Lixisenatide

Category: peptide

Aliases: Adlyxin, Lyxumia, AVE0010

Pharmacological Mechanism

Exenatide backbone with a 6-lysine C-terminal extension (and Pro replacement at position 38). Short plasma t½ (~3 h) produces predominantly prandial GLP-1R exposure → strong postprandial glycaemic effect mostly through slowed gastric emptying. Less sustained basal effect than weekly GLP-1 agonists; ELIXA trial was CV-neutral.

Half-Life (t½)

SC: 3h

Dosing Guidelines

• SC: Typical 10 mcg (Range: 10–10 mcg)

Target Organ Systems

• endocrine
• digestive

Pathways It Modulates

• Insulin signaling + glucose homeostasis (activator) — GLP-1R (short-acting)

Chemical Identifiers

• PubChem CID: 90472060
• Formula: C215H347N61O65S
• Molecular weight: 4858 g/mol
• InChIKey: XVVOERDUTLJJHN-IAEQDCLQSA-N
• SMILES: CC[C@H](C)[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N)C(=O)NCC(=O)NCC(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N4CCC[C@H]4C(=O)N5CCC[C@H]5C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC7=CC=CC=C7)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CC8=CNC=N8)N

References

• PMID 28133970