Exenatide

What it is and how it works

Mechanism of Action Incretins, such as glucagon-like peptide-1 (GLP-1), enhance glucose-dependent insulin secretion and exhibit other antihyperglycemic actions following their release into the circulation from the gut. Exenatide is a GLP-1 receptor agonist that enhances glucose-dependent insulin secretion by the pancreatic beta-cell, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying. The amino acid sequence of exenatide partially overlaps that of human GLP-1. Exenatide has been shown to bind and activate the human GLP-1 receptor in vitro .

Mechanism class: Glucagon-like Peptide-1 (GLP-1) Agonists

Indications

Exenatide injection is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Exenatide injection is a glucagon-like peptide-1 (GLP-1) receptor agonist indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. ( 1 , 14 ) Limitations of Use Co-administration with other exenatide-containing products is not recommended. Limitations of Use Exenatide injection contains exenatide. Co-administration with other exenatide-containing products is not recommended.

Dosage and administration (summary)

Inject subcutaneously within 60 minutes prior to morning and evening meals (or before the two main meals of the day, approximately 6 hours or more apart). Initiate at 5 mcg per dose twice daily; increase to 10 mcg twice daily after 1 month based on clinical response. Recommended Dosing Initiate exenatide injection at 5 mcg administered subcutaneously twice daily at any time within the 60-minute period before the morning and evening meals (or before the two main meals of the day, approximately 6 hours or more apart). Do not administer after a meal.

Contraindications

Exenatide injection is contraindicated in patients with: A prior severe hypersensitivity reaction to exenatide or to any of the excipients in exenatide injection. Serious hypersensitivity reactions including anaphylaxis and angioedema have been reported with exenatide injection . A history of drug-induced immune-mediated thrombocytopenia from exenatide products. Serious bleeding, which may be fatal, from drug-induced immune-mediated thrombocytopenia has been reported with exenatide use .

Warnings and precautions

Acute Pancreatitis : Has been observed in patients treated with GLP-1 receptor agonists, including exenatide. Discontinue if pancreatitis is suspected. Never share an exenatide injection pen between patients, even if the needle is changed. Hypoglycemia with Concomitant Use of Insulin Secretagogues or Insulin : Patients taking an insulin secretagogue or insulin may have an increased risk of hypoglycemia, including severe hypoglycemia. Reduction in the dose of insulin secretagogues or insulin may be necessary.

Pregnancy

Pregnancy Risk Summary Limited data with exenatide in pregnant women are not sufficient to determine a drug-associated risk for major birth defects or miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy (see Clinical Considerations) .

Storage and supply

How Supplied Exenatide Injection, USP is supplied as a clear, colorless sterile solution for subcutaneous injection containing 250 mcg/mL exenatide, USP. The following packages are available: 5 mcg per dose, in a single-patient-use prefilled pen containing 300 mcg/1.2 mL (250mcg/mL), 60 doses: NDC 70121-1685-1 10 mcg per dose, in a single-patient-u…

Source: Exenatide (Exenatide) — US FDA prescribing information, 2026-05-27, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.