Lixisenatide (revision 2)
Old revision·16:53, 11 Oct 2024·HOMA_Hettie
| Lixisenatide | |
|---|---|
| Class | GLP-1 receptor agonist |
| Origin | Exendin-4 derivative |
| Route | Subcutaneous, once daily |
| Outcome trial | ELIXA; neutral |
| Compound infobox · conventions | |
Lixisenatide is a GLP-1 receptor agonist derived from exendin-4, the same scaffold as exenatide, with a modified C-terminus. It is short-acting and given once daily.[1]
Its pharmacological profile emphasises postprandial glycaemic control through pronounced delay of gastric emptying, an effect that does not attenuate as it does with continuously present long-acting agonists.[2]
Pharmacology
[edit]Like exenatide, lixisenatide carries glycine at position 2 of the exendin scaffold and is therefore not a substrate for DPP-4. Its half-life of about three hours nonetheless requires daily dosing, since renal clearance dominates once proteolysis is removed.[2]
The short exposure profile produces a large gastric-emptying effect at each dose, and it is this rather than a large fasting-glucose effect that drives its glycaemic action. Its effect on glycated haemoglobin is modest by current standards.[1]
References
- ^ a b Pfeffer MA, Claggett B, Diaz R, et al. "Lixisenatide in patients with type 2 diabetes and acute coronary syndrome." New England Journal of Medicine 373(23):2247–2257 (2015). PMID 26630143.
- ^ a b Drucker DJ. "Mechanisms of action and therapeutic application of glucagon-like peptide-1." Cell Metabolism 27(4):740–756 (2018). PMID 29617641.