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Liraglutide

Victoza · Saxenda

Metabolic & WeightApproved
MW
3751g/mol
Formula
C172H265N43O51

Liraglutide is a synthetic analog of glucagon-like peptide-1 (GLP-1), classified as a GLP-1 receptor agonist, originally developed for the management of type 2 diabetes. Researchers primarily study liraglutide for its effects on glycemic control and weight reduction in individuals with obesity and diabetes. Key findings from numerous studies indicate that liraglutide enhances insulin secretion, suppresses glucagon release, and promotes weight loss through mechanisms involving central nervous system pathways, particularly in the arcuate nucleus of the hypothalamus. Additionally, liraglutide has been associated with cardiovascular benefits and renal protection, suggesting its potential utility beyond glycemic management. Current research is exploring its efficacy in various populations and conditions, including its role in neurodegenerative diseases and other metabolic disorders.

Chemical Profile

Chemical Profile

Chemical structure
Chemical Structure
FormulaC172H265N43O51
Molecular Weight3751 g/mol
CAS Number204656-20-2
PubChem CID16134956

Half-Life

SCSubcutaneous

~13 hours

INIntranasal

Not applicable

POOral

Poor bioavailability

The extended half-life allows for once-daily dosing in clinical use.

Mechanism

Mechanism of Action

Liraglutide acts as a GLP-1 receptor agonist, primarily activating GLP-1 receptors (GLP-1Rs) in pancreatic β-cells, which enhances insulin secretion and suppresses glucagon release through the cAMP/PKA signaling pathway. Additionally, liraglutide influences appetite regulation by stimulating proopiomelanocortin (POMC) and cocaine- and amphetamine-regulated transcript (CART) neurons in the arcuate nucleus, while inhibiting neuropeptide Y (NPY) and agouti-related peptide (AgRP) neurons via GABAergic signaling. Although the precise mechanisms underlying its effects on weight loss are not fully understood, liraglutide's actions on these neural pathways are crucial for its therapeutic benefits.

Research

70 Research Publications

10,475

Total Citations

26

Human/RCT

13.8

Avg. Influence

2024

Latest

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#01

The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes.

ReviewInfluence247.0
3792
Researchers observed that GLP-1 receptor agonists, including liraglutide, effectively lower HbA1c and promote weight loss, with mild nausea being the most common adverse event.
10 nmol/kgintraperitoneal(mouse)10 weeks
PubMed
#02

Efficacy of Liraglutide for Weight Loss Among Patients With Type 2 Diabetes: The SCALE Diabetes Randomized Clinical Trial.

Davies Melanie J, et al. · JAMA · 2015

HumanInfluence44.0
998
Researchers found that the weight-loss drug liraglutide was effective for adults with type 2 diabetes who are overweight or obese. Over 56 weeks, participants using liraglutide lost significantly more weight compared to those receiving a placebo. The study highlights liraglutide's potential as a weight-management option in this population.

Key findings

  1. 01Participants using liraglutide (3.0 mg) lost an average of 6.0% of their body weight, compared to 2.0% with placebo.
  2. 02More than half (54.3%) of those on liraglutide (3.0 mg) lost at least 5% of their body weight, compared to only 21.4% with placebo.
  3. 03Gastrointestinal issues were more common in those taking liraglutide, but no cases of pancreatitis were reported.
PubMed
#03

Effects of glucagon-like peptide-1 receptor agonists on weight loss: systematic review and meta-analyses of randomised controlled trials.

ReviewInfluence22.0
880
The study demonstrated that GLP-1 receptor agonists, including liraglutide, lead to significant weight loss in overweight or obese patients with or without type 2 diabetes.
10 nmol/kgintraperitoneal(mouse)10 weeks
PubMed
#04

The arcuate nucleus mediates GLP-1 receptor agonist liraglutide-dependent weight loss.

Secher Anna, et al. · The Journal of clinical investigation · 2014

AnimalInfluence53.0
809
Researchers observed that liraglutide induces weight loss in rats through mechanisms involving the arcuate nucleus and GLP-1 receptor activation in specific hypothalamic neurons.

Key findings

  1. 01Liraglutide does not activate GLP-1-producing neurons in the hindbrain.
  2. 02The drug binds to neurons in the arcuate nucleus and is essential for weight loss effects.
  3. 03Liraglutide stimulates specific neurons that promote weight loss while inhibiting others that encourage appetite.
10 nmol/kgintraperitoneal(mouse)10 weeks
PubMed
#05

Effect of liraglutide, a glucagon-like peptide-1 analogue, on left ventricular function in stable chronic heart failure patients with and without diabetes (LIVE)-a multicentre, double-blind, randomised, placebo-controlled trial.

HumanInfluence28.0
491
Researchers observed that liraglutide did not significantly improve left ventricular function in chronic heart failure patients compared to placebo, although it was associated with increased heart rate and serious cardiac events.
10 nmol/kgintraperitoneal(mouse)10 weeks
PubMed
#06

Efficacy and safety of glucagon-like peptide-1 receptor agonists in type 2 diabetes: A systematic review and mixed-treatment comparison analysis.

ReviewInfluence21.0
381
Researchers observed that all GLP-1 receptor agonists, including liraglutide, improve glycemic control and reduce body weight without increasing hypoglycemia risk compared to placebo.
10 nmol/kgintraperitoneal(mouse)10 weeks
PubMed
#07

Occurrence of nausea, vomiting and diarrhoea reported as adverse events in clinical trials studying glucagon-like peptide-1 receptor agonists: A systematic analysis of published clinical trials.

ReviewInfluence9.0
302
Researchers observed that the risk of gastrointestinal adverse events with GLP-1 receptor agonists was dose-dependent and varied among different compounds, with long-acting agents showing less nausea and vomiting.
10 nmol/kgintraperitoneal(mouse)10 weeks
PubMed
#08

Effects of Cotadutide on Metabolic and Hepatic Parameters in Adults With Overweight or Obesity and Type 2 Diabetes: A 54-Week Randomized Phase 2b Study.

HumanInfluence19.0
265
The study demonstrated that cotadutide significantly improved glycemic control and weight loss in adults with overweight or obesity and type 2 diabetes, outperforming liraglutide in hepatic parameter improvements.
10 nmol/kgintraperitoneal(mouse)10 weeks
PubMed
#09

GLP-1 and weight loss: unraveling the diverse neural circuitry.

Kanoski Scott E, et al. · American journal of physiology. Regulatory, integrative and comparative physiology · 2016

ReviewInfluence13.0
261
Researchers found that glucagon-like peptide-1 (GLP-1) and its long-acting versions can significantly reduce food intake and body weight. They explored the complex neural pathways in the brain that GLP-1 influences, which could lead to new obesity treatments with fewer side effects.

Key findings

  1. 01GLP-1 reduces food intake primarily by acting on specific brain receptors.
  2. 02The study identified various brain regions involved in GLP-1's effects, including the hypothalamus and reward circuitry.
  3. 03Certain neural pathways activated by GLP-1 can decrease appetite without causing nausea, suggesting potential for safer obesity therapies.
PubMed
#10

Resolution of NASH and hepatic fibrosis by the GLP-1R/GcgR dual-agonist Cotadutide via modulating mitochondrial function and lipogenesis.

AnimalInfluence12.0
223
Researchers observed that cotadutide significantly alleviates hepatic fibrosis and improves mitochondrial function in preclinical models of non-alcoholic steatohepatitis compared to liraglutide.
10 nmol/kgintraperitoneal(mouse)10 weeks
PubMed
Safety

Safety & Handling

Research Gaps

The precise mechanisms by which liraglutide induces weight loss in humans remain unclear, particularly regarding its direct actions in the brain and the specific pathways involved. Additionally, there is a lack of long-term human trials assessing the sustained effects of liraglutide on weight loss and metabolic health, as well as its potential impacts on neurodegenerative diseases and other novel indications outside of type 2 diabetes.

Solubility

Liraglutide is soluble in water and exhibits limited solubility in organic solvents like acetonitrile and DMSO.

Storage & Handling

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 30 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

Legal Status

🇩🇪DE

Approved as a medicinal product for diabetes and obesity. Not a controlled substance.

🇺🇸US

FDA approved for type 2 diabetes and chronic weight management. Not a controlled substance.

🇦🇺AU

Approved by TGA for type 2 diabetes and obesity management.

🇬🇧UK

Approved by MHRA for type 2 diabetes and weight management.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

Community Insights

Community Insights

Publications per Year

48 total
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14
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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer