolute bioavailability after subcutaneous injection ranges from 55% to 77% with doses between 0.1 to 0.2 unit/kg, inclusive. The mean observed area under the serum insulin concentration-time curve from time zero to infinity was 2360 pmol hr/L and 2390 pmol hr/L for HUMALOG U-200 and HUMALOG U-100, respectively. The corresponding mean peak serum insulin concentration was 795 pmol/L and 909 pmol/L for HUMALOG U-200 and HUMALOG U-100, respectively. The median time to maximum concentration was 1.0 hour for both formulations.

Volume of distribution

When administered intravenously as bolus injections of 0.1 and 0.2 U/kg dose in two separate groups of healthy subjects, the mean volume of distribution of insulin lispro appeared to decrease with increase in dose (1.55 and 0.72 L/kg, respectively).

Protein binding
Not Available
Metabolism

Insulin is predominantly cleared by metabolic degradation via a receptor-mediated process.

Route of elimination
Not Available
Half-life

After subcutaneous administration of insulin lispro, the t1/2 is shorter than that of regular human insulin (1 versus 1.5 hours, respectively).

Clearance

Clearance is dose dependent. When a dose of 0.1 unit/kg and 0.2 unit/kg were administered intravenously, the mean clearance was 21.0 mL/min/kg and 9.6 mL/min/kg respectively.

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. Rare cases of lipoatrophy or lipohypertrophy reactions have been observed.

Affected organisms
  • Humans and other mammals
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 Insulin lispro is combined with Acarbose.
AcebutololThe therapeutic efficacy of Insulin lispro can be increased when used in combination with Acebutolol.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Insulin lispro.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Insulin lispro.
AcetazolamideThe therapeutic efficacy of Insulin lispro can be increased when used in combination with Acetazolamide.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Insulin lispro is combined with Acetohexamide.
Acetyl sulfisoxazoleThe therapeutic efficacy of Insulin lispro can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidThe risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Insulin lispro.
AcyclovirThe metabolism of Acyclovir can be increased when combined with Insulin lispro.
AgomelatineThe metabolism of Agomelatine can be increased when combined with Insulin lispro.
Additional Data Available
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Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AdmelogInjection, solution100 U/1mLSubcutaneoussanofi-aventis U.S. LLC2017-12-11Not applicableUS flag
AdmelogSolution100 unitSubcutaneousSanofi Aventis2019-11-22Not applicableCanada flag
AdmelogInjection, solution100 U/1mLIntravenous; Subcutaneoussanofi-aventis U.S. LLC2017-12-11Not applicableUS flag
AdmelogInjection, solution100 U/1mLIntravenous; SubcutaneousREMEDYREPACK INC.2019-10-30Not applicableUS flag
AdmelogSolution100 unitSubcutaneousSanofi Aventis2019-11-22Not applicableCanada flag
AdmelogInjection, solution100 U/1mLIntravenous; Subcutaneoussanofi-aventis U.S. LLC2018-10-19Not applicableUS flag
Admelog SolostarSolutionSubcutaneousSanofi Aventis2019-11-22Not applicableCanada flag
HumalogInjection, solution100 [iU]/1mLIntravenous; SubcutaneousA-S Medication Solutions1996-06-14Not applicableUS flag
HumalogInjection, solution100 [iU]/1mLIntravenous; SubcutaneousEli Lilly and Company1996-06-14Not applicableUS flag
HumalogInjection, solution100 [iU]/1mLIntravenous; SubcutaneousREMEDYREPACK INC.2018-08-27Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Insulin lisproInjection, solution100 [iU]/1mLIntravenous; SubcutaneousREMEDYREPACK INC.2019-10-30Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Humalog Mix 25 (cartridge)Insulin lispro (25 unit) + Insulin lispro (75 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.1999-07-05Not applicableCanada flag
Humalog Mix 25 (cartridge)Insulin lispro (25 unit) + Insulin lispro (75 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.1999-07-05Not applicableCanada flag
Humalog Mix 25 (kwikpen)Insulin lispro (25 unit) + Insulin lispro (75 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.2013-09-30Not applicableCanada flag
Humalog Mix 25 (kwikpen)Insulin lispro (25 unit) + Insulin lispro (75 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.2013-09-30Not applicableCanada flag
Humalog Mix 25 (pen)Insulin lispro (25 unit) + Insulin lispro (75 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.2000-01-102011-04-29Canada flag
Humalog Mix 25 (pen)Insulin lispro (25 unit) + Insulin lispro (75 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.2000-01-102011-04-29Canada flag
Humalog Mix 50 (cartridge)Insulin lispro (50 unit) + Insulin lispro (50 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.2007-01-12Not applicableCanada flag
Humalog Mix 50 (cartridge)Insulin lispro (50 unit) + Insulin lispro (50 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.2007-01-12Not applicableCanada flag
Humalog Mix 50 (kwikpen)Insulin lispro (50 unit) + Insulin lispro (50 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.2014-01-23Not applicableCanada flag
Humalog Mix 50 (kwikpen)Insulin lispro (50 unit) + Insulin lispro (50 unit)SuspensionSubcutaneousEli Lilly & Co. Ltd.2014-01-23Not applicableCanada flag

Categories

ATC Codes
A10AC04 — Insulin lisproA10AB04 — Insulin lisproA10AD04 — Insulin lispro
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

Chemical Identifiers

UNII
GFX7QIS1II
CAS number
133107-64-9

References

General References
  1. Miles HL, Acerini CL: Insulin analog preparations and their use in children and adolescents with type 1 diabetes mellitus. Paediatr Drugs. 2008;10(3):163-76. [PubMed:18454569]
  2. Zib I, Raskin P: Novel insulin analogues and its mitogenic potential. Diabetes Obes Metab. 2006 Nov;8(6):611-20. [PubMed:17026485]
  3. Holleman F, Hoekstra JB: Insulin lispro. N Engl J Med. 1997 Jul 17;337(3):176-83. doi: 10.1056/NEJM199707173370307. [PubMed:9219705]
  4. Candido R, Wyne K, Romoli E: A Review of Basal-Bolus Therapy Using Insulin Glargine and Insulin Lispro in the Management of Diabetes Mellitus. Diabetes Ther. 2018 Jun;9(3):927-949. doi: 10.1007/s13300-018-0422-4. Epub 2018 Apr 13. [PubMed:29654514]
  5. Brems DN, Alter LA, Beckage MJ, Chance RE, DiMarchi RD, Green LK, Long HB, Pekar AH, Shields JE, Frank BH: Altering the association properties of insulin by amino acid replacement. Protein Eng. 1992 Sep;5(6):527-33. [PubMed:1438163]
  6. Howey DC, Bowsher RR, Brunelle RL, Woodworth JR: [Lys(B28), Pro(B29)]-human insulin. A rapidly absorbed analogue of human insulin. Diabetes. 1994 Mar;43(3):396-402. [PubMed:8314011]
  7. Torlone E, Fanelli C, Rambotti AM, Kassi G, Modarelli F, Di Vincenzo A, Epifano L, Ciofetta M, Pampanelli S, Brunetti P, et al.: Pharmacokinetics, pharmacodynamics and glucose counterregulation following subcutaneous injection of the monomeric insulin analogue [Lys(B28),Pro(B29)] in IDDM. Diabetologia. 1994 Jul;37(7):713-20. [PubMed:7958544]
  8. HUMALOG FDA Label [Link]
KEGG Drug
D04477
PubChem Substance
46507498
RxNav
314684
ChEMBL
CHEMBL1201538
Therapeutic Targets Database
DNC000800
PharmGKB
PA164747059
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Insulin_lispro
AHFS Codes
  • 68:20.08 — Insulins
FDA label
Download (1.13 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableType 2 Diabetes Mellitus1
4CompletedPreventionCoronary Artery Disease (CAD)1
4CompletedPreventionHyperglycemia2
4CompletedPreventionNephropathy, Diabetic1
4CompletedTreatmentAcute Myocardial Infarction (AMI) / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus / Ventricular Dysfunction1
4CompletedTreatmentGestational Diabetes Mellitus (GDM)2
4CompletedTreatmentHospitalizations / Hyperglycemia / Type 2 Diabetes Mellitus1
4CompletedTreatmentHyperglycemia2
4CompletedTreatmentType 1 Diabetes Mellitus9

Pharmacoeconomics

Manufacturers
  • Eli lilly and co
Packagers
  • Eli Lilly & Co.
  • Hospira Inc.
  • Lilly Del Caribe Inc.
  • Midwest IV and Home Care
  • Physicians Total Care Inc.
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous; Subcutaneous100 U/1mL
Injection, solutionSubcutaneous100 U/1mL
SolutionSubcutaneous100 unit
Injection, solution100 iu/1mL
Injection, solution40 U/ML
Injection, solutionCutaneous100 U/ML
Injection, solutionCutaneous200 U/ML
Injection, solutionIntravenous100 U/ML
Injection, solutionIntravenous; Subcutaneous100 [iU]/1mL
Injection, solutionIntravenous; Subcutaneous100 U/ml
Injection, solutionSubcutaneous100 [iU]/1mL
Injection, suspensionCutaneous; Parenteral100 U/ML
Injection, suspensionParenteral; Subcutaneous100 IU/ml
Injection, suspensionParenteral; Subcutaneous100 U/ML
Injection, suspensionSubcutaneous100
SolutionIntramuscular; Intravenous; Subcutaneous100 unit
SolutionSubcutaneous100 U/ml
SolutionIntramuscular; Intravenous; Subcutaneous
SolutionSubcutaneous100 iu/ml
SolutionIntravenous; Subcutaneous3.5 mg
SolutionSubcutaneous
InjectionIntravenous; Subcutaneous100 IU/ML
Injection, solutionIntravenous; Subcutaneous100 iu/1mL
Injection, solutionSubcutaneous200 U/ml
Injection, solutionSubcutaneous200 [iU]/1mL
Injection200 U/mL
Injection, suspension25 iu/1mL
SuspensionSubcutaneous
Injection, suspensionSubcutaneous100 IU/mL
Injection, suspension50 iu/1mL
Injection, suspensionSubcutaneous100 U/ml
Injection
Injection, suspensionSubcutaneous100 [iU]/1mL
LiquidIntramuscular; Intravenous; Subcutaneous100 unit
Injection, solutionCutaneous; Parenteral100 U/ML
Prices
Unit descriptionCostUnit
HumaLOG KwikPen 100 unit/ml Solution (1box = 5 Pens = 15ml)240.18USD box
HumaLOG Mix 50/50 KwikPen 50-50% Suspension Five 3ml Pens Per Box = 15ml240.18USD box
HumaLOG Mix 75/25 KwikPen 75-25% Suspension Five 3ml Pen Per Box = 15ml240.18USD box
HumaLOG Mix 75/25 Pen 75-25% Suspension 15ml Box240.18USD box
HumaLOG Pen (five 3ml Pens Per Box) 15ml Box240.18USD box
HumaLOG 100 unit/ml Solution 1 Box = Five 3ml Cartridges = 15ml231.0USD box
HumaLOG 100 unit/ml Solution 10ml Vial124.36USD vial
Humalog 100 unit/ml kwikpen15.4USD ml
Humalog 100 unit/ml pen15.4USD ml
Humalog mix 50-50 kwikpen15.4USD ml
Humalog mix 50-50 pen15.4USD ml
Humalog mix 50/50 kwikpen11.83USD ml
Humalog 100 unit/ml Cartridge9.37USD cartridge
Humalog 100 unit/ml2.95USD cartridge
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5474978No1995-12-122014-06-16US flag
US5514646No1996-05-072013-05-07US flag
CA2151564No2003-02-112015-06-12Canada flag
CA2151560No2000-05-092015-06-12Canada flag
US9011391No2015-04-212024-03-26US flag
US7291132No2007-11-062024-08-09US 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
US6551992No2003-04-222018-06-11US flag
US6034054No2000-03-072018-06-11US 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
US9775954No2017-10-032024-03-02US flag
US9827379No2017-11-282024-03-02US flag
US9717852No2017-08-012033-04-08US flag
Additional Data Available
  • Filed On
    Filed On
    Available for Purchase

    The date on which a patent was filed with the relevant government.

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Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)81 °CKhachidze, D.G. et al., J. Biol. Phys. Chem. 1:64-67 (2001)
hydrophobicity0.218Not Available
isoelectric point5.39Not 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
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Jehle PM, Fussgaenger RD, Kunze U, Dolderer M, Warchol W, Koop I: The human insulin analog insulin lispro improves insulin binding on circulating monocytes of intensively treated insulin-dependent diabetes mellitus patients. J Clin Endocrinol Metab. 1996 Jun;81(6):2319-27. [PubMed:8964871]
  3. Jehle PM, Fussganger RD, Seibold A, Luttke B, Bohm BO: Pharmacodynamics of insulin Lispro in 2 patients with type II diabetes mellitus. Int J Clin Pharmacol Ther. 1996 Nov;34(11):498-503. [PubMed:8937933]
  4. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. [PubMed:22420005]

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. [PubMed:1562279]
  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. [PubMed:12130701]

Drug created on June 13, 2005 07:24 / Updated on November 23, 2020 09:08

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