Liraglutide
Identification
- Name
- Liraglutide
- Accession Number
- DB06655
- Description
Victoza contains liraglutide, a synthetic analog of human glucagon-like peptide-1(GLP-1) and acts as a GLP-1 receptor agonistLabel,1. Liraglutide is 97% homologous to native human GLP-1 by substituting arginine for lysine at position 341. Liraglutide is made by attaching a C-16 fatty acid (palmitic acid) with a glutamic acid spacer on the remaining lysine residue at position 26 of the peptide precursor1. Liraglutide was granted FDA approval on Januray 25, 20104.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Chemical Formula
- C172H265N43O51
- Protein Average Weight
- 3751.2 Da
- Sequences
>Liraglutide Sequence (gamma-E-palmitoyl at E21) HAEGTFTSDVSSYLEGQAAKEEFIAWLVRGRG
Download FASTA Format- Synonyms
- Arg34Lys26-(N-ε-(γ-Glu(N-α-hexadecanoyl)))-GLP-1[7-37]
- Liraglutida
- Liraglutide (genetical recombination)
- Liraglutide (rDNA origin)
- Liraglutide recombinant
- Liraglutidum
- N²⁶-(hexadecanoyl-gamma-glutamyle)-[34-arginine]GLP-1-(7-37)-peptide
- N²⁶-(N-Hexadecanoyl-L-gamma-glutamyl)-[34-L-arginine]glucagon-like peptide 1-(7-37)-peptide
- External IDs
- NN 2211
- NN-2211
- NN-9924
- NN2211
- NN9924
- NNC 90-1170
- NNC-90-1170
Pharmacology
- Indication
Liraglutide is indicated in combination with diet and exercise to improve glycemic control in patients 10 years and older with type 2 diabetes mellitusLabel,5. It is also indicated to reduce the risk of major adverse cardiovascular events in patients with type 2 diabetes mellitus as well as cardiovascular diseaseLabel.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Liraglutide is a once-daily GLP-1 derivative for the treatment of type 2 diabetesLabel,2. The prolonged action of liraglutide is achieved by attaching a fatty acid molecule at position 26 of the GLP-1 molecule, enabling it to bind reversibly to albumin within the subcutaneous tissue and bloodstream and be released slowly over timeLabel,2,3. Binding with albumin results in slower degradation and reduced elimination of liraglutide from the circulation by the kidneys compared to GLP-12,3. The effect of liraglutide is the increased secretion of insulin and decreased secretion of glucagon in response to glucose as well as slower gastric emptyingLabel. Liraglutide also does not adversely affect glucagon secretion in response to low blood sugarLabel,2.
- Mechanism of action
Liraglutide is an acylated synthetic glucagon-like peptide-1 analogLabel,1,2. Liraglutide is an agonist of the glucagon-like peptide-1 receptor which is coupled to adenylate cyclaseLabel. The increase in cyclic AMP stimulates the glucose dependant release of insulin, inhibits the glucose dependant release of glucagon, and slows gastric emptying to increase control of blood sugarLabel,3.
Target Actions Organism AGlucagon-like peptide 1 receptor agonistHumans - Absorption
Bioavailability of liraglutide after subcutaneous injection is approximately 55%Label and maximum concentrations are reached after 11.7 hours1.
- Volume of distribution
13LLabel.
- Protein binding
>98%Label.
- Metabolism
Liraglutide is less sensitive to metabolism than the endogenous GLP-1 and so is more slowly metabolized by dipeptidyl peptidase-4 and neutral endopeptidase to various smaller polypeptides which have not all been structurally determined1. A portion of Liraglutide may be completely metabolized to carbon dioxide and water1.
- Route of elimination
6% excreted in urine and 5% excreted in feces1.
- Half-life
Terminal half life of 13 hours1.
- Clearance
1.2L/hLabel.
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
There is no clinical significance of race or ethnicity on the safety or efficacy of liraglutideLabel. Geriatric patients do not experience clinically significant differences in pharmacokinetics though patients at an especially advanced age may be more susceptible to adverse effectsLabel. Female patients have reduced clearance of liraglutide but no dose adjustment is necessaryLabel. The risk and benefit of liraglutide in pregnancy must be weighed before prescribingLabel. In animal studies, liraglutide is associated with an increased risk of embryonic death and fetal abnormalities though an HbA1c > 7 is also associated with a 20-25% risk of birth defectsLabel. In animal studies, liraglutide is present in the milk of lactating rats at half the plasma concentration of the mother but these results may not translate to humansLabel. Because it is not known if liraglutide is present in breast milk and the effects on infants are also unknown, the risk and benefit of liraglutide in breastfeeding must be considered before prescribingLabel. Liraglutide was shown to be safe and effective in patients up to 160kg in weight but has not been studied in patients at a higher weightLabel. A patient's weight significantly affects the pharmacokinetics of liraglutideLabel. Liraglutide has not been investigated for use in pediatric patientsLabel. No dosage adjustments are necessary in patients with renal impairment but studies have not been performed in patients with end stage renal diseaseLabel. There are no recommendations on dosage adjustment in patients with hepatic impairment, though caution should still be exercised when prescribing to this populationLabel.
- 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.
Drug Interaction Unlock Additional DataAcarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Liraglutide. Acebutolol The therapeutic efficacy of Liraglutide can be increased when used in combination with Acebutolol. Acetazolamide The therapeutic efficacy of Liraglutide can be increased when used in combination with Acetazolamide. Acetohexamide Liraglutide may increase the hypoglycemic activities of Acetohexamide. Acetyl sulfisoxazole The therapeutic efficacy of Liraglutide 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 Liraglutide. Albiglutide The risk or severity of hypoglycemia can be increased when Liraglutide is combined with Albiglutide. Alclometasone The risk or severity of hyperglycemia can be increased when Alclometasone is combined with Liraglutide. Alogliptin The risk or severity of hypoglycemia can be increased when Alogliptin is combined with Liraglutide. Amcinonide The risk or severity of hyperglycemia can be increased when Amcinonide is combined with Liraglutide. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Take with or without food.
Products
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataSaxenda Solution 6 mg Subcutaneous Novo Nordisk 2015-05-27 Not applicable Canada 
Saxenda Injection, solution 6 mg/ml Subcutaneous Novo Nordisk 2015-03-23 Not applicable EU 
Saxenda Injection, solution 6 mg/1mL Subcutaneous A-S Medication Solutions 2014-12-31 Not applicable US 
Saxenda Injection, solution 6 mg/ml Subcutaneous Novo Nordisk 2015-03-23 Not applicable EU Saxenda Injection, solution 6 mg/1mL Subcutaneous Novo Nordisk 2014-12-31 Not applicable US Saxenda Injection, solution 6 mg/ml Subcutaneous Novo Nordisk 2015-03-23 Not applicable EU Victoza Injection, solution 6 mg/ml Subcutaneous Novo Nordisk 2009-06-30 Not applicable EU Victoza Injection 6 mg/1mL Subcutaneous A-S Medication Solutions 2010-01-25 2019-02-25 US Victoza Injection, solution 6 mg/ml Subcutaneous Novo Nordisk 2009-06-30 Not applicable EU Victoza Injection 6 mg/1mL Subcutaneous A-S Medication Solutions 2010-01-25 Not applicable US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Xultophy Liraglutide (3.6 mg/ml) + Insulin degludec (100 U/ml) Injection, solution Subcutaneous Novo Nordisk 2014-09-18 Not applicable EU Xultophy Liraglutide (3.6 mg/ml) + Insulin degludec (100 U/ml) Injection, solution Subcutaneous Novo Nordisk 2014-09-18 Not applicable EU Xultophy Liraglutide (3.6 mg) + Insulin degludec (100 unit) Solution Subcutaneous Novo Nordisk 2018-06-06 Not applicable Canada Xultophy Liraglutide (3.6 mg/ml) + Insulin degludec (100 U/ml) Injection, solution Subcutaneous Novo Nordisk 2014-09-18 Not applicable EU Xultophy 100/3.6 Liraglutide (3.6 mg/1mL) + Insulin degludec (100 [iU]/1mL) Injection, solution Subcutaneous Novo Nordisk 2016-11-21 Not applicable US Xultophy Pre-filled Pen Liraglutide (3.6 mg/ml) + Insulin degludec (100 U/ml) Injection, solution Subcutaneous Novo Nordisk 2014-09-18 Not applicable EU
Categories
- ATC Codes
- A10AE56 — Insulin degludec and liraglutide
- 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
- Drugs Used in Diabetes
- Gastrointestinal Hormones
- GLP-1 Agonists
- Glucagon-Like Peptide 1
- Glucagon-like Peptide-1 (GLP-1) Agonists
- Glucagon-like peptide-1 (GLP-1) analogues
- Glucagon-Like Peptides
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypoglycemia-Associated Agents
- Incretin Mimetics
- Incretins
- Pancreatic Hormones
- Peptide Hormones
- Peptides
- Proglucagon
- 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
- 839I73S42A
- CAS number
- 204656-20-2
References
- General References
- Malm-Erjefalt M, Bjornsdottir I, Vanggaard J, Helleberg H, Larsen U, Oosterhuis B, van Lier JJ, Zdravkovic M, Olsen AK: Metabolism and excretion of the once-daily human glucagon-like peptide-1 analog liraglutide in healthy male subjects and its in vitro degradation by dipeptidyl peptidase IV and neutral endopeptidase. Drug Metab Dispos. 2010 Nov;38(11):1944-53. doi: 10.1124/dmd.110.034066. Epub 2010 Aug 13. [PubMed:20709939]
- Knudsen B, Jesper Lau: The Discovery and Development of Liraglutide and Semaglutide Frontiers in Endocrinology.
- Russell-Jones D: Molecular, pharmacological and clinical aspects of liraglutide, a once-daily human GLP-1 analogue. Mol Cell Endocrinol. 2009 Jan 15;297(1-2):137-40. doi: 10.1016/j.mce.2008.11.018. Epub 2008 Nov 25. [PubMed:19041364]
- FDA Drug Approval Package: Liraglutide [Link]
- FDA News Release: Liraglutide Indication [Link]
- External Links
- UniProt
- P01275
- KEGG Drug
- D06404
- PubChem Substance
- 347910356
- 475968
- ChEBI
- 71193
- ChEMBL
- CHEMBL1201866
- PharmGKB
- PA165958364
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Liraglutide
- AHFS Codes
- 68:20.06 — Incretin Mimetics
- FDA label
- Download (1.32 MB)
- MSDS
- Download (569 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Basic Science Insulin Resistance 1 4 Active Not Recruiting Other BMI >30 kg/m2 1 4 Active Not Recruiting Prevention Cardiovascular Heart Disease / Lipid Metabolism Disorders / Obesity, Visceral 1 4 Active Not Recruiting Prevention Gestational Diabetes Mellitus (GDM) 1 4 Active Not Recruiting Treatment BMI >30 kg/m2 3 4 Active Not Recruiting Treatment Type 2 Diabetes Mellitus 1 4 Active Not Recruiting Treatment Type II Diabetes in Subjects BMI 27 to 32 1 4 Completed Basic Science Diabetes / Effects of Liraglutide Administration on Brain Activity / Hunger / Weight Loss 1 4 Completed Basic Science Healthy Human Male Subjects 1 4 Completed Basic Science Systolic Hypertension / Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Cutaneous 6 MG/ML Injection, solution Subcutaneous 6 mg/ml Injection, solution Subcutaneous 6 mg/1mL Injection 6 mg/ml Solution Solution Subcutaneous 6 mg Injection Injection Subcutaneous 6 mg/1mL Injection, solution 18 mg/3mL Injection, solution Cutaneous; Parenteral 6 MG/ML Injection, solution 100 iu/1mL Injection, solution Parenteral; Subcutaneous 100 IU/ml Injection, solution Subcutaneous Solution Subcutaneous Injection Subcutaneous 3.6 mg/mL Solution Subcutaneous 100 U - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataCA2264243 No 2004-10-05 2017-08-22 Canada 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 US9108002 Yes 2015-08-18 2026-07-26 US USRE41956 Yes 2010-11-23 2021-07-21 US US9265893 Yes 2016-02-23 2033-03-23 US US6004297 Yes 1999-12-21 2019-07-28 US USRE43834 No 2012-11-27 2019-01-28 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 US8114833 Yes 2012-02-14 2026-02-13 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 US9968659 Yes 2018-05-15 2037-07-09 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 Additional Data Available- Filed On
Properties
- State
- Solid
- Experimental Properties
Property Value Source isoelectric point 4.9 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206321Orig1s000ChemR.pdf
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Transmembrane signaling receptor activity
- Specific Function
- This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- GLP1R
- Uniprot ID
- P43220
- Uniprot Name
- Glucagon-like peptide 1 receptor
- Molecular Weight
- 53025.22 Da
References
- Bock T, Pakkenberg B, Buschard K: The endocrine pancreas in non-diabetic rats after short-term and long-term treatment with the long-acting GLP-1 derivative NN2211. APMIS. 2003 Dec;111(12):1117-24. [PubMed:14678021]
- Larsen PJ, Wulff EM, Gotfredsen CF, Brand CL, Sturis J, Vrang N, Knudsen LB, Lykkegaard K: Combination of the insulin sensitizer, pioglitazone, and the long-acting GLP-1 human analog, liraglutide, exerts potent synergistic glucose-lowering efficacy in severely diabetic ZDF rats. Diabetes Obes Metab. 2008 Apr;10(4):301-11. doi: 10.1111/j.1463-1326.2008.00865.x. [PubMed:18333889]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Virus receptor activity
- Specific Function
- Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by bindi...
- Gene Name
- DPP4
- Uniprot ID
- P27487
- Uniprot Name
- Dipeptidyl peptidase 4
- Molecular Weight
- 88277.935 Da
References
- Malm-Erjefalt M, Bjornsdottir I, Vanggaard J, Helleberg H, Larsen U, Oosterhuis B, van Lier JJ, Zdravkovic M, Olsen AK: Metabolism and excretion of the once-daily human glucagon-like peptide-1 analog liraglutide in healthy male subjects and its in vitro degradation by dipeptidyl peptidase IV and neutral endopeptidase. Drug Metab Dispos. 2010 Nov;38(11):1944-53. doi: 10.1124/dmd.110.034066. Epub 2010 Aug 13. [PubMed:20709939]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Zinc ion binding
- Specific Function
- Thermolysin-like specificity, but is almost confined on acting on polypeptides of up to 30 amino acids (PubMed:15283675, PubMed:8168535). Biologically important in the destruction of opioid peptide...
- Gene Name
- MME
- Uniprot ID
- P08473
- Uniprot Name
- Neprilysin
- Molecular Weight
- 85513.225 Da
References
- Malm-Erjefalt M, Bjornsdottir I, Vanggaard J, Helleberg H, Larsen U, Oosterhuis B, van Lier JJ, Zdravkovic M, Olsen AK: Metabolism and excretion of the once-daily human glucagon-like peptide-1 analog liraglutide in healthy male subjects and its in vitro degradation by dipeptidyl peptidase IV and neutral endopeptidase. Drug Metab Dispos. 2010 Nov;38(11):1944-53. doi: 10.1124/dmd.110.034066. Epub 2010 Aug 13. [PubMed:20709939]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Knudsen B, Jesper Lau: The Discovery and Development of Liraglutide and Semaglutide Frontiers in Endocrinology.
Drug created on March 19, 2008 10:45 / Updated on October 23, 2020 21:53
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