Identification
- Summary
Insulin degludec is a long acting insulin used to treat hyperglycemia caused by type 1 and 2 diabetes mellitus.
- Brand Names
- Ryzodeg, Tresiba, Xultophy
- Generic Name
- Insulin degludec
- DrugBank Accession Number
- DB09564
- Background
Insulin degludec is an ultra-long-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes.1,2,3,4,5 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.1,2,3,4,5 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.1,2,3,4,5 Absorption of glucose into cells allows for its transformation into glycogen or fat for storage.1,2,3,4,5 Insulin also inhibits hepatic glucose production, enhances protein synthesis, and inhibits lipolysis and proteolysis among many other functions.1,2,3,4,5
Insulin is an essential 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.1,2,3,4,5 As a result, people with T1D rely primarily on exogenous forms of insulin, such as insulin degludec, to lower glucose levels in the blood.1,2,3,4,5 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.1,2,3,4,5 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.1,2,3,4,5 Insulin is typically prescribed later in the course of T2D, after 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.1,2,3,4,5
Marketed as the brand name product Tresiba, insulin degludec has a duration of action up to 42 hours allowing for once-daily dosing, typically at bedtime.1,2,3,4,5 Due to its duration of action, Tresiba is considered "basal insulin" as it provides low concentrations of background insulin that can keep blood sugar stable between meals or overnight.1,2,3,4,5 Basal insulin is often combined with short-acting "bolus insulin" such as Insulin lispro, Insulin glulisine, or Insulin aspart to provide higher doses of insulin required following meals. Use of basal and bolus insulin together is intended to mimic the pancreas' production of endogenous insulin, with the goal of avoiding any periods of hypoglycemia.1,2,3,4,5
Compared to endogenous insulin, insulin degludec has an added hexadecanedioic acid on lysine at the B29 position, allowing for the formation of multi-hexamers.1,2,3,4,5 When injected subcutaneously, these multi-hexamers form a drug depot store from which monomers are slowly and continuously absorbed into circulation.1,2,3,4,5 As a result, Insulin Degludec has a protracted time action profile due to the delayed absorption from subcutaneous tissue depots into the systemic circulation.1,2,3,4,5 Compared to available long-acting analogs such as Insulin glargine and Insulin detemir, which have a duration of action of 20-24 hours, insulin degludec provides a consistent level of basal insulin over 42 hours with a low peak: trough ratio.1,2,3,4,5 Limitations of shorter-acting analogs include more frequent dosing and less stable pharmacokinetics, which may negatively impact patient adherence and glucose control, particularly nocturnal control.1,2,3,4,5
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.1,2,3,4,5 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.1,2,3,4,5
Insulin Degludec was approved by the FDA in September 2015 as the product Tresiba, for use in providing glycemic control to adults with diabetes mellitus.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Hormones / Insulins - Protein Structure
- Protein Chemical Formula
- C274H411N65O81S6
- Protein Average Weight
- 6103.97 Da
- Sequences
>A Chain GIVEQCCTSICSLYQLENYCN
>B Chain FVNQHLCGSHLVEALYLVCGERGFFYTPK
Download FASTA FormatReferences:
- FDA Approved Drug Products: Tresiba (insulin degludec) for subcutaneous injection [Link]
- Synonyms
- Insulin degludec
- Insulina degludec
- External IDs
- NN-1250
- NN1250
Pharmacology
- Indication
Insulin degludec is indicated to improve glycemic control in patients 1 year of age and older with diabetes mellitus.10
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to manage Diabetes mellitus Combination Product in combination with: Insulin aspart (DB01306) •••••••••••• ••••••••••• •••••• •••••••• •••••••••• •••••••• Management of Diabetes mellitus •••••••••••• ••••• •••••••••• •••••••• Management of Diabetes mellitus •••••••••••• •••••• •••••••• •••••••••• •••••••• Management of Diabetes mellitus type 1 •••••••••••• ••••••••• •••••••••• •••••••• Used as adjunct in combination to manage Type 2 diabetes mellitus Combination Product in combination with: Liraglutide (DB06655) •••••••••••• ••••• •••••••••••• •••• •••• •• ••••• ••••••••••• •••••••••• •••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Insulin is a natural hormone produced by beta cells of the pancreas. In nondiabetic individuals, the pancreas produces a continuous supply of low basal insulin levels and spikes of insulin following meals.1,2,3,4,5 Increased insulin secretion following meals is responsible for the metabolic changes that occur as the body transitions from a postabsorptive to an absorptive state.1,2,3,4,5 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 the liver, muscle and adipose tissue, and modifies the activity of numerous enzymes involved in glycogen synthesis and glycolysis.1,2,3,4,5 Insulin also promotes growth and is required for the actions of growth hormone (e.g. protein synthesis, cell division, DNA synthesis).1,2,3,4,5 Insulin detemir is a long-acting insulin analogue with a flat and predictable action profile.1,2,3,4,5 It mimics the basal insulin levels in diabetic individuals. The onset of action of insulin detemir is 1 to 2 hours and its duration of action is up to 24 hours. Interestingly, it has a lower affinity (30%) for the insulin receptor than human insulin.1,2,3,4,5
- Mechanism of action
Insulin detemir binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units.8 The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor.8 The bound receptor autophosphorylates and phosphorylates numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc, and Gab 1.8 Activation of these proteins leads to activation of downstream signaling molecules including PI3 kinase and Akt.8 Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC), both of which play critical roles in metabolism and catabolism.8
Target Actions Organism AInsulin receptor agonistHumans UInsulin-like growth factor 1 receptor activatorHumans - Absorption
In patients with type 1 diabetes, after 8 days of once-daily subcutaneous dosing with 0.4 U/kg, maximum insulin degludec concentrations of 4472 pmol/L were attained at a median of 9 hours (tmax).10 After the first dose, the median onset of appearance was around one hour. The glucose-lowering effect lasted at least 42 hours after the last of 8 once-daily injections. Insulin degludec concentration reaches steady-state levels after 3-4 days.10
- Volume of distribution
Using a one-compartment pharmacokinetics model, the apparent volume of distribution was estimated to be 10.6 L for the pediatric population and 13.9 L for the adult population.14
- Protein binding
The affinity of insulin degludec to serum albumin corresponds to a plasma protein binding of >99% in human plasma.10 The results of the in vitro protein binding studies demonstrate that there is no clinically relevant interaction between insulin degludec and other protein-bound drugs.10
- Metabolism
All insulin degludec metabolites are inactive.10 The liver and kidney play the major role in metabolizing insulin.7However, while the liver predominantly metabolizes endogenous insulin, exogenous insulin is primarily metabolized due to the kidney since it is not directly delivered into the portal system.7
- Route of elimination
30 to 80% of circulating insulin is removed by the kidney.6
- Half-life
The half-life after subcutaneous administration is determined primarily by the rate of absorption from the subcutaneous tissue. On average, the half-life at a steady state is approximately 25 hours independent of dose.10
- Clearance
The mean apparent clearance of insulin degludec is 0.03 L/kg (2.1 L/h in 70 kg individuals) after a single subcutaneous dose of 0.4 units/kg.10
- Adverse Effects
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An excess of insulin relative to food intake, energy expenditure, or both may lead to severe and sometimes prolonged and life-threatening hypoglycemia and hypokalemia [see Warnings and Precautions (5.3, 5.6)]. Mild episodes of hypoglycemia can usually be treated with oral glucose. Lowering the insulin dosage and adjusting meal patterns or exercise may be needed. More severe episodes of hypoglycemia with coma, seizure, or neurologic impairment may be treated with glucagon for emergency use or concentrated intravenous glucose. After apparent clinical recovery from hypoglycemia, continued observation and additional carbohydrate intake may be necessary to avoid the reoccurrence of hypoglycemia. Hypokalemia must be corrected appropriately.10
Insulin degludec was investigated in studies covering fertility, embryo-fetal development, and pre and post-natal development in rats and during the period of embryo-fetal development in rabbits. Human insulin (NPH insulin) was included as a comparator. In these studies, insulin degludec caused pre and post-implantation losses and visceral/skeletal abnormalities when given subcutaneously at up to 21 U/kg/day in rats and 3.3 U/kg/day in rabbits, resulting in 5 times (rat) and 10 times (rabbit) the human exposure (AUC) at a human subcutaneous dose of 0.75 U/kg/day. Overall, the effects of insulin degludec were similar to those observed with human insulin, which was probably secondary to maternal hypoglycemia.10
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Insulin degludec. Acebutolol The therapeutic efficacy of Insulin degludec can be increased when used in combination with Acebutolol. Acetazolamide The risk or severity of hypoglycemia can be increased when Acetazolamide is combined with Insulin degludec. Acetohexamide The risk or severity of hypoglycemia can be increased when Acetohexamide is combined with Insulin degludec. Acetophenazine The therapeutic efficacy of Insulin degludec can be decreased when used in combination with Acetophenazine. - Food Interactions
- Avoid alcohol. Alcohol may impair blood glucose control.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Insulin Degludec Injection, solution 100 U/1mL Subcutaneous Novo Nordisk Pharma, Inc. 2022-07-01 Not applicable US 
Insulin Degludec Injection, solution 200 U/1mL Subcutaneous Novo Nordisk Pharma, Inc. 2022-07-01 Not applicable US Insulin Degludec Injection, solution 100 U/1mL Subcutaneous Novo Nordisk Pharma, Inc. 2022-07-01 Not applicable US Tresiba Injection, solution 100 U/ml Subcutaneous Novo Nordisk 2016-09-08 Not applicable EU 
Tresiba Injection, solution 200 U/ml Subcutaneous Novo Nordisk 2016-09-08 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image RYZODEG Insulin degludec (70 U/ML) + Insulin aspart (30 U/mL) Injection, solution Subcutaneous Novo Nordisk 2014-07-08 Not applicable Italy 
RYZODEG Insulin degludec (70 U/ML) + Insulin aspart (30 U/mL) Injection, solution Subcutaneous Novo Nordisk 2014-07-08 Not applicable Italy Ryzodeg Insulin degludec (2.56 mg/ml) + Insulin aspart (1.05 mg/ml) Injection, solution Subcutaneous Novo Nordisk 2016-09-08 Not applicable EU RYZODEG Insulin degludec (70 U/ML) + Insulin aspart (30 U/mL) Injection, solution Subcutaneous Novo Nordisk 2014-10-06 Not applicable Italy Ryzodeg Insulin degludec (2.56 mg/ml) + Insulin aspart (1.05 mg/ml) Injection, solution Subcutaneous Novo Nordisk 2016-09-08 Not applicable EU
Categories
- ATC Codes
- A10AD06 — Insulin degludec and insulin aspart
- 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
- A10AE — Insulins and analogues for injection, long-acting
- 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
- Insulin
- Insulin Analog
- Insulin, Long-Acting
- Long-acting Insulins
- Pancreatic Hormones
- Peptide Hormones
- Peptides
- 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
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 54Q18076QB
- CAS number
- 844439-96-9
References
- General References
- Garber AJ, King AB, Del Prato S, Sreenan S, Balci MK, Munoz-Torres M, Rosenstock J, Endahl LA, Francisco AM, Hollander P: Insulin degludec, an ultra-longacting basal insulin, versus insulin glargine in basal-bolus treatment with mealtime insulin aspart in type 2 diabetes (BEGIN Basal-Bolus Type 2): a phase 3, randomised, open-label, treat-to-target non-inferiority trial. Lancet. 2012 Apr 21;379(9825):1498-507. doi: 10.1016/S0140-6736(12)60205-0. [Article]
- Wang F, Surh J, Kaur M: Insulin degludec as an ultralong-acting basal insulin once a day: a systematic review. Diabetes Metab Syndr Obes. 2012;5:191-204. doi: 10.2147/DMSO.S21979. Epub 2012 Jul 5. [Article]
- Haahr H, Heise T: A review of the pharmacological properties of insulin degludec and their clinical relevance. Clin Pharmacokinet. 2014 Sep;53(9):787-800. doi: 10.1007/s40262-014-0165-y. [Article]
- Jonassen I, Havelund S, Hoeg-Jensen T, Steensgaard DB, Wahlund PO, Ribel U: Design of the novel protraction mechanism of insulin degludec, an ultra-long-acting basal insulin. Pharm Res. 2012 Aug;29(8):2104-14. doi: 10.1007/s11095-012-0739-z. Epub 2012 Apr 7. [Article]
- Thuillier P, Alavi Z, Kerlan V: Long-term safety and efficacy of insulin degludec in the management of type 2 diabetes. Diabetes Metab Syndr Obes. 2015 Oct 1;8:483-93. doi: 10.2147/DMSO.S54953. eCollection 2015. [Article]
- Morello CM: Pharmacokinetics and pharmacodynamics of insulin analogs in special populations with type 2 diabetes mellitus. Int J Gen Med. 2011;4:827-35. doi: 10.2147/IJGM.S26889. Epub 2011 Dec 12. [Article]
- Donner T, Sarkar S: Insulin - Pharmacology, Therapeutic Regimens, and Principles of Intensive Insulin Therapy . [Article]
- De Meyts P: The Insulin Receptor and Its Signal Transduction Network . [Article]
- FDA Approved Drug Products: Tresiba (insulin degludec) for subcutaneous injection [Link]
- FDA Approved Drug Products: Tresiba (insulin degludec) for subcutaneous injection 2022 [Link]
- FDA Approved Drug Products: XULTOPHY® 100/3.6 (insulin degludec and liraglutide) injection, for subcutaneous use [Link]
- EMA Approved Drug Proucts: RYZODEG® 70/30 (insulin degludec and insulin aspart injection), for 7 subcutaneous use [Link]
- Health Canada Approved Drug Proucts: Tresiba (insulin degludec) for subcutaneous injection [Link]
- Clinical Pharmacology Review: Tresiba [Link]
- External Links
- KEGG Drug
- D09727
- PubChem Substance
- 347910463
- 1670007
- ChEMBL
- CHEMBL2107869
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Insulin_degludec
- FDA label
- Download (7.77 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Type 1 Diabetes Mellitus 1 4 Completed Treatment Nocturnal Hypoglycemia / Recurrent Severe Hypoglycaemia / Type 1 Diabetes Mellitus 1 4 Completed Treatment Type 1 Diabetes Mellitus 7 4 Completed Treatment Type 2 Diabetes Mellitus 8 4 Recruiting Treatment Diabetes Mellitus / Diabetic Kidney Disease (DKD) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Subcutaneous Injection Injection, solution Subcutaneous 100 U/1mL Injection, solution Subcutaneous 200 U/1mL Solution Subcutaneous 100 U Solution Subcutaneous 100 unit / mL Solution Subcutaneous 200 unit / mL Injection, solution Subcutaneous Solution Subcutaneous 100 IU Solution Subcutaneous 10000000 IU Injection, solution Subcutaneous 100 U/ml Injection, solution Subcutaneous 200 U/ml Solution Subcutaneous 200 IU Injection Subcutaneous 100 IU/ml Injection, solution Parenteral; Subcutaneous Solution Subcutaneous Injection Subcutaneous Injection, solution Injection, solution Subcutaneous 100 iu/1ml - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8672898 Yes 2014-03-18 2022-07-02 US US8684969 Yes 2014-04-01 2026-04-20 US US9132239 Yes 2015-09-15 2032-08-01 US US8920383 Yes 2014-12-30 2027-01-17 US US7686786 No 2010-03-30 2026-08-03 US US6899699 Yes 2005-05-31 2022-07-01 US US5866538 Yes 1999-02-02 2017-12-20 US US9108002 Yes 2015-08-18 2026-07-26 US US6458924 No 2002-10-01 2017-08-22 US US6268343 Yes 2001-07-31 2023-02-22 US US8846618 Yes 2014-09-30 2022-12-27 US US7235627 No 2007-06-26 2017-08-22 US US7615532 Yes 2009-11-10 2029-12-28 US US9486588 Yes 2016-11-08 2022-07-02 US US9457154 Yes 2016-10-04 2028-03-27 US USRE46363 Yes 2017-04-11 2027-02-03 US US8937042 Yes 2015-01-20 2029-11-05 US US9687611 Yes 2017-06-27 2027-08-27 US US9775953 Yes 2017-10-03 2027-01-17 US US8579869 Yes 2013-11-12 2023-12-30 US US7762994 Yes 2010-07-27 2024-11-23 US US9884094 No 2018-02-06 2033-05-01 US US9861757 Yes 2018-01-09 2026-07-20 US US9616180 Yes 2017-04-11 2026-07-20 US US10220155 Yes 2019-03-05 2027-01-17 US US10357616 No 2019-07-23 2026-01-20 US US10376652 No 2019-08-13 2026-01-20 US
Properties
- State
- Liquid
- Experimental Properties
- 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
- De Meyts P: The Insulin Receptor and Its Signal Transduction Network . [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Activator
- 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
- Wang F, Surh J, Kaur M: Insulin degludec as an ultralong-acting basal insulin once a day: a systematic review. Diabetes Metab Syndr Obes. 2012;5:191-204. doi: 10.2147/DMSO.S21979. Epub 2012 Jul 5. [Article]
- 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]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- 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]
- 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]
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- Farris W, Mansourian S, Chang Y, Lindsley L, Eckman EA, Frosch MP, Eckman CB, Tanzi RE, Selkoe DJ, Guenette S: Insulin-degrading enzyme regulates the levels of insulin, amyloid beta-protein, and the beta-amyloid precursor protein intracellular domain in vivo. Proc Natl Acad Sci U S A. 2003 Apr 1;100(7):4162-7. doi: 10.1073/pnas.0230450100. Epub 2003 Mar 12. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Ryberg LA, Sonderby P, Barrientos F, Bukrinski JT, Peters GHJ, Harris P: Solution structures of long-acting insulin analogues and their complexes with albumin. Acta Crystallogr D Struct Biol. 2019 Mar 1;75(Pt 3):272-282. doi: 10.1107/S2059798318017552. Epub 2019 Feb 26. [Article]
Drug created at November 30, 2015 19:10 / Updated at September 05, 2022 12:50