Insulin human

Identification

Name

Insulin human

Accession Number

DB00030

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.

Type

Biotech

Groups

Approved, Investigational

Biologic Classification

Protein Based Therapies
Hormones / Insulins

Protein Structure

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
• 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
• Neutral insulin
• Regular Insulin, human
• Soluble insulin

Pharmacology

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Indication

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

Associated Conditions

• Diabetes Mellitus
• Type 1 Diabetes Mellitus

Contraindications & Blackbox Warnings

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. 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.

Target	Actions	Organism
AInsulin receptor	agonist	Humans
UInsulin-like growth factor 1 receptor	Not Available	Humans
URetinoblastoma-associated protein	Not Available	Humans
UCarboxypeptidase E	modulator	Humans

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

Adverse Effects

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Toxicity

Not Available

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Acarbose	The risk or severity of hypoglycemia can be increased when Insulin human is combined with Acarbose.
Acebutolol	The therapeutic efficacy of Insulin human can be increased when used in combination with Acebutolol.
Acetazolamide	The therapeutic efficacy of Insulin human can be increased when used in combination with Acetazolamide.
Acetohexamide	The risk or severity of hypoglycemia can be increased when Insulin human is combined with Acetohexamide.
Acetyl sulfisoxazole	The therapeutic efficacy of Insulin human can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acid	The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Insulin human.
Albiglutide	Albiglutide may increase the hypoglycemic activities of Insulin human.
Alclometasone	The risk or severity of hyperglycemia can be increased when Alclometasone is combined with Insulin human.
Alogliptin	Alogliptin may increase the hypoglycemic activities of Insulin human.
Amcinonide	The risk or severity of hyperglycemia can be increased when Amcinonide is combined with Insulin human.

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Food Interactions

• Avoid alcohol. Alcohol may impair blood glucose control.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Insulin human zinc suspension	Not Available	Not Available	Not applicable
NPH insulin	Not Available	53027-39-7	Not applicable

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Actraphane 30	Injection, suspension	40 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable
Actraphane 30	Injection, suspension	100 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable
Actraphane 30	Injection, suspension	40 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable
Actraphane 30	Injection, suspension	100 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable
Actraphane 30	Injection, suspension	100 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable
Actraphane 30	Injection, suspension	40 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable
Actraphane 30 Flexpen	Injection, suspension	100 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable
Actraphane 30 Flexpen	Injection, suspension	100 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable
Actraphane 30 Flexpen	Injection, suspension	100 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable
Actraphane 30 Innolet	Injection, suspension	100 iu/ml	Subcutaneous	Novo Nordisk	2016-09-07	Not applicable

Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Humalog 70/30	Injection, suspension	100 [iU]/1mL	Subcutaneous	Physicians Total Care, Inc.	1994-12-28	Not applicable
Humulin 50/50	Injection, suspension	100 [iU]/1mL	Subcutaneous	Eli Lilly & Co. Ltd.	1992-05-18	2010-05-31
Humulin 70/30	Injection, suspension	100 [iU]/1mL	Subcutaneous	A-S Medication Solutions	1989-06-26	Not applicable
Humulin 70/30	Injection, suspension	100 [iU]/1mL	Subcutaneous	Eli Lilly and Company	1989-06-26	Not applicable
Humulin 70/30 70/30	Injection, suspension	100 [iU]/1mL	Subcutaneous	REMEDYREPACK INC.	2015-04-27	2016-02-22
Humulin 70/30 KwikPen	Injection, suspension	100 [iU]/1mL	Subcutaneous	Eli Lilly and Company	2013-11-07	Not applicable
Humulin L	Injection, suspension	100 [iU]/1mL	Subcutaneous	Eli Lilly & Co. Ltd.	1985-09-30	2007-02-01
Humulin N	Injection, suspension	100 [iU]/1mL	Subcutaneous	Eli Lilly and Company	1983-06-27	Not applicable
Humulin N	Injection, suspension	100 [iU]/1mL	Subcutaneous	Physicians Total Care, Inc.	1994-10-24	Not applicable
Humulin N	Injection, suspension	100 [iU]/1mL	Subcutaneous	A-S Medication Solutions	1983-06-27	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Afrezza	Insulin human (8 1/1) + Insulin human (4 1/1) + Insulin human (12 1/1)		Respiratory (inhalation)	Mannkind Corporation	2014-07-11	Not applicable
Afrezza	Insulin human (8 1/1) + Insulin human (12 1/1)	Kit	Respiratory (inhalation)	Sanofi Aventis	2014-07-11	2017-11-07
Afrezza	Insulin human (4 1/1) + Insulin human (8 1/1)	Kit	Respiratory (inhalation)	Mannkind Corporation	2014-07-11	2014-10-22
Afrezza	Insulin human (8 1/1) + Insulin human (12 1/1)	Kit	Respiratory (inhalation)	Mannkind Corporation	2014-07-11	Not applicable
Afrezza	Insulin human (4 1/1) + Insulin human (8 1/1)	Kit	Respiratory (inhalation)	Mannkind Corporation	2014-07-11	2016-08-03
Afrezza	Insulin human (4 1/1) + Insulin human (8 1/1)	Kit	Respiratory (inhalation)	Sanofi Aventis	2014-07-11	2017-11-07
Afrezza	Insulin human (4 1/1) + Insulin human (8 1/1)	Kit	Respiratory (inhalation)	Mannkind Corporation	2014-07-11	Not applicable
Afrezza	Insulin human (8 1/1) + Insulin human (4 1/1)	Kit	Respiratory (inhalation)	Mannkind Corporation	2014-07-11	Not applicable
Afrezza	Insulin human (4 1/1) + Insulin human (8 1/1)	Kit	Respiratory (inhalation)	Mannkind Corporation	2014-07-11	2014-10-22
Afrezza	Insulin human (4 1/1) + Insulin human (8 1/1)	Kit	Respiratory (inhalation)	Mannkind Corporation	2014-07-11	2014-10-22

Categories

ATC Codes

A10AC01 — Insulin (human)

• A10AC — Insulins and analogues for injection, intermediate-acting
• A10A — INSULINS AND ANALOGUES
• A10 — DRUGS USED IN DIABETES
• A — ALIMENTARY TRACT AND METABOLISM

A10AE01 — Insulin (human)

• A10AE — Insulins and analogues for injection, long-acting
• A10A — INSULINS AND ANALOGUES
• A10 — DRUGS USED IN DIABETES
• A — ALIMENTARY TRACT AND METABOLISM

A10AB01 — Insulin (human)

• A10AB — Insulins and analogues for injection, fast-acting
• A10A — INSULINS AND ANALOGUES
• A10 — DRUGS USED IN DIABETES
• A — ALIMENTARY TRACT AND METABOLISM

A10AD01 — Insulin (human)

• A10AD — Insulins and analogues for injection, intermediate- or long-acting combined with fast-acting
• A10A — INSULINS AND ANALOGUES
• A10 — DRUGS USED IN DIABETES
• A — ALIMENTARY TRACT AND METABOLISM

A10AF01 — Insulin (human)

• A10AF — Insulins and analogues for inhalation
• A10A — INSULINS AND ANALOGUES
• A10 — DRUGS USED IN DIABETES
• A — ALIMENTARY TRACT AND METABOLISM

Drug Categories

• Alimentary Tract and Metabolism
• Amino Acids, Peptides, and Proteins
• Blood Glucose Lowering Agents
• Cytochrome P-450 CYP1A2 Inducers
• Cytochrome P-450 CYP1A2 Inducers (strength unknown)
• Cytochrome P-450 Enzyme Inducers
• Drugs Used in Diabetes
• Hormones
• Hormones, Hormone Substitutes, and Hormone Antagonists
• Hypoglycemia-Associated Agents
• Insulin
• Insulin, metabolism
• Insulin, Short-Acting
• Insulins and Analogues for Injection, Fast-Acting
• Pancreatic Hormones
• Peptide Hormones
• Peptides
• Protein Precursors
• Proteins

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

1Y17CTI5SR

CAS number

11061-68-0

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]
7. FDA Approved Drug Products: Humulin R (insulin human) [Link]

External Links

UniProt

Q8HXV2

Genbank

AY137503

KEGG Drug

D03230

KEGG Compound

C00723

PubChem Substance

46506231

RxNav

253182

ChEBI

5931

Therapeutic Targets Database

DAP000802

PharmGKB

PA164744571

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

Wikipedia

Insulin

AHFS Codes

• 68:20.08 — Insulins

FDA label

Download (828 KB)

MSDS

Download (47 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Type 1 Diabetes Mellitus	1
4	Active Not Recruiting	Treatment	Type 2 Diabetes Mellitus	1
4	Active Not Recruiting	Treatment	Type 2 Diabetes Treated With Insulin	1
4	Completed	Basic Science	Type 2 Diabetes Mellitus / Weight Gain	1
4	Completed	Diagnostic	Diabetes Mellitus	1
4	Completed	Health Services Research	Hypoglycemia	1
4	Completed	Prevention	Coronary Artery Disease (CAD)	1
4	Completed	Prevention	Hyperglycemia	1
4	Completed	Screening	Diabetes Mellitus	1
4	Completed	Supportive Care	Hyperglycemia Steroid-induced	1

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

Form	Route	Strength
Injection, suspension	Cutaneous; Parenteral	100 IU/ml
Injection, suspension	Cutaneous; Parenteral	40 IU/ml
Injection, suspension	Parenteral; Subcutaneous	100 IU/ml
Injection, suspension	Parenteral; Subcutaneous	100 UI/ML
Injection, suspension	Parenteral; Subcutaneous	40 UI/ML
Injection, suspension	Parenteral	30 IU/mL
Injection, suspension	Parenteral	50 IU/mL
Injection, solution	Intravenous; Parenteral	100 IU/ML
Injection, solution	Intravenous; Parenteral	40 IU/ML
Injection, solution	Parenteral; Subcutaneous	100 IU/ML
Solution	Subcutaneous	100 IU/ml
Injection, solution	Parenteral	100 IU/mL
Injection, solution		100 iu/ml
Injection		100 iu/ml
Injection, solution	Parenteral	100 IE
Injection, solution	Parenteral
Injection, solution	Parenteral	100 IE/ML
Injection, solution	Parenteral	100 I.E./ML
Kit	Respiratory (inhalation)
Powder, metered	Respiratory (inhalation)	12 1/1
Powder, metered	Respiratory (inhalation)	4 1/1
Powder, metered	Respiratory (inhalation)	8 1/1
Injection, suspension	Parenteral	3 ML
Injection, solution	Parenteral	3 ML
Injection, suspension
Solution	Subcutaneous
Aerosol, powder	Respiratory (inhalation)	1 mg/1
Aerosol, powder	Respiratory (inhalation)	3 mg/1
Injection	Parenteral	100 I.E./ml
Injection, solution	Subcutaneous	100 I.E./ml
Injection, solution		100 I.E./ml
Injection, suspension	Parenteral	100 IU
Injection, suspension	Parenteral	1000 IU
Injection, solution	Parenteral	100 IU
Injection, suspension	Parenteral	70 IU
Injection, solution	Intravenous	100 IU/ML
Injection, suspension	Subcutaneous	100 units/mL
Injection, suspension	Subcutaneous	40 units/mL
Suspension	Subcutaneous	30 IU
Injection	Subcutaneous	100 U/ML
Injection, suspension		100 IU
Injection, suspension	Subcutaneous	100 [iU]/1mL
Injection, suspension	Subcutaneous	100
Injection, suspension	Parenteral	300 IU
Suspension	Subcutaneous	100 unit/mL
Suspension	Subcutaneous
Injection, solution	Parenteral	300 IU
Injection, suspension	Parenteral	90 IU
Injection, solution		100 IU
Injection, solution	Parenteral	100 [iU]/1mL
Injection, solution	Subcutaneous	100 [iU]/1mL
Solution	Intramuscular; Intravenous; Subcutaneous	100 unit/mL
Solution	Intramuscular; Subcutaneous
Injection, solution	Subcutaneous	500 [iU]/1mL
Suspension		100 iu/ml
Solution		100 iu/ml
Injection	Subcutaneous	100 IU/mL
Suspension	Subcutaneous	100 IU/ml
Injection, suspension	Parenteral
Injection, suspension	Parenteral	100 IE/ML
Suspension	Intramuscular; Subcutaneous	100 IU
Solution	Subcutaneous	100 IU
Injection, suspension	Subcutaneous	100 IU/ml
Injection, suspension	Subcutaneous	40 IU/ml
Injection, solution	Subcutaneous	100 IU/ml
Injection, solution	Intravenous; Subcutaneous	100 IU/ml
Injection, solution	Intravenous; Subcutaneous	40 IU/ml
Injection, solution	Intramuscular; Parenteral	100 IU/ML
Injection, solution	Intravenous; Parenteral	100 UI/ML
Injection, solution	Parenteral; Subcutaneous	100 UI/ML
Injection, solution	Parenteral; Subcutaneous	40 UI/ML
Injection, suspension	Intramuscular	100 IU/ML
Injection, suspension	Intramuscular	40 IU/ml
Injection, suspension	Intramuscular; Subcutaneous	100 IU/ml
Injection, suspension	Subcutaneous	100 UI/ML
Injection, suspension	Subcutaneous	40 UI/ML
Solution	Subcutaneous	100 UI/ML
Solution	Subcutaneous	40 UI/ML
Injection, suspension	Parenteral	100 I.E./ML
Injection, suspension	Parenteral	25 IU/mL
Injection, suspension	Parenteral	75 IU
Injection, suspension	Parenteral	100 IE
Injection, solution	Intraperitoneal	400 IU/ml
Injection		300 IU/ml
Injection	Subcutaneous	30 %
Injection, suspension	Parenteral	100 IU/ml
Injection, suspension	Subcutaneous	30 iu/1mL
Injection, solution	Intravenous	1.00 [iU]/1mL
Injection, suspension	Subcutaneous	100 [USP'U]/1mL
Suspension	Subcutaneous
Solution	Intramuscular; Intravenous; Subcutaneous
Solution	Intravenous; Subcutaneous	100 IU
Liquid	Intramuscular; Intravenous; Subcutaneous
Injection, suspension	Parenteral; Subcutaneous	40 IU/ML
Injection, suspension	Parenteral	100 UI/ml
Solution	Intramuscular; Intravenous; Subcutaneous	100 IU
Suspension	Subcutaneous	100 IU
Injection, suspension
Suspension
Suspension
Injection, solution
Solution

Prices

Unit description	Cost	Unit
NovoLIN R PenFill 100 unit/ml Solution Five 3ml Cartridges Per Box = 15ml	162.26USD	cartridge
NovoLIN R 100 unit/ml Solution 10ml Vial	73.19USD	vial
Novolin r 100 unit/ml cartridg	33.33USD	ml
NovoLIN R InnoLet 100 unit/ml Solution 3ml Cartridge	24.17USD	cartridge
Humulin N Cartridge 100 unit/ml Cartridge	2.99USD	cartridge
Humulin R Cartridge 100 unit/ml Cartridge	2.99USD	cartridge
Novolin Ge Toronto Penfill 100 unit/ml Cartridge	2.8USD	cartridge
Novolin Ge Nph Penfill 100 unit/ml Cartridge	2.78USD	cartridge
Humulin N 100 unit/ml	2.29USD	cartridge
Humulin R 100 unit/ml	2.29USD	cartridge
Novolin Ge Nph 100 unit/ml	2.14USD	cartridge
Novolin Ge Toronto 100 unit/ml	2.14USD	cartridge

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
USRE37872	No	2002-10-08	2010-02-12
CA2183577	No	2007-10-30	2015-02-07
CA2253393	No	2007-10-09	2017-05-07
US7291132	No	2007-11-06	2024-08-09
US6257233	No	2001-07-10	2019-05-14
US6546929	No	2003-04-15	2019-05-14
US6685967	No	2004-02-03	2018-09-11
US6582728	No	2003-06-24	2020-06-24
US8912193	No	2014-12-16	2029-06-12
US7648960	No	2010-01-19	2020-06-29
US6652885	No	2003-11-25	2020-06-29
US8258095	No	2012-09-04	2029-08-11
US8778403	No	2014-07-15	2030-06-11
US6444226	No	2002-09-03	2020-06-29
US7943572	No	2011-05-17	2026-08-10
US8119593	No	2012-02-21	2029-08-11
US7943178	No	2011-05-17	2020-06-29
US8889099	No	2014-11-18	2020-06-29
US8623817	No	2014-01-07	2029-09-18
US8389470	No	2013-03-05	2020-06-29
US9192675	No	2015-11-24	2029-06-12
US8215300	No	2012-07-10	2022-11-24
US8146588	No	2012-04-03	2023-04-24
US8950397	No	2015-02-10	2021-07-20
US8485180	No	2013-07-16	2030-03-25
US9283193	No	2016-03-15	2026-09-14
US8636001	No	2014-01-28	2032-07-12
US8424518	No	2013-04-23	2031-10-17
US8551528	No	2013-10-08	2030-06-11
US7464706	No	2008-12-16	2023-03-02
US8729019	No	2014-05-20	2028-12-26
US7305986	No	2007-12-11	2023-01-16
US8499757	No	2013-08-06	2032-02-19
US8156936	No	2012-04-17	2023-01-16
US8734845	No	2014-05-27	2030-06-11
US8227409	No	2012-07-24	2031-03-08
US9393372	No	2016-07-19	2029-07-04
US9339615	No	2016-05-17	2029-10-20
US9511198	No	2016-12-06	2030-02-16
US9597374	No	2017-03-21	2031-10-08
US9358352	No	2016-06-07	2031-02-15
US9446133	No	2016-09-20	2029-06-12
US9662461	No	2017-05-30	2029-06-12
US9717689	No	2017-08-01	2026-09-14
US9943571	No	2018-04-17	2029-08-11
US10046031	No	2018-08-14	2029-08-11
US10201672	No	2019-02-12	2030-08-02
US10342938	No	2019-07-09	2029-06-12
US10500159	No	2019-12-10	2030-11-02

Properties

State

Liquid

Experimental Properties

Property	Value	Source
melting point (°C)	81 °C	Khachidze, D.G. et al., J. Biol. Phys. Chem. 1:64-67 (2001)

Targets

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Details1. Insulin receptor

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]

Details2. Insulin-like growth factor 1 receptor

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]

Details3. Retinoblastoma-associated protein

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]

Details4. Carboxypeptidase E

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Modulator

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. Liew CW, Assmann A, Templin AT, Raum JC, Lipson KL, Rajan S, Qiang G, Hu J, Kawamori D, Lindberg I, Philipson LH, Sonenberg N, Goldfine AB, Stoffers DA, Mirmira RG, Urano F, Kulkarni RN: Insulin regulates carboxypeptidase E by modulating translation initiation scaffolding protein eIF4G1 in pancreatic beta cells. Proc Natl Acad Sci U S A. 2014 Jun 3;111(22):E2319-28. doi: 10.1073/pnas.1323066111. Epub 2014 May 19. [PubMed:24843127]

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Drug created on June 13, 2005 13:24 / Updated on March 04, 2021 11:02