Investigational Drug Details
| Drug ID: | D207 |
| Drug Name: | Liraglutide |
| Synonyms: | Arg34Lys26-(N-ε-(γ-Glu(N-α-hexadecanoyl)))-GLP-1[7-37]; Liraglutide; Liraglutide (genetical recombination); Liraglutide (rDNA origin); Liraglutide recombinant; 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 |
| Type: | Biological drug |
| DrugBank ID: | DB06655 |
| DrugBank Description: | Victoza contains liraglutide, a synthetic analog of human glucagon-like peptide-1(GLP-1) and acts as a GLP-1 receptor agonist. Liraglutide is 97% homologous to native human GLP-1 by substituting arginine for lysine at position 34. 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 precursor. Liraglutide was granted FDA approval on Januray 25, 2010. |
| PubChem ID: | 16134956 |
| CasNo: | 204656-20-2 |
| Repositioning for NAFLD: | Yes |
| SMILES: | O=C(N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1[nH]cnc1)C)CCC(=O)O)[C@H](O)C)Cc1ccccc1)[C@H](O)C)CO)CC(=O)O)C(C)C)CO)CO)Cc1ccc(O)cc1)CC(C)C)CCC(=O)O)CCC(=O)N)C)C)CCCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC)C(=O)O)CCC(=O)O)Cc1ccccc1)[C@H](CC)C)C)Cc1c2c([nH]c1)cccc2)CC(C)C |
| Structure: |
|
| InChiKey: | YSDQQAXHVYUZIW-QCIJIYAXSA-N |
| Molecular Weight: | 3751.262 |
| DrugBank Targets: | Glucagon-like peptide 1 receptor agonist |
| DrugBank MoA: | Liraglutide is an acylated synthetic glucagon-like peptide-1 analog. Liraglutide is an agonist of the glucagon-like peptide-1 receptor which is coupled to adenylate cyclase. 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 sugar. |
| DrugBank Pharmacology: | Liraglutide is a once-daily GLP-1 derivative for the treatment of type 2 diabetes. 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 time. Binding with albumin results in slower degradation and reduced elimination of liraglutide from the circulation by the kidneys compared to GLP-1. The effect of liraglutide is the increased secretion of insulin and decreased secretion of glucagon in response to glucose as well as slower gastric emptying. Liraglutide also does not adversely affect glucagon secretion in response to low blood sugar. |
| DrugBank Indication: | Liraglutide is indicated in combination with diet and exercise to improve glycemic control in patients 10 years and older with type 2 diabetes mellitus. It is also indicated to reduce the risk of major adverse cardiovascular events in patients with type 2 diabetes mellitus as well as cardiovascular disease. |
| Targets: | GLP1R activator; GLP1R agonist; GCG receptor antagonist activity |
| Therapeutic Category: | Improve insulin resistance |
| Clinical Trial Progress: | Phase 2 completed (NCT01237119: Liraglutide was safe, well tolerated, and led to histological resolution of non-alcoholic steatohepatitis, warranting extensive, longer-term studies.) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0049 | NCT02147925 | Phase 4 | Completed | No Results Available | August 2014 | May 18, 2018 | Details |
| L0081 | NCT03068065 | Phase 4 | Completed | No Results Available | May 2014 | March 1, 2017 | Details |
| L0160 | NCT01399645 | Phase 2 | Completed | No Results Available | May 2011 | August 27, 2014 | Details |
| L0430 | EUCTR2020-000220-19-AT | Phase 4 | Authorised | No Results Available | 24/03/2020 | 7 December 2020 | Details |
| L0435 | IRCT20200128046294N1 | Phase 3 | Not Recruiting | No Results Available | 22/02/2020 | 21 June 2021 | Details |
| L0479 | EUCTR2016-002045-36-GB | Phase 2 | Not Recruiting | No Results Available | 05/02/2019 | 20 July 2020 | Details |
| L0532 | EUCTR2009-015927-94-GB | Phase 4 | Not Recruiting | Has Results | 17/03/2010 | 25 November 2019 | Details |
| L0630 | ChiCTR-TRC-14004464 | Other | Not Recruiting | No Results Available | 18/03/2014 | 18 April 2017 | Details |
| L0677 | EUCTR2009-016761-29-GB | Phase 2 | Not Recruiting | No Results Available | 16/04/2010 | 10 December 2019 | Details |
| L0849 | NCT02721888 | Phase 4 | Recruiting | No Results Available | 29/02/2016 | 11 April 2016 | Details |
| L0855 | NCT02654665 | Phase 3 | Not recruiting | No Results Available | 11/01/2016 | 12 December 2020 | Details |
| L0893 | ChiCTR-TRC-14004660 | Post-market | Not Recruiting | No Results Available | 21/09/2014 | 18 April 2017 | Details |
| L0938 | EUCTR2012-001371-37-DK | Phase 4 | Not Recruiting | No Results Available | 09/07/2012 | 10 December 2019 | Details |
| L0989 | NCT01237119 | Phase 2 | Completed | No Results Available | August 2010 | March 23, 2016 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S08 | Lifestyle measures | Lifestyle intervention; weight loss; diet adaptation; dietary interventions; lifestyle modifications; Exercise | -- | -- | Details |
| S01 | Improve insulin resistance | insulin sensitizer; insulin resistance; glucose tolerance | Biguanide: increases 5-AMP activated protein kinase signaling; SGLT-2 inhibitor; Thiazalidinedione: selective PPAR-γ agonists; GLP-1 agonist | Metformin; Empagliflozin; Canagliflozin; Rosiglitazone; Pioglitazone; Liraglutide | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00251 | 35164657 | Bioengineered | Liraglutide inhibits receptor for advanced glycation end products (RAGE)/reduced form of nicotinamide-adenine dinucleotide phosphate (NAPDH) signaling to ameliorate non-alcoholic fatty liver disease (NAFLD) in vivo and vitro. | Details |
| A00267 | 35160204 | J Clin Med | Liraglutide + PYY3-36 Combination Therapy Mimics Effects of Roux-en-Y Bypass on Early NAFLD Whilst Lacking-Behind in Metabolic Improvements. | Details |
| A00609 | 35030323 | Lancet Gastroenterol Hepatol | Efficacy of peroxisome proliferator-activated receptor agonists, glucagon-like peptide-1 receptor agonists, or sodium-glucose cotransporter-2 inhibitors for treatment of non-alcoholic fatty liver disease: a systematic review. | Details |
| A01668 | 34660809 | J Diabetes Res | Liraglutide Decreases Liver Fat Content and Serum Fibroblast Growth Factor 21 Levels in Newly Diagnosed Overweight Patients with Type 2 Diabetes and Nonalcoholic Fatty Liver Disease. | Details |
| A02287 | 34435378 | Aliment Pharmacol Ther | Systematic review with network meta-analysis: comparative efficacy of pharmacologic therapies for fibrosis improvement and resolution of NASH. | Details |
| A02349 | 34406410 | J Clin Endocrinol Metab | The Emerging Role of Glucagon-like Peptide-1 Receptor Agonists for the Management of NAFLD. | Details |
| A03013 | 34164242 | Cureus | Role of Glucagon-Like Peptide-1 Receptor Agonists in the Management of Non-Alcoholic Steatohepatitis: A Clinical Review Article. | Details |
| A03159 | 34107584 | Zhonghua Gan Zang Bing Za Zhi | [Liraglutide alleviates lipotoxic liver cell damage and promotes autophagy to improve non-alcoholic fatty liver]. | Details |
| A03282 | 34062416 | Biomed Pharmacother | The HIF-2α/PPARα pathway is essential for liraglutide-alleviated, lipid-induced hepatic steatosis. | Details |
| A03289 | 34059612 | Curr Opin Cardiol | Update on cardiovascular risk in nonalcoholic fatty liver disease. | Details |
| A03385 | 34022222 | J Biol Chem | Novel insulin sensitizer MSDC-0602K improves insulinemia and fatty liver disease in mice, alone and in combination with liraglutide. | Details |
| A03431 | 34002333 | Diabetes Ther | Effects of Liraglutide on Nonalcoholic Fatty Liver Disease in Patients with Type 2 Diabetes Mellitus: A Systematic Review and Meta-Analysis. | Details |
| A03840 | 33852508 | Eur J Gastroenterol Hepatol | The role of nursing care in the type 2 diabetes treatment associated with chronic liver diseases. | Details |
| A03843 | 33851458 | Hepatology | Hepatic Fibroblast Growth Factor 21 Is Involved in Mediating Functions of Liraglutide in Mice With Dietary Challenge. | Details |
| A03861 | 33841337 | Front Endocrinol (Lausanne) | Efficacy of Various Hypoglycemic Agents in the Treatment of Patients With Nonalcoholic Liver Disease With or Without Diabetes： A Network Meta-Analysis. | Details |
| A04016 | 33788377 | Liver Int | Elafibranor and liraglutide improve differentially liver health and metabolism in a mouse model of non-alcoholic steatohepatitis. | Details |
| A04068 | 33771699 | Pharmacol Res | Epigenetics in NAFLD/NASH: Targets and therapy. | Details |
| A04128 | 33746742 | Front Pharmacol | Liraglutide Alleviates Hepatic Steatosis and Liver Injury in T2MD Rats via a GLP-1R Dependent AMPK Pathway. | Details |
| A04163 | 33732030 | Clin Pharmacol | Clinical Impact of Liraglutide as a Treatment of Obesity. | Details |
| A04706 | 33534958 | ESC Heart Fail | Non-alcoholic fatty liver disease and heart failure with preserved ejection fraction: from pathophysiology to practical issues. | Details |