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Liraglutide

Victoza · Saxenda

Metabolic & WeightApproved
MW
3751g/mol
Formula
C172H265N43O51

Liraglutide is a glucagon-like peptide-1 (GLP-1) analog derived from the natural hormone GLP-1, primarily studied for its effects on glycemic control and weight management in individuals with type 2 diabetes. Researchers observed that liraglutide not only lowers blood glucose levels but also induces significant weight loss, with mechanisms involving the central nervous system, particularly the arcuate nucleus of the hypothalamus. Key findings from clinical studies indicate that liraglutide can lead to reductions in glycated hemoglobin (HbA1c) and body weight, with some reports highlighting its association with psychiatric adverse events, including depression and anxiety. Current research continues to explore liraglutide's broader applications, including its potential roles in obesity management and other metabolic disorders, while also investigating the safety profile of GLP-1 receptor agonists.

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 glucagon-like peptide-1 (GLP-1) receptor agonist, primarily binding to GLP-1 receptors (GLP-1Rs) in the brain, particularly in the arcuate nucleus (ARC), where it stimulates proopiomelanocortin (POMC) and cocaine- and amphetamine-regulated transcript (CART) neurons while inhibiting neuropeptide Y (NPY) and agouti-related peptide (AgRP) neurons through GABA-dependent signaling. This activation leads to enhanced insulin secretion, suppression of glucagon release, delayed gastric emptying, and reduced appetite, contributing to weight loss and improved glycemic control. The precise mechanisms underlying liraglutide's effects on weight loss and its central nervous system actions remain incompletely understood.

Research

136 Research Publications

14,383

Total Citations

47

Human/RCT

10.1

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.

ReviewInfluence246.0
3840
Researchers observed that GLP-1 receptor agonists, including liraglutide, significantly reduce HbA1c levels and body weight while showing a favorable safety profile compared to DPP-4 inhibitors.
10 nmol/kgintraperitoneal(mouse)10 weeks0.026 mg/kgsubcutaneous(rat)not mentioned0.056 mg/kgsubcutaneous(rat)not mentioned0.078 mg/kgsubcutaneous(rat)not mentioned
PubMed
#02

GLP-1 receptor agonists in the treatment of type 2 diabetes - state-of-the-art.

ReviewInfluence71.0
1406
The study demonstrated that GLP-1 receptor agonists, including liraglutide, effectively lower HbA1c levels and promote weight loss, making them a preferred first injectable therapy for type 2 diabetes.
1.7 mgsubcutaneously(human)72 weeks2.4 mgsubcutaneously(human)72 weeks5 mgsubcutaneously(human)40 weeks10 mgsubcutaneously(human)40 weeks15 mgsubcutaneously(human)40 weeks1 mgsubcutaneously(human)40 weeks2.4 mgsubcutaneously(human)68 weeks0.5 mgsubcutaneous(human)30 weeks1.0 mgsubcutaneous(human)30 weeks14 mgoral(human)not mentioned
PubMed
#03

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
#04

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

ReviewInfluence23.0
900
The systematic review provided evidence that GLP-1 receptor agonists lead to significant weight loss in overweight or obese patients, regardless of diabetes status.
10 nmol/kgintraperitoneal(mouse)10 weeks
PubMed
#05

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

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

AnimalInfluence54.0
857
Researchers observed that liraglutide's weight loss effects in rats are mediated by GLP-1 receptors in the arcuate nucleus, influencing specific neuronal pathways related to appetite regulation.

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 weeks0.026 mg/kgsubcutaneous(rat)not mentioned0.056 mg/kgsubcutaneous(rat)not mentioned0.078 mg/kgsubcutaneous(rat)not mentioned
PubMed
#06

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.

HumanInfluence31.0
520
The study demonstrated that liraglutide did not affect left ventricular systolic function in chronic heart failure patients, while it was associated with increased heart rate and more serious cardiac adverse events.
10 nmol/kgintraperitoneal(mouse)10 weeks100 μgsubcutaneous(human)54 weeks200 μgsubcutaneous(human)54 weeks300 μgsubcutaneous(human)54 weeks
PubMed
#07

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
#08

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
#09

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.

HumanInfluence20.0
277
The study demonstrated that cotadutide significantly improves glycemic control and weight loss in adults with overweight or obesity and type 2 diabetes over 54 weeks.
10 nmol/kgintraperitoneal(mouse)10 weeks0.026 mg/kgsubcutaneous(rat)not mentioned0.056 mg/kgsubcutaneous(rat)not mentioned0.078 mg/kgsubcutaneous(rat)not mentioned
PubMed
#10

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
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 studies assessing the sustained effects of liraglutide on psychiatric outcomes and its overall safety profile in diverse populations beyond the initial clinical trial settings.

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

49 total
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Mechanism

Tools

Reconstitution Calculator

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Serum Level Visualizer

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Mechanism

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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