Insulin aspart



Insulin aspart is a rapid-acting form of insulin used for glycemic control in type 1 and type 2 diabetes mellitus.

Brand Names
Fiasp, Novolog, Novolog Mix, Novomix, Novorapid, Novorapid Penfill, Ryzodeg
Generic Name
Insulin aspart
DrugBank Accession Number

Insulin aspart is a rapid-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Insulin is typically prescribed for the management of diabetes mellitus to mimic the activity of endogenously produced human insulin, a peptide hormone produced by beta cells of the pancreas that promotes glucose metabolism. Insulin is released from the pancreas following a meal to promote the uptake of glucose from the blood into internal organs and tissues such as the liver, fat cells, and skeletal muscle. Absorption of glucose into cells allows for its transformation into glycogen or fat for storage. Insulin also inhibits hepatic glucose production, enhances protein synthesis, and inhibits lipolysis and proteolysis 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, such as insulin aspart, 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 NovoRapid, insulin aspart 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, NovoRapid 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.

Insulin aspart is a recombinant, biosynthetic, fast-acting insulin analogue. Compared to human insulin, it has a single amino acid substitution at position B28 where proline is replaced with aspartic acid. This substitution decreases its propensity to form hexamers and gives it a higher rate of absorption following subcutaneous administration compared to native insulin. Insulin aspart is produced in a genetically modified strain of Saccharomyces cerevisiae (baker's yeast)

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.

Biologic Classification
Protein Based Therapies
Hormones / Insulins
Protein Structure
Protein Chemical Formula
Protein Average Weight
5825.8 Da
>A chain
>B chain
Download FASTA Format
  • Aspart
  • Aspart Insulin
  • B28-Aspart-Insulin
  • Insulin aspart
  • Insulin aspart protamine
  • Insulin aspart protamine recombinant
  • Insulin aspart recombinant
  • Insulin X14
  • Insulin, aspart protamine, human
  • Insulin, aspart, human
  • Insulin,aspart protamine
  • Insulina asparta
External IDs
  • INA-X14
  • NN-1218
  • NN1218



Insulin aspart is indicated to improve glycemic control in adults and children with diabetes mellitus.5,6

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofDiabetes mellitus••••••••••••••••••••••• •••••• •••••••••
Management ofDiabetes mellitus••• ••••••••••••• ••••••••
Management ofDiabetes mellitus•••••••••••••••••••••• ••••••••
Management ofDiabetes mellitus•••••••••••••••••• •••••••••••••••••• ••••••••
Management ofDiabetes mellitus••••••••••••••••••••••••••• ••••••••
Contraindications & Blackbox Warnings
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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). Insulin aspart is a rapid-acting insulin analogue used to mimic postprandial insulin spikes in diabetic individuals. The onset of action of insulin aspart is 10-15 minutes. Its activity peaks 60-90 minutes following subcutaneous injection and its duration of action is 4-5 hours.

Mechanism of action

Insulin aspart 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. Substitution of the proline residue at B28 with aspartic acid reduces the tendency to form hexamers and results in a faster rate of absorption and onset of action and shorter duration of action.

AInsulin receptor
UInsulin-like growth factor 1 receptor

In studies of healthy volunteers and patients with type 1 diabetes, the median time to maximum concentration of insulin aspart in these trials was 40 to 50 minutes versus 80 to 120 minutes, for regular human insulin respectively. Compared to human insulin, insulin aspart has a faster absorption, a faster onset of action, and a shorter duration of action than regular human insulin after subcutaneous injection. It takes 40 - 50 minutes to reach maximum concentration. When a dose of 0.15 U/kg body weight was injected in type 1 diabetes patients, the mean maximum concentration (Cmax) was 82 mU/L. The site of injection has no impact on extent or speed of absorption.

Volume of distribution

Not Available

Protein binding

Insulin aspart has a low binding affinity to plasma proteins (<10%), similar to that seen with regular human insulin.

Not Available
Route of elimination

Not Available


Elimination half-life was found to be 81 minutes (following subcutaneous administration in healthy subjects).


1.2 L/h/kg

Adverse Effects
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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.

Not Available
Pharmacogenomic Effects/ADRs
Not Available


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.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Insulin aspart.
AcebutololThe therapeutic efficacy of Insulin aspart can be increased when used in combination with Acebutolol.
AcetazolamideThe risk or severity of hypoglycemia can be increased when Acetazolamide is combined with Insulin aspart.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Acetohexamide is combined with Insulin aspart.
AcetophenazineThe therapeutic efficacy of Insulin aspart can be decreased when used in combination with Acetophenazine.
Food Interactions
  • Take with food. Dose adjust as needed. Changes in meal composition may alter the response to insulin aspart.


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International/Other Brands
Novolog FlexPen (Novo Nordisk) / Novolog Penfill (Novo Nordisk)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
.Insulin Aspart Protamine and Insulin AspartInjection, suspension100 [iU]/1mLSubcutaneousA-S Medication Solutions2002-09-11Not applicableUS flag
FiaspInjection, solution100 [iU]/1mLSubcutaneousNovo Nordisk2017-10-20Not applicableUS flag
FiaspSolution100 unit / mLSubcutaneousNovo Nordisk2017-03-03Not applicableCanada flag
FiaspInjection, solution100 U/mlSubcutaneousNovo Nordisk2020-12-16Not applicableEU flag
FiaspInjection, solution100 U/mlIntravenous; SubcutaneousNovo Nordisk2020-12-16Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Novomix 30Insulin aspart (30 unit / mL) + Insulin aspart (70 unit / mL)SuspensionSubcutaneousNovo Nordisk2005-09-12Not applicableCanada flag
Novomix 30Insulin aspart (30 unit / mL) + Insulin aspart (70 unit / mL)SuspensionSubcutaneousNovo Nordisk2005-09-12Not applicableCanada flag
Novomix 30 (flexpen)Insulin aspart (30 %) + Insulin aspart (70 %)SuspensionSubcutaneousNovo NordiskNot applicableNot applicableCanada flag
Novomix 30 (flexpen)Insulin aspart (30 %) + Insulin aspart (70 %)SuspensionSubcutaneousNovo NordiskNot applicableNot applicableCanada flag
NOVOMIX 30 FLEXPEN INJECTION 100 u/mlInsulin aspart (70 %) + Insulin aspart (30 %)InjectionSubcutaneousNOVO NORDISK PHARMA (SINGAPORE) PTE LTD2003-06-02Not applicableSingapore flag


ATC Codes
A10AD06 — Insulin degludec and insulin aspartA10AD05 — Insulin aspartA10AB05 — Insulin aspart
Drug Categories
Chemical TaxonomyProvided by Classyfire
Not Available
Organic Compounds
Super Class
Organic Acids
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Alternative Parents
Not Available
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

CAS number


Synthesis Reference

Ronald E. Zimmerman, David John Stokell, Michael Patrick Akers, "ASPART PROINSULIN COMPOSITIONS AND METHODS OF PRODUCING ASPART INSULIN ANALOGS THEREFROM." U.S. Patent US20120214963, issued August 23, 2012.

General References
  1. Heller S, Kurtzhals P, Verge D, Lindholm A: Insulin aspart: promising early results borne out in clinical practice. Expert Opin Pharmacother. 2002 Feb;3(2):183-95. [Article]
  2. Sciacca L, Cassarino MF, Genua M, Pandini G, Le Moli R, Squatrito S, Vigneri R: Insulin analogues differently activate insulin receptor isoforms and post-receptor signalling. Diabetologia. 2010 Aug;53(8):1743-53. doi: 10.1007/s00125-010-1760-6. Epub 2010 Apr 28. [Article]
  3. Home PD: The pharmacokinetics and pharmacodynamics of rapid-acting insulin analogues and their clinical consequences. Diabetes Obes Metab. 2012 Sep;14(9):780-8. doi: 10.1111/j.1463-1326.2012.01580.x. Epub 2012 Mar 9. [Article]
  4. Varewijck AJ, Janssen JA: Insulin and its analogues and their affinities for the IGF1 receptor. Endocr Relat Cancer. 2012 Sep 5;19(5):F63-75. doi: 10.1530/ERC-12-0026. Print 2012 Oct. [Article]
  5. FDA Approved Drug Products: Novolog (insulin aspart) for SC/IV injection [Link]
  6. EMA Approved Drug Products: Truvelog Mix 30 (insulin aspart and protamine-crystallised insulin aspart, 30:70) subcutaneous injection [Link]
  7. FDA Approved Drug Products: Fiasp (insulin aspart) injection for subcutaneous or intravenous administration (June 2023) [Link]
PubChem Substance
Therapeutic Targets Database
RxList Drug Page Drug Page
FDA label
Download (909 KB)

Clinical Trials

Clinical Trials
4CompletedBasic ScienceHyperglycemia, Postprandial / Type 2 Diabetes Mellitus1
4CompletedBasic ScienceRenal Failure, Chronic Renal Failure1
4CompletedDiagnosticDiabetes / Type 1 Diabetes Mellitus / Type 2 Diabetes Mellitus1
4CompletedHealth Services ResearchType 2 Diabetes Mellitus1
4CompletedPreventionCoronary Artery Disease (CAD)1


Not Available
  • Novo Nordisk Inc.
  • Physicians Total Care Inc.
Dosage Forms
Injection, solutionSubcutaneous100 [iU]/1mL
Injection, solutionSubcutaneous600 nmol/ml
Injection, solutionIntravenous; Subcutaneous600 nmol/ml
SolutionIntravenous; Subcutaneous100 IU
Injection, solutionIntravenous100 U/ML
Injection, solutionIntravenous; Subcutaneous100 [iU]/1mL
Injection, suspensionSubcutaneous100 [iU]/1mL
Injection, suspensionParenteral; Subcutaneous100 U/ML
Injection, suspensionParenteral; Subcutaneous100 IU/ml
Injection; injection, suspensionSubcutaneous100 IU/ml
SuspensionSubcutaneous100 U
SuspensionSubcutaneous70 %
Injection, suspensionSubcutaneous
InjectionSubcutaneous100 U/mL
Injection, suspensionSubcutaneous100 U/ml
SuspensionSubcutaneous100 U/ml
InjectionSubcutaneous100 IU/ml
Injection, solutionIntravenous; Parenteral100 U/ML
Injection, solutionIntravenous; Subcutaneous100 U/ml
Injection, solutionParenteral; Subcutaneous100 U/ML
SolutionSubcutaneous100 unit / mL
SolutionSubcutaneous100 U
Injection, solutionSubcutaneous
InjectionIntravenous; Subcutaneous100 u/ml
Injection, solutionSubcutaneous100 U/ml
Solution100 U/ml
InjectionParenteral100 U/mL
Injection, solutionSubcutaneous
Injection, solutionSubcutaneous180 nmol/ml
SolutionIntravenous; Subcutaneous100 unit / mL
Injection, solution100 iu/1ml
Injection, suspension
Solution100 iu/1ml
Unit descriptionCostUnit
Novolog 100 unit/ml cartridge14.81USD ml
Novolog mix 70-30 cartridge10.45USD ml
Novorapid 100 unit/ml Cartridge3.89USD cartridge
Novorapid 100 unit/ml2.92USD cartridge
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5618913No1997-04-082014-06-07US flag
US8672898Yes2014-03-182022-07-02US flag
US8684969Yes2014-04-012026-04-20US flag
US9132239Yes2015-09-152032-08-01US flag
US8920383Yes2014-12-302027-01-17US flag
US7686786No2010-03-302026-08-03US flag
US6899699Yes2005-05-312022-07-01US flag
US5866538Yes1999-02-022017-12-20US flag
US9108002Yes2015-08-182026-07-26US flag
USRE41956Yes2010-11-232021-07-21US flag
US9265893Yes2016-02-232033-03-23US flag
US6004297Yes1999-12-212019-07-28US flag
USRE43834No2012-11-272019-01-28US flag
US7615532Yes2009-11-102029-12-28US flag
US9486588Yes2016-11-082022-07-02US flag
US9457154Yes2016-10-042028-03-27US flag
USRE46363Yes2017-04-112027-02-03US flag
US9687611Yes2017-06-272027-08-27US flag
US9775953Yes2017-10-032027-01-17US flag
US8324157No2012-12-042030-06-25US flag
US8579869Yes2013-11-122023-12-30US flag
US7762994Yes2010-07-272024-11-23US flag
US9884094No2018-02-062033-05-01US flag
US9861757Yes2018-01-092026-07-20US flag
US9616180Yes2017-04-112026-07-20US flag
US10220155Yes2019-03-052027-01-17US flag
US10357616No2019-07-232026-01-20US flag
US10376652No2019-08-132026-01-20US flag


Experimental Properties
Not Available


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Pharmacological action
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
Uniprot ID
Uniprot Name
Insulin receptor
Molecular Weight
156331.465 Da
  1. Zib I, Raskin P: Novel insulin analogues and its mitogenic potential. Diabetes Obes Metab. 2006 Nov;8(6):611-20. [Article]
  2. De Meyts P: The Insulin Receptor and Its Signal Transduction Network . [Article]
Pharmacological action
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
Uniprot ID
Uniprot Name
Insulin-like growth factor 1 receptor
Molecular Weight
154791.73 Da
  1. Varewijck AJ, Janssen JA: Insulin and its analogues and their affinities for the IGF1 receptor. Endocr Relat Cancer. 2012 Sep 5;19(5):F63-75. doi: 10.1530/ERC-12-0026. Print 2012 Oct. [Article]
  2. Vigneri R, Squatrito S, Sciacca L: Insulin and its analogs: actions via insulin and IGF receptors. Acta Diabetol. 2010 Dec;47(4):271-8. doi: 10.1007/s00592-010-0215-3. Epub 2010 Aug 21. [Article]


Pharmacological action
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
Uniprot ID
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
  1. Barnett CR, Wilson J, Wolf CR, Flatt PR, Ioannides C: Hyperinsulinaemia causes a preferential increase in hepatic P4501A2 activity. Biochem Pharmacol. 1992 Mar 17;43(6):1255-61. doi: 10.1016/0006-2952(92)90500-i. [Article]
  2. Pass GJ, Becker W, Kluge R, Linnartz K, Plum L, Giesen K, Joost HG: Effect of hyperinsulinemia and type 2 diabetes-like hyperglycemia on expression of hepatic cytochrome p450 and glutathione s-transferase isoforms in a New Zealand obese-derived mouse backcross population. J Pharmacol Exp Ther. 2002 Aug;302(2):442-50. doi: 10.1124/jpet.102.033553. [Article]
  3. Flockhart Table of Drug Interactions [Link]

Drug created at June 30, 2007 14:44 / Updated at July 01, 2023 10:08