Liraglutide (revision 1)
Old revision·09:00, 12 Aug 2024·Peptide_Pete
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| Liraglutide | |
|---|---|
| INN | liraglutide |
| Class | GLP-1 receptor agonist |
| Route | Subcutaneous, daily |
| First approval | 2009 (type 2 diabetes) |
| Compound infobox · conventions | |
Liraglutide is an acylated analogue of Glucagon-like peptide-1 and was the first GLP-1 receptor agonist to use albumin binding for half-life extension. A C-16 palmitic acid is attached to Lys26 through a γ-glutamate spacer, and Lys34 is substituted with arginine so that acylation occurs at a single site.[1]
The resulting half-life of about thirteen hours supports once-daily subcutaneous dosing. Liraglutide was approved for type 2 diabetes in 2009 and, at a higher dose, for weight management in 2014; the LEADER trial subsequently established cardiovascular benefit in type 2 diabetes with high cardiovascular risk.[2]
References
- ^ Knudsen LB, Lau J. "The discovery and development of liraglutide and semaglutide." Frontiers in Endocrinology 10:155 (2019). PMID 31031702.
- ^ Marso SP, Daniels GH, Brown-Frandsen K, et al. "Liraglutide and cardiovascular outcomes in type 2 diabetes." New England Journal of Medicine 375(4):311–322 (2016). DOI:10.1056/NEJMoa1603827. PMID 27295427.
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