Exenatide
Synthetic version of exendin-4, originally isolated from the saliva of the Gila monster (Heloderma suspectum). First GLP-1 receptor agonist, FDA-approved 2005 as Byetta. Weekly depot form Bydureon approved 2012.
Mechanism of action
Exenatide is a 39-amino-acid peptide with about 53% sequence homology to human GLP-1. A glycine substitution at position 2 prevents dipeptidyl-peptidase-IV cleavage and extends the half-life from native GLP-1 (minutes) to about 2.4 hours. GLP-1 receptor activation glucose-dependently stimulates insulin secretion, inhibits glucagon and delays gastric emptying.
Evidence at a glance
What the studies show
Where studies disagree
Does exenatide reduce cardiovascular events?
Pharmacokinetics
Theoretical concentration curve at a half-life of 2.4 h. Pure pharmacokinetic model — not a dosing recommendation.
Open in PK tool →Routes of administration in the literature
Amounts reported in sources
Safer use & risks
Known adverse events from studies
Interactions & combinations
Risks & hygiene aspects in the literature
Thyroid C-cell carcinoma (boxed warning)
Anecdotal observations
What online communities discuss
Legal status by country
Reconstitution calculator
Peptides ship as a dry powder. Once dissolved in a liquid (reconstitution), this calculator answers a single question: how much substance is in one millilitre of solution afterwards?
- 1Enter the vial's substance amount (printed on the label).
- 2Enter how much solvent you add.
- 3Result = concentration in mg per mL.
Cofactors
These cofactors relate to the peptide class, not to a specific use. No recommendation, no dosing.
Study register
Effect of exenatide on glycemic control over 30 weeks in patients with type 2 diabetes treated with metformin and a sulfonylurea (AMIGO)
Effects of once-weekly exenatide on cardiovascular outcomes in type 2 diabetes (EXSCEL)
Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom
Liraglutide once a day versus exenatide twice a day for type 2 diabetes: a 26-week randomised, parallel-group, multinational, open-label trial (LEAD-6)
Sources & method
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