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Liraglutide

Category: Peptides · Last updated

Liraglutide is a 31-amino-acid GLP-1 receptor agonist marketed as Victoza (type 2 diabetes, FDA-approved 2010) and Saxenda (chronic weight management, FDA-approved 2014) by Novo Nordisk. It is the predecessor of the current once-weekly GLP-1 agonist Semaglutide and a forerunner of the dual-incretin agonist Tirzepatide.

All human-clinical results summarized below are the property of the publishing investigators and Novo Nordisk. They are reproduced as references, not as claims of this product.

Overview

Liraglutide is engineered from native GLP-1 by a single amino-acid substitution (Lys26 to Arg) and a γ-glutamic-acid spacer plus C16 palmitoyl fatty-acid linker at Lys26. The linker drives albumin binding, dramatically slowing renal and proteolytic clearance.

The molecule was the second GLP-1 receptor agonist to reach market (after exenatide) and the first amenable to once-daily dosing. Victoza launched 2010 for type 2 diabetes glycemic control; Saxenda followed 2014 at a higher dose (3.0 mg) for chronic weight management.

Mechanism

GLP-1 receptor agonism drives a coordinated set of glucoregulatory + appetite effects:

  • Glucose-dependent insulin secretion. Pancreatic β-cell GLP-1R activation increases insulin release only when plasma glucose is elevated, minimizing hypoglycemia risk.
  • Glucagon suppression. α-cell GLP-1R signaling suppresses inappropriate postprandial glucagon.
  • Delayed gastric emptying. Vagal-mediated slowing of gastric transit blunts postprandial glucose excursions.
  • Central appetite suppression. Brainstem + hypothalamic GLP-1 receptors (arcuate nucleus POMC/CART neurons) reduce caloric intake.

See: GLP-1_receptor.

Evidence

The pivotal trial programs for liraglutide:

  • LEAD program. Six Phase 3 trials (LEAD-1 through LEAD-6) established efficacy and safety in type 2 diabetes. Buse JB, et al. Lancet. 2009;374(9683):39-47. (LEAD-6 vs exenatide.)
  • SCALE program. Four Phase 3 trials at the 3.0 mg dose established efficacy in obesity. Pi-Sunyer X, Astrup A, Fujioka K, et al. "A Randomized, Controlled Trial of 3.0 mg of Liraglutide in Weight Management." N Engl J Med. 2015;373(1):11-22. PMID 26132939.
  • LEADER cardiovascular outcomes trial. Marso SP, et al. "Liraglutide and Cardiovascular Outcomes in Type 2 Diabetes." N Engl J Med. 2016;375(4):311-22. PMID 27295427. Established cardiovascular benefit (MACE reduction) in T2D with elevated CV risk.

Pharmacokinetics

Liraglutide carries a C16 palmitoyl linker that binds plasma albumin, extending half-life from native GLP-1's ~2 minutes to approximately 13 hours, sufficient for once-daily subcutaneous administration. Tmax occurs 8 to 12 hours post-injection. Steady-state plasma concentration is reached after 3 days of repeated daily dosing.

Dosing literature

Per the Victoza label, T2D dosing is titrated weekly from 0.6 mg to 1.2 mg to 1.8 mg subcutaneous daily. Per the Saxenda label, obesity dosing titrates weekly from 0.6 mg up to 3.0 mg daily. This wiki does not recommend any human dose. The compound, when supplied as research-grade reference material, is for laboratory in-vitro use only.

Storage

Lyophilized: 2 to 8 °C, stable per manufacturer label. Reconstituted prefilled pen: 2 to 8 °C until first use, then 30 days at room temperature per Novo Nordisk label. Lab-supplied research-grade vials follow general peptide storage practice: refrigerate lyophilized cake; reconstitute in Bacteriostatic_water for short-term in-vitro use.

Regulatory status

  • United States. FDA-approved as Victoza (T2D, 2010) and Saxenda (chronic weight management, 2014). Generic liraglutide approved 2024.
  • European Union. EMA-approved (same brand names).
  • WADA. Not currently on the WADA Prohibited List as of the 2026 publication.

Side effects (per FDA label)

  • Gastrointestinal. Nausea, vomiting, diarrhea, constipation. Most common at initiation; usually decline with continued use.
  • Pancreatitis. Rare; class-based caution. Discontinue if confirmed.
  • Thyroid C-cell tumors. Class-based boxed warning based on rodent C-cell tumor signal. Contraindicated in personal/family history of medullary thyroid carcinoma or MEN-2.
  • Gallbladder disease. Increased cholelithiasis risk in obesity trials.
  • Hypoglycemia. Rare unless combined with sulfonylureas or insulin.

See also

References

  • Buse JB, Rosenstock J, Sesti G, et al. "Liraglutide once a day versus exenatide twice a day for type 2 diabetes (LEAD-6)." Lancet. 2009;374(9683):39-47.
  • Pi-Sunyer X, Astrup A, Fujioka K, et al. "A Randomized, Controlled Trial of 3.0 mg of Liraglutide in Weight Management." N Engl J Med. 2015;373(1):11-22. [PMID 26132939](https://pubmed.ncbi.nlm.nih.gov/26132939/).
  • Marso SP, Daniels GH, Brown-Frandsen K, et al. "Liraglutide and Cardiovascular Outcomes in Type 2 Diabetes." N Engl J Med. 2016;375(4):311-22. [PMID 27295427](https://pubmed.ncbi.nlm.nih.gov/27295427/).
Research framing only. Peppu Wiki documents the published research literature surrounding peptide compounds. Articles describe in-vitro and animal-model evidence, regulatory status, and community-reported protocols. Nothing on this site is medical advice, a recommendation for human use, or a substitute for consultation with a qualified clinician. All compounds discussed are research-use only. Citations should be verified at the source before relying on any quantitative claim.
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