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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 various studies indicate that liraglutide not only enhances insulin secretion and suppresses glucagon release but also promotes significant weight loss through mechanisms involving central nervous system pathways. Additionally, liraglutide has been associated with cardiovascular benefits and potential renal protection, although concerns regarding its safety in specific populations, such as those with chronic heart failure, have been raised. Current research continues to explore liraglutide's broader therapeutic applications and its effects on different patient subgroups.

Chemical Profile

Chemical Structure

Formula	C172H265N43O51
Molecular Weight	3751 g/mol
CAS Number	204656-20-2
PubChem CID	16134956

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 binding to the GLP-1 receptors (GLP-1Rs) located in pancreatic beta cells and the central nervous system, particularly in the arcuate nucleus of the hypothalamus. This binding activates the cAMP/PKA signaling pathway, leading to enhanced insulin secretion in response to hyperglycemia, suppression of glucagon release, deceleration of gastric emptying, and modulation of appetite through the activation of proopiomelanocortin (POMC) and cocaine- and amphetamine-regulated transcript (CART) neurons. While its effects on glucose metabolism are well characterized, the precise mechanisms underlying liraglutide's weight loss effects and its central nervous system actions remain incompletely understood.

Research

74 Research Publications

10,591

Total Citations

Human/RCT

13.2

Avg. Influence

2024

Latest

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01Top

#01

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

ReviewInfluence247.0

3805

Researchers observed that GLP-1 receptor agonists, including liraglutide, effectively lower HbA1c by 1-2% and promote weight loss, with mild nausea as the most common adverse event.

10 nmol/kgintraperitoneal(mouse)10 weeks100 μgsubcutaneous(human)54 weeks200 μgsubcutaneous(human)54 weeks300 μgsubcutaneous(human)54 weeks1.8 mgsubcutaneous(human)54 weeks

PubMed

02Top

#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

01Participants using liraglutide (3.0 mg) lost an average of 6.0% of their body weight, compared to 2.0% with placebo.
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.
03Gastrointestinal issues were more common in those taking liraglutide, but no cases of pancreatitis were reported.

PubMed

03Top

#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

832

Researchers observed that liraglutide induces weight loss in rats through mechanisms involving GLP-1 receptors in the arcuate nucleus, impacting POMC and CART neurons.

Key findings

01Liraglutide does not activate GLP-1-producing neurons in the hindbrain.
02The drug binds to neurons in the arcuate nucleus and is essential for weight loss effects.
03Liraglutide stimulates specific neurons that promote weight loss while inhibiting others that encourage appetite.

10 nmol/kgintraperitoneal(mouse)10 weeks100 μgsubcutaneous(human)54 weeks200 μgsubcutaneous(human)54 weeks300 μgsubcutaneous(human)54 weeks1.8 mgsubcutaneous(human)54 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.

HumanInfluence29.0

504

Researchers observed that liraglutide did not significantly improve left ventricular function in patients with chronic heart failure compared to placebo, but was associated with increased heart rate and serious cardiac events.

10 nmol/kgintraperitoneal(mouse)10 weeks100 μgsubcutaneous(human)54 weeks200 μgsubcutaneous(human)54 weeks300 μgsubcutaneous(human)54 weeks1.8 mgsubcutaneous(human)54 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

271

The study demonstrated that cotadutide significantly improved glycemic control and weight loss in adults with obesity and type 2 diabetes compared to liraglutide.

10 nmol/kgintraperitoneal(mouse)10 weeks100 μgsubcutaneous(human)54 weeks200 μgsubcutaneous(human)54 weeks300 μgsubcutaneous(human)54 weeks1.8 mgsubcutaneous(human)54 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

01GLP-1 reduces food intake primarily by acting on specific brain receptors.
02The study identified various brain regions involved in GLP-1's effects, including the hypothalamus and reward circuitry.
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

229

Researchers observed that Cotadutide, a dual GLP-1R/GcgR agonist, significantly reduces hepatic fibrosis and lipid content more effectively than liraglutide in preclinical models of NASH.

10 nmol/kgintraperitoneal(mouse)10 weeks100 μgsubcutaneous(human)54 weeks200 μgsubcutaneous(human)54 weeks300 μgsubcutaneous(human)54 weeks1.8 mgsubcutaneous(human)54 weeks

PubMed

Safety

Safety & Handling

Research Gaps

The mechanisms by which liraglutide induces weight loss, particularly its direct actions in the brain, remain unclear, and further studies are needed to elucidate these pathways. Additionally, while liraglutide has been associated with serious cardiac events in chronic heart failure patients, more comprehensive data on its long-term safety and efficacy in various heart failure subgroups are lacking.

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

🇩🇪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

Publications per Year

48 total

Mechanism

Tools

Reconstitution Calculator

Calculate reconstitution volumes for Liraglutide

Serum Level Visualizer

Visualize Liraglutide serum levels over time

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