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Exenatide (revision 3)

Old revision·10:48, 6 Oct 2024·LiraLotte

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Exenatide
INNexenatide
ClassGLP-1 receptor agonist
OriginSynthetic exendin-4
First approval2005
Compound infobox · conventions

Exenatide is a synthetic version of exendin-4, a 39-residue peptide isolated from the venom of the Gila monster, Heloderma suspectum. It shares approximately 53% sequence identity with human Glucagon-like peptide-1 and is a full agonist at the GLP-1 receptor. Approved in 2005, it was the first GLP-1 receptor agonist to reach the market.[1]

Its therapeutic relevance rests on an accident of sequence: exendin-4 carries glycine rather than alanine at position 2, so DPP-4 does not cleave it. No engineering was required to obtain protease resistance — the peptide is naturally resistant, and this is why a venom peptide became a diabetes drug.[1]

References

  1. ^ a b Nielsen LL, Young AA, Parkes DG. "Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of type 2 diabetes." Regulatory Peptides 117(2):77–88 (2004). PMID 14700743.