Identification

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Name
Insulin Human
Accession Number
DB00030  (BTD00105, BIOD00105, DB01383, DB05278, DB05215, DB05283, DB08914)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Hormones / Insulins
Description

Human Insulin, also known as Regular Insulin, is a short-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Human insulin is produced by recombinant DNA technology and is identical to endogenously produced insulin. Typically prescribed for the management of diabetes mellitus, insulin is 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 or synthesize the insulin needed to manage circulating blood sugar levels. As a result, people with T1D rely primarily on exogenous forms of insulin 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 trying 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.

Marketed as the brand name product Humulin R or Novolin R, human insulin begins to exert its effects within 30 minutes of subcutaneous administration, while peak levels occur 3-4 hours after administration. Due to its quick onset of action, human insulin 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, and 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.

Human insulin is also available in an inhalable form, intended to be used as a bolus meal-time insulin. Exubera was the first inhaled insulin available on the market and was developed by Inhale Therapeutics (later named Nektar Therapeutics). Unfortunately, limited uptake by physicians and patients, poor sales, bulky packaging, and concerns over the possible impact on lung cancer development resulted in Exubera products being withdrawn from the US markets 6. Exubera was followed by Afrezza, a monomeric inhaled insulin developed by Mannkind Corporation, which received FDA approval in 2016. While still available in the US, Afrezza has had similar concerns associated with its use, and had an FDA "black box" warning added to it to warn about use in patients with chronic lung disease. Afrezza does not currently have Health Canada or European Medicines Agency approval for marketing in Canada or the EU.

Human Insulin is a 51 residue peptide hormone produced by recombinant DNA technology by inserting the human insulin gene into Escherichia coli bacteria or Saccharomyces cerevisiae. The structure is identical to native human insulin, with two amino acid chains covalently linked by disulfide bonds.

Human insulin is also available in an intermediate-acting form as NPH (Neutral Protamine Hagedorn) as the marketed products Novolin N and Humulin N. NPH insulin is provided as a crystalline suspension of insulin with protamine and zinc, resulting in an onset of action in 1 to 3 hours, duration of action up to 24 hours, and peak action from 6 to 8 hours. Due to the added crystals, NPH insulin is typically cloudy when compared to other forms of insulin and has a neutral pH.

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.

Protein structure
Db00030
Protein chemical formula
C257H383N65O77S6
Protein average weight
5808.0 Da
Sequences
>A chain
GIVEQCCTSICSLYQLENYCN
>B chain
FVNQHLCGSHLVEALYLVCGERGFFYTPKT
Download FASTA Format
Synonyms
  • High molecular weight insulin human
  • Human insulin
  • human insulin (rDNA)
  • Insulin (human)
  • Insulin human [rDNA origin]
  • Insulin Human Regular
  • Insulin human regular (rDNA)
  • Insulin human, rDNA origin
  • Insulin recombinant human
  • Insulin recombinant purified human
  • Insulin regular
  • Insulin, human
  • Insulina regular
  • Regular Insulin, human
Product Ingredients
IngredientUNIICASInChI Key
Insulin human zinc suspensionNot AvailableNot AvailableNot applicable
NPH insulinNot Available53027-39-7Not applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Actraphane 30Injection, suspension100 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Actraphane 30Injection, suspension100 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Actraphane 30Injection, suspension40 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Actraphane 30Injection, suspension100 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Actraphane 30Injection, suspension40 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Actraphane 30Injection, suspension40 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Actraphane 30 FlexpenInjection, suspension100 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Actraphane 30 FlexpenInjection, suspension100 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Actraphane 30 FlexpenInjection, suspension100 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Actraphane 30 InnoletInjection, suspension100 iu/mlSubcutaneousNovo Nordisk2002-10-07Not applicableEu
Additional Data Available
  • Application Number
    Application Number

    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

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

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Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Humalog 70/30Injection, suspension100 [iU]/1mLSubcutaneousPhysicians Total Care, Inc.1994-12-28Not applicableUs
Humulin 50/50Injection, suspension100 [iU]/1mLSubcutaneousEli Lilly & Co. Ltd.1992-05-182010-05-31Us
Humulin 70/30Injection, suspension100 [iU]/1mLSubcutaneousA-S Medication Solutions1989-06-26Not applicableUs
Humulin 70/30Injection, suspension100 [iU]/1mLSubcutaneousEli Lilly and Company1989-06-26Not applicableUs
Humulin 70/30 70/30Injection, suspension100 [iU]/1mLSubcutaneousREMEDYREPACK INC.2015-04-272016-02-22Us
Humulin 70/30 KwikPenInjection, suspension100 [iU]/1mLSubcutaneousEli Lilly and Company2013-11-07Not applicableUs
Humulin LInjection, suspension100 [iU]/1mLSubcutaneousEli Lilly & Co. Ltd.1985-09-302007-02-01Us
Humulin NInjection, suspension100 [iU]/1mLSubcutaneousEli Lilly and Company1983-06-27Not applicableUs
Humulin NInjection, suspension100 [iU]/1mLSubcutaneousPhysicians Total Care, Inc.1994-10-24Not applicableUs
Humulin NInjection, suspension100 [iU]/1mLSubcutaneousA-S Medication Solutions1983-06-27Not applicableUs
Additional Data Available
  • Application Number
    Application Number

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

    Learn more
  • Product Code
    Product Code

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

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AfrezzaInsulin Human (4 1/1) + Insulin Human (8 1/1)KitMannkind Corporation2014-07-112014-10-22Us
AfrezzaInsulin Human (8 1/1) + Insulin Human (4 1/1) + Insulin Human (12 1/1)KitMannkind Corporation2014-07-11Not applicableUs
AfrezzaInsulin Human (8 1/1) + Insulin Human (12 1/1)KitMannkind Corporation2014-07-11Not applicableUs
AfrezzaInsulin Human (4 1/1) + Insulin Human (8 1/1)KitSanofi Aventis2014-07-112017-11-07Us
AfrezzaInsulin Human (4 1/1) + Insulin Human (8 1/1)KitMannkind Corporation2014-07-112016-08-03Us
AfrezzaInsulin Human (4 1/1) + Insulin Human (8 1/1)KitMannkind Corporation2014-07-112014-10-22Us
AfrezzaInsulin Human (8 1/1) + Insulin Human (12 1/1)KitMannkind Corporation2014-07-11Not applicableUs
AfrezzaInsulin Human (8 1/1) + Insulin Human (12 1/1)KitMannkind Corporation2014-07-11Not applicableUs
AfrezzaInsulin Human (4 1/1) + Insulin Human (8 1/1)KitMannkind Corporation2014-07-112016-08-03Us
AfrezzaInsulin Human (4 1/1) + Insulin Human (8 1/1)KitSanofi Aventis2014-07-112017-11-07Us
Categories
UNII
1Y17CTI5SR
CAS number
11061-68-0

Pharmacology

Indication

Human insulin is indicated to improve glycemic control in adults and pediatric patients with diabetes mellitus.

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. Postprandial insulin spikes are 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).

Mechanism of action

The primary activity of insulin is the regulation of glucose metabolism. Insulin promotes glucose and amino acid uptake into muscle and adipose tissues, and other tissues except brain and liver. It also has an anabolic role in stimulating glycogen, fatty acid, and protein synthesis. Insulin inhibits gluconeogenesis in the liver. Insulin 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 is able to autophosphorylate and phosphorylate numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. These activated proteins, in turn, lead 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) which play a critical role in metabolism and catabolism.

TargetActionsOrganism
AInsulin receptor
agonist
Humans
UInsulin-like growth factor 1 receptorNot AvailableHumans
URetinoblastoma-associated proteinNot AvailableHumans
Additional Data Available
Adverse Effects

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

When injected subcutaneously, the glucose-lowering effect of human insulin begins approximately 30 minutes post-dose. After a single subcutaneous administration of 0.1 unit/kg of human insulin to healthy subjects, peak insulin concentrations occurred between 1.5 to 2.5 hours post-dose.

When administered in an inhaled form (as the product Afrezza), the time to maximum serum insulin concentration ranges from 10-20 minutes after oral inhalation of 4 to 48 units of human insulin. Serum insulin concentrations declined to baseline by approximately 60-240 minutes for these dose levels. Intrapatient variability in insulin exposure measured by AUC and Cmax is approximately 16% (95% CI 12-23%) and 21% (95% CI 16-30%), respectively.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

The metabolism and elimination of orally inhaled human insulin are comparable to regular human insulin.

Route of elimination

Following oral inhalation of human insulin, a mean of 39% of the inhaled dose of carrier particles was distributed to the lungs and a mean of 7% of the dose was swallowed. The swallowed fraction was not absorbed from the GI tract and was eliminated unchanged in the feces.

Half life

Systemic insulin disposition (apparent terminal half-life) following oral inhalation of 4 to 48 units of human insulin was 120-206 minutes.

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

Interactions

Drug Interactions
DrugInteraction
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Insulin Human is combined with 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Insulin Human can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Insulin Human.
AcarboseThe risk or severity of hypoglycemia can be increased when Insulin Human is combined with Acarbose.
AcebutololAcebutolol may increase the hypoglycemic activities of Insulin Human.
AcetazolamideThe therapeutic efficacy of Insulin Human can be increased when used in combination with Acetazolamide.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Insulin Human is combined with Acetohexamide.
Acetyl sulfisoxazoleThe therapeutic efficacy of Insulin Human 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 Human.
AgmatineThe risk or severity of hypoglycemia can be increased when Agmatine is combined with Insulin Human.
Additional Data Available
  • Extended Description
    Extended Description

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  • Severity
    Severity

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  • Evidence Level
    Evidence Level

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  • Action
    Action

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Food Interactions
Not Available

References

Synthesis Reference

Humulin is synthesized in a special non-disease-producing laboratory strain of Escherichia coli bacteria that has been genetically altered to produce human insulin.

General References
  1. Herrmann BL, Kasser C, Keuthage W, Huptas M, Dette H, Klute A: Comparison of insulin aspart vs. regular human insulin with or without insulin detemir concerning adipozytokines and metabolic effects in patients with type 2 diabetes mellitus. Exp Clin Endocrinol Diabetes. 2013 Apr;121(4):210-3. doi: 10.1055/s-0033-1334905. Epub 2013 Mar 19. [PubMed:23512415]
  2. Lepore M, Pampanelli S, Fanelli C, Porcellati F, Bartocci L, Di Vincenzo A, Cordoni C, Costa E, Brunetti P, Bolli GB: Pharmacokinetics and pharmacodynamics of subcutaneous injection of long-acting human insulin analog glargine, NPH insulin, and ultralente human insulin and continuous subcutaneous infusion of insulin lispro. Diabetes. 2000 Dec;49(12):2142-8. [PubMed:11118018]
  3. Owens DR, Coates PA, Luzio SD, Tinbergen JP, Kurzhals R: Pharmacokinetics of 125I-labeled insulin glargine (HOE 901) in healthy men: comparison with NPH insulin and the influence of different subcutaneous injection sites. Diabetes Care. 2000 Jun;23(6):813-9. [PubMed:10841002]
  4. Danne T, Lupke K, Walte K, Von Schuetz W, Gall MA: Insulin detemir is characterized by a consistent pharmacokinetic profile across age-groups in children, adolescents, and adults with type 1 diabetes. Diabetes Care. 2003 Nov;26(11):3087-92. [PubMed:14578244]
  5. 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]
  6. Oleck J, Kassam S, Goldman JD: Commentary: Why Was Inhaled Insulin a Failure in the Market? Diabetes Spectr. 2016 Aug;29(3):180-4. doi: 10.2337/diaspect.29.3.180. [PubMed:27574374]
External Links
UniProt
Q8HXV2
Genbank
AY137503
KEGG Drug
D03230
KEGG Compound
C00723
PubChem Substance
46506231
ChEBI
5931
Therapeutic Targets Database
DAP000802
PharmGKB
PA164744571
Wikipedia
Insulin
ATC Codes
A10AC01 — Insulin (human)A10AE01 — Insulin (human)A10AB01 — Insulin (human)A10AD01 — Insulin (human)A10AF01 — Insulin (human)
AHFS Codes
  • 68:20.08 — Insulins
FDA label
Download (828 KB)
MSDS
Download (47 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentAnhedonia / Bipolar Disorder (BD) / Intranasal Insulin / Major Depressive Disorder (MDD)1
0WithdrawnOtherBMI >30 kg/m2 / Hyperinsulinemia1
1CompletedNot AvailableDiabetes Mellitus (DM)1
1CompletedBasic ScienceSarcopenia1
1CompletedBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus1
1CompletedBasic ScienceType 2 Diabetes Mellitus1
1CompletedHealth Services ResearchDiabetes Mellitus (DM)4
1CompletedOtherHealthy Volunteers1
1CompletedTreatmentDiabetes Mellitus (DM)2
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers2
1CompletedTreatmentDiabetes Mellitus (DM) / Type 1 Insulin-Dependent Diabetes Mellitus1
1CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
1CompletedTreatmentType 2 Diabetes Mellitus1
1RecruitingBasic ScienceAortic Aneurysms / Ischaemic Heart Diseases1
1RecruitingTreatmentPost-Prandial Hyperglycemia / Post-Prandial Hypoglycemia1
1RecruitingTreatmentType1 Diabetes Mellitus1
1TerminatedBasic ScienceBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
1WithdrawnBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus1
1, 2CompletedPreventionType 1 Insulin-Dependent Diabetes Mellitus1
1, 2CompletedTreatmentDiabetes Mellitus (DM)1
1, 2CompletedTreatmentType 2 Diabetes Mellitus1
1, 2RecruitingTreatmentHIV Dementia / HIV-Associated Cognitive Motor Complex1
2CompletedNot AvailableType 1 Insulin-Dependent Diabetes Mellitus1
2CompletedBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus1
2CompletedOtherType 2 Diabetes Mellitus1
2CompletedTreatmentAlzheimer's Disease (AD) / Mild Cognitive Impairment (MCI)1
2CompletedTreatmentDiabetes Mellitus (DM) / Type 1 Insulin-Dependent Diabetes Mellitus1
2CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
2CompletedTreatmentHyperglycemias1
2CompletedTreatmentImpaired Glucose Tolerance (IGT) / Type 2 Diabetes Mellitus1
2CompletedTreatmentMultiple System Atrophy (MSA) / Parkinson's Disease (PD)1
2CompletedTreatmentNon Insulin Dependent Diabetes / Pregnancy1
2CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
2CompletedTreatmentType 2 Diabetes Mellitus3
2Not Yet RecruitingBasic ScienceBipolar I Disorder / Psychosis / Schizo Affective Disorder / Schizophrenic Disorders1
2RecruitingDiagnosticCessation, Smoking1
2RecruitingTreatmentHIV Associated Neurocognitive Disorder (HAND)1
2RecruitingTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
2TerminatedTreatmentDiabetes Mellitus (DM)1
2WithdrawnBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus1
2, 3CompletedTreatmentType 2 Diabetes Mellitus1
3CompletedNot AvailableType 1 Insulin-Dependent Diabetes Mellitus1
3CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Blood Pressure (Hypertension) / High Cholesterol / Type 2 Diabetes Mellitus1
3CompletedTreatmentAsthma Bronchial / Diabetes Mellitus (DM)1
3CompletedTreatmentCystic Fibrosis (CF) / Diabetes Mellitus (DM)1
3CompletedTreatmentDiabetes Mellitus (DM)4
3CompletedTreatmentDiabetes Mellitus (DM) / Gestational Diabetes Mellitus (GDM)1
3CompletedTreatmentDiabetes Mellitus (DM) / Type 1 Insulin-Dependent Diabetes Mellitus3
3CompletedTreatmentDiabetes Mellitus, Insulin-Dependent1
3CompletedTreatmentGestational Diabetes Mellitus as Antepartum Condition1
3CompletedTreatmentSevere Sepsis / Shock, Septic1
3CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus4
3CompletedTreatmentType 2 Diabetes Mellitus5
3TerminatedTreatmentAsthma Bronchial / Moderate Chronic Obstructive Pulmonary Disease / Type 1 Insulin-Dependent Diabetes Mellitus / Type 2 Diabetes Mellitus1
3TerminatedTreatmentChronic Obstructive Pulmonary Disease (COPD) / Diabetes Mellitus (DM)1
3TerminatedTreatmentDiabetes Mellitus (DM)1
3TerminatedTreatmentHyperglycemias1
3TerminatedTreatmentType 1 Insulin-Dependent Diabetes Mellitus2
3TerminatedTreatmentType 1 Insulin-Dependent Diabetes Mellitus / Type 2 Diabetes Mellitus1
3TerminatedTreatmentType 2 Diabetes Mellitus1
3TerminatedTreatmentType I Diabetes1
4CompletedNot AvailableDiabetes Mellitus (DM) / Type 1 Insulin-Dependent Diabetes Mellitus / Type 2 Diabetes Mellitus1
4CompletedDiagnosticDiabetes Mellitus (DM)1
4CompletedHealth Services ResearchHypoglycemia1
4CompletedScreeningDiabetes Mellitus (DM)1
4CompletedTreatmentCancer Cachexia1
4CompletedTreatmentChronic Kidney Disease (CKD) / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus (DM)3
4CompletedTreatmentDiabetes Mellitus (DM) / Hyperglycemias3
4CompletedTreatmentDiabetes Mellitus (DM) / Type 1 Insulin-Dependent Diabetes Mellitus2
4CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
4CompletedTreatmentHyperglycemias / Type 2 Diabetes Mellitus1
4CompletedTreatmentInpatient Hyperglycemia / Type 2 Diabetes Mellitus1
4CompletedTreatmentInsufficient Metabolic Control / OAD Treatment / Type 2 Diabetic Patients1
4CompletedTreatmentKetoacidosis, Diabetic1
4CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus15
4Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
4RecruitingDiagnosticHigh Blood Pressure (Hypertension)1
4RecruitingTreatmentHyperglycemia Steroid-induced / Insulin Resistance, Diabetes1
4SuspendedTreatmentAcute Coronary Syndromes (ACS)1
4TerminatedTreatmentDiabetes Mellitus (DM)1
4TerminatedTreatmentPost-Transplant Glucocorticoid Induced Diabetes1
4TerminatedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
4TerminatedTreatmentType 2 Diabetes Mellitus1
4Unknown StatusPreventionType 2 Diabetes Mellitus1
4Unknown StatusTreatmentBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentDiabetes Mellitus (DM)1
4Unknown StatusTreatmentInsulin-requiring Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentIntracranial Hemorrhages / Subarachnoid Hemorrhage / Traumatic Brain Injury (TBI)1
4Unknown StatusTreatmentLiver Cirrhosis / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
4Unknown StatusTreatmentType 2 Diabetes Mellitus2
Not AvailableCompletedNot AvailableDiabetes Mellitus (DM)2
Not AvailableCompletedNot AvailableDiabetes Mellitus (DM) / Type 1 Insulin-Dependent Diabetes Mellitus / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus3
Not AvailableCompletedBasic ScienceBMI >30 kg/m22
Not AvailableCompletedBasic ScienceBMI >30 kg/m2 / Diabetes Mellitus (DM)1
Not AvailableCompletedBasic ScienceBMI >30 kg/m2 / Sarcopenia1
Not AvailableCompletedBasic ScienceHypoglycemia / Type 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableCompletedBasic ScienceInsulin Resistance2
Not AvailableCompletedBasic ScienceKetoacidosis / Type 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableCompletedBasic ScienceSarcopenia1
Not AvailableCompletedBasic ScienceType 2 Diabetes Mellitus2
Not AvailableCompletedOtherCognitive Impairments / Hypoglycemia1
Not AvailableCompletedTreatmentDiabetes Mellitus (DM)1
Not AvailableCompletedTreatmentHeart Defects,Congenital / Hyperglycemias1
Not AvailableCompletedTreatmentImpaired Glucose Tolerance (IGT) / Macrosomia, Fetal1
Not AvailableCompletedTreatmentRenal Failure / Respiratory Failure / Sepsis / Surgical Site Infections1
Not AvailableCompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus2
Not AvailableNot Yet RecruitingPreventionCognitive Decline / Delirium / Heart Diseases1
Not AvailableRecruitingOtherType 2 Diabetes Mellitus1
Not AvailableRecruitingPreventionDelirium / Heart Diseases1
Not AvailableRecruitingPreventionGestational Diabetes Mellitus (GDM)1
Not AvailableRecruitingTreatmentMinor burns1
Not AvailableTerminatedNot AvailableDiabetes Mellitus (DM) / Type 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableUnknown StatusNot AvailableArterial Hypertension / Diabetes Mellitus (DM)1
Not AvailableUnknown StatusBasic ScienceHuman Physiology of Energy Homeostasis1
Not AvailableUnknown StatusPreventionSurgery, Cardiac1
Not AvailableWithdrawnTreatmentIntracranial Aneurysms1
Not AvailableWithdrawnTreatmentType 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
  • Novo nordisk inc
Packagers
  • A-S Medication Solutions LLC
  • DispenseXpress Inc.
  • Eli Lilly & Co.
  • Hospira Inc.
  • Intervet International
  • Novo Nordisk Inc.
  • Pfizer Inc.
  • Physicians Total Care Inc.
Dosage forms
FormRouteStrength
Kit
Powder, meteredRespiratory (inhalation)12 1/1
Powder, meteredRespiratory (inhalation)4 1/1
Powder, meteredRespiratory (inhalation)8 1/1
SolutionSubcutaneous500 unit
Aerosol, powderRespiratory (inhalation)1 mg/1
Aerosol, powderRespiratory (inhalation)3 mg/1
SuspensionSubcutaneous
Injection, suspensionSubcutaneous100 [iU]/1mL
Injection, suspensionSubcutaneous100
SuspensionSubcutaneous100 unit
Injection, solutionParenteral100 [iU]/1mL
Injection, solutionSubcutaneous100 [iU]/1mL
SolutionIntramuscular; Subcutaneous100 unit
Injection, solutionSubcutaneous500 [iU]/1mL
Injection, suspensionSubcutaneous100 IU/ml
Injection, suspensionSubcutaneous40 IU/ml
Injection, solutionSubcutaneous100 IU/ml
Injection, solutionIntravenous; Subcutaneous100 IU/ml
Injection, solutionIntravenous; Subcutaneous40 IU/ml
Injection, solutionIntraperitoneal400 IU/ml
Injection, suspensionSubcutaneous100 [USP'U]/1mL
SolutionIntramuscular; Intravenous; Subcutaneous100 unit
LiquidIntramuscular; Intravenous; Subcutaneous100 unit
Prices
Unit descriptionCostUnit
NovoLIN R PenFill 100 unit/ml Solution Five 3ml Cartridges Per Box = 15ml162.26USD cartridge
NovoLIN R 100 unit/ml Solution 10ml Vial73.19USD vial
Novolin r 100 unit/ml cartridg33.33USD ml
NovoLIN R InnoLet 100 unit/ml Solution 3ml Cartridge24.17USD cartridge
Humulin N Cartridge 100 unit/ml Cartridge2.99USD cartridge
Humulin R Cartridge 100 unit/ml Cartridge2.99USD cartridge
Novolin Ge Toronto Penfill 100 unit/ml Cartridge2.8USD cartridge
Novolin Ge Nph Penfill 100 unit/ml Cartridge2.78USD cartridge
Humulin N 100 unit/ml2.29USD cartridge
Humulin R 100 unit/ml2.29USD cartridge
Novolin Ge Nph 100 unit/ml2.14USD cartridge
Novolin Ge Toronto 100 unit/ml2.14USD cartridge
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
USRE37872No2002-10-082010-02-12Us
CA2183577No2007-10-302015-02-07Canada
CA2253393No2007-10-092017-05-07Canada
US7291132No2007-11-062024-08-09Us
US6257233No2001-07-102019-05-14Us
US6546929No2003-04-152019-05-14Us
US6685967No2004-02-032018-09-11Us
US6582728No2003-06-242020-06-24Us
US8912193No2014-12-162029-06-12Us
US7648960No2010-01-192020-06-29Us
US6652885No2003-11-252020-06-29Us
US8258095No2012-09-042029-08-11Us
US8778403No2014-07-152030-06-11Us
US6444226No2002-09-032020-06-29Us
US7943572No2011-05-172026-08-10Us
US8119593No2012-02-212029-08-11Us
US7943178No2011-05-172020-06-29Us
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US8215300No2012-07-102022-11-24Us
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Additional Data Available
  • Filed On
    Filed On

    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)

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
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. Desbuquois B, Chauvet G, Kouach M, Authier F: Cell itinerary and metabolic fate of proinsulin in rat liver: in vivo and in vitro studies. Endocrinology. 2003 Dec;144(12):5308-21. Epub 2003 Sep 11. [PubMed:12970169]
  2. Chen LM, Yang XW, Tang JG: Acidic residues on the N-terminus of proinsulin C-Peptide are important for the folding of insulin precursor. J Biochem. 2002 Jun;131(6):855-9. [PubMed:12038982]
  3. Bell DS: Insulin therapy in diabetes mellitus: how can the currently available injectable insulins be most prudently and efficaciously utilised? Drugs. 2007;67(13):1813-27. [PubMed:17722952]
  4. Tanti JF, Jager J: Cellular mechanisms of insulin resistance: role of stress-regulated serine kinases and insulin receptor substrates (IRS) serine phosphorylation. Curr Opin Pharmacol. 2009 Dec;9(6):753-62. doi: 10.1016/j.coph.2009.07.004. Epub 2009 Aug 13. [PubMed:19683471]
  5. Chiu SL, Cline HT: Insulin receptor signaling in the development of neuronal structure and function. Neural Dev. 2010 Mar 15;5:7. doi: 10.1186/1749-8104-5-7. [PubMed:20230616]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Weinstein D, Simon M, Yehezkel E, Laron Z, Werner H: Insulin analogues display IGF-I-like mitogenic and anti-apoptotic activities in cultured cancer cells. Diabetes Metab Res Rev. 2009 Jan;25(1):41-9. doi: 10.1002/dmrr.912. [PubMed:19145584]
  4. Werner H, Weinstein D, Yehezkel E, Laron Z: Controversies in the use of insulin analogues. Expert Opin Biol Ther. 2011 Feb;11(2):199-209. doi: 10.1517/14712598.2011.540233. [PubMed:21219237]
  5. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Key regulator of entry into cell division that acts as a tumor suppressor. Promotes G0-G1 transition when phosphorylated by CDK3/cyclin-C. Acts as a transcription repressor of E2F1 target genes. Th...
Gene Name
RB1
Uniprot ID
P06400
Uniprot Name
Retinoblastoma-associated protein
Molecular Weight
106158.335 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Radulescu RT, Bellitti MR, Ruvo M, Cassani G, Fassina G: Binding of the LXCXE insulin motif to a hexapeptide derived from retinoblastoma protein. Biochem Biophys Res Commun. 1995 Jan 5;206(1):97-102. doi: 10.1006/bbrc.1995.1014. [PubMed:7818556]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Plays a role in the cellular breakdown of insulin, IAPP, glucagon, bradykinin, kallidin and other peptides, and thereby plays a role in intercellular peptide signaling. Degrades amyloid formed by A...
Gene Name
IDE
Uniprot ID
P14735
Uniprot Name
Insulin-degrading enzyme
Molecular Weight
117967.49 Da
References
  1. Amata O, Marino T, Russo N, Toscano M: Human insulin-degrading enzyme working mechanism. J Am Chem Soc. 2009 Oct 21;131(41):14804-11. doi: 10.1021/ja9037142. [PubMed:19785409]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Serine-type endopeptidase activity
Specific Function
Involved in the processing of hormone and other protein precursors at sites comprised of pairs of basic amino acid residues. Responsible for the release of glucagon from proglucagon in pancreatic A...
Gene Name
PCSK2
Uniprot ID
P16519
Uniprot Name
Neuroendocrine convertase 2
Molecular Weight
70564.735 Da
References
  1. Uniprot P16519 [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Removes residual C-terminal Arg or Lys remaining after initial endoprotease cleavage during prohormone processing. Processes proinsulin.
Gene Name
CPE
Uniprot ID
P16870
Uniprot Name
Carboxypeptidase E
Molecular Weight
53150.185 Da
References
  1. Naggert JK, Fricker LD, Varlamov O, Nishina PM, Rouille Y, Steiner DF, Carroll RJ, Paigen BJ, Leiter EH: Hyperproinsulinaemia in obese fat/fat mice associated with a carboxypeptidase E mutation which reduces enzyme activity. Nat Genet. 1995 Jun;10(2):135-42. doi: 10.1038/ng0695-135. [PubMed:7663508]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Serine-type endopeptidase activity
Specific Function
Involved in the processing of hormone and other protein precursors at sites comprised of pairs of basic amino acid residues. Substrates include POMC, renin, enkephalin, dynorphin, somatostatin, ins...
Gene Name
PCSK1
Uniprot ID
P29120
Uniprot Name
Neuroendocrine convertase 1
Molecular Weight
84150.92 Da
References
  1. Uniprot P29120 [Link]

Drug created on June 13, 2005 07:24 / Updated on July 18, 2019 18:45