Exenatide

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. BYETTA 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.

• BYETTA is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use • BYETTA contains exenatide.ICD-10: E11.9

• BYETTA is contraindicated in patients with: • A prior severe hypersensitivity reaction to exenatide or to any of the excipients in BYETTA. Serious hypersensitivity reactions including anaphylaxis and angioedema have been reported with BYETTA [see Warnings and Precautions (5.7) ].contraindicated

• 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). ( 2.1 ) • Initiate at 5 mcg per dose twice daily; increase to 10 mcg twice daily after 1 month based on clinical response. ( 2.1 ) 2.1 Recommended Dosing • Initiate BYETTA 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. • Based on clinical response, the dose of BYETTA can be increased to 10 mcg twice daily which is recommended after 1 month of therapy, in order to reduce the risk of gastrointestinal adverse reactions [see Warnings and Precautions (5.5) and Adverse Reactions (6.1) ] . • Administer as a subcutaneous injection in the thigh, abdomen, or upper arm. • Rotate injections sites with each dose. Do not use the same site for each injection. • Inspect visually for particulate matter and discoloration. Only use BYETTA if the solution appears clear, colorless, and contains no particles. • When using BYETTA with insulin, administer as separate injections and never mix. It is acceptable to inject BYETTA and insulin in the same body region, but the injections should not be adjacent to each other. • If a dose is missed, resume the treatment regimen as prescribed with the next scheduled dose.

• Acute Pancreatitis : Has been observed in patients treated with GLP-1 receptor agonists, including BYETTA. Discontinue if pancreatitis is suspected. ( 5.1 ) • Never share a BYETTA pen between patients, even if the needle is changed. ( 5.2 ) • 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. ( 5.3 ) • Acute Kidney Injury Due to Volume Depletion : Monitor renal function in patients reporting adverse reactions that could lead to volume depletion ( 5.4 ) • Severe Gastrointestinal Adverse Reactions : Use has been associated with gastrointestinal adverse reactions, sometimes severe. BYETTA is not recommended in patients with severe gastroparesis. ( 5.5 ) • Immunogenicity: Patients may develop antibodies to exenatide. If there is worsening glycemic control or failure to achieve target glycemic control, consider alternative antidiabetic therapy. ( 5.6 ) • Hypersensitivity: Serious hypersensitivity reactions (e.g., anaphylaxis and angioedema) have been reported. Discontinue BYETTA and promptly seek medical advice. ( 5.7 ) • Drug-induced Immune-mediated Thrombocytopenia: Serious bleeding which may be fatal has been reported. Discontinue BYETTA promptly and avoid re-exposure to exenatide. ( 5.8 ) • Acute Gallbladder Disease: If cholelithiasis or cholecystitis are suspected, gallbladder studies are indicated.

The following serious adverse reactions are described below or elsewhere in the prescribing information: • Acute Pancreatitis [see Warnings and Precautions (5.1) ] • Never Share a BYETTA Pen Between Patients [see Warnings and Precautions (5.2) ] • Hypoglycemia with Concomitant Use of Insulin Secretagogues or Insulin [see Warnings and Precautions (5.3) ] • Acute Kidney Injury Due to Volume Depletion [see Warnings and Precautions (5.4) ] • Severe Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.5) ] • Immunogenicity [see Warnings and Precautions (5.6) ] • Hypersensitivity [see Warnings and Precautions (5.7) ] • Drug-Induced Thrombocytopenia [see Warnings and Precautions (5.8) ] • Acute Gallbladder Disease [see Warnings and Precautions (5.9) ] • Pulmonary Aspiration During General Anesthesia or Deep Sedation [see Warnings and Precautions (5.10) ] • Most common (≥5%) and occurring more frequently than placebo in clinical trials: nausea, hypoglycemia, vomiting, diarrhea, feeling jittery, dizziness, headache, dyspepsia, constipation, asthenia. Nausea usually decreases over time. ( 5.3 , 6 ) To report SUSPECTED ADVERSE REACTIONS, contact AstraZeneca at 1-800-236-9933 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

• Pregnancy: Use during pregnancy only if the potential benefit justifies the risk to the fetus. (8.1) 8.1 Pregnancy Risk Summary Limited data with BYETTA 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 ). Based on animal reproduction studies, there may be risks to the fetus from exposure to BYETTA during pregnancy. BYETTA should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal reproduction studies identified increased adverse fetal and neonatal outcomes from exposure to exenatide during pregnancy and lactation in association with maternal effects. In mice, exenatide administered during gestation and lactation caused increased neonatal deaths at systemic exposure 3-times the human exposure resulting from the maximum recommended human dose (MRHD) of 20 mcg/day for BYETTA (see Data ) . The estimated background risk of major birth defects is 6-10% in women with pre-gestational diabetes with an HbA1c >7 and has been reported to be as high as 20-25% in women with HbA1c >10. The estimated background risk of miscarriage for the indicated population is unknown. In the U.S.

Metabolism

Absorption Following SC administration to patients with type 2 diabetes, exenatide reaches median peak plasma concentrations in 2.1 hours. The mean peak exenatide concentration (C max ) was 211 pg/mL and overall mean area under the time-concentration curve (AUC 0-inf ) was 1036 pg∙h/mL following SC administration of a 10-mcg dose of BYETTA.

In a clinical study of BYETTA, three patients with type 2 diabetes each experienced a single overdose of 100 mcg SC (10 times the maximum recommended dose). Effects of the overdoses included severe nausea, severe vomiting, and rapidly declining blood glucose concentrations. One of the three patients experienced severe hypoglycemia requiring parenteral glucose administration. The three patients recovered without complication. In the event of overdose, consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations. Initiate appropriate supportive treatment according to the patient's clinical signs and symptoms.

• Apr 28, 2005NDANDA021773Astrazeneca Ab
• Nov 19, 2024ANDAANDA206697Amneal

1. 1Blood Glucose Increased15,47230%
2. 2Weight Decreased12,12723%
3. 3Nausea12,04123%
4. 4Decreased Appetite5,64311%
5. 5Blood Glucose Decreased5,51711%
6. 6Vomiting4,3458.3%
7. 7Diarrhoea2,7425.2%
8. 8Dizziness2,6735.1%
9. 9Drug Ineffective2,2494.3%
10. 10Headache2,0864.0%
11. 11Injection Site Pain2,0233.9%
12. 12Pancreatitis2,0123.8%
13. 13Injection Site Bruising1,8433.5%
14. 14Injection Site Haemorrhage1,8093.5%
15. 15Fatigue1,7603.4%

Recent PubMed references pinned to Exenatide as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Hemodynamic and metabolomic responses to infusion of GLP-1 agonist exenatide in pulmonary arterial hypertension.
  JCI insight · 2026 · Samaranayake CB, Niglas M, Baxan N, et al.
  PMID 42171611DOI 10.1172/jci.insight.202660
• The glucagon-like peptide-1 receptor agonist, Ex4, reduces intromission in sexually experienced male mice.
  Psychoneuroendocrinology · 2026 · Shevchouk O, Edvardsson CE, Ericson M, et al.
  PMID 42166808DOI 10.1016/j.psyneuen.2026.107893
• The novel GLP-1/GIP dual receptor agonist DA5-CH is superior to tirzepatide and exendin-4 in the 6-OHDA Parkinson rat model.
  Frontiers in endocrinology · 2026 · Lingyu Z, Peng F, Wanting Z, et al.
  PMID 42165019DOI 10.3389/fendo.2026.1825379
• Serial assessment of NT-proBNP and high-sensitivity cardiac troponin with glucagon-like peptide-1 receptor agonist therapy in type 2 diabetes: Insights from EXSCEL.
  American heart journal · 2026 · Kittipibul V, Nguyen M, Welsh P, et al.
  PMID 42102896DOI 10.1016/j.ahj.2026.107475
• Study on chitosan/carrageenan core-shell nanoparticles for oral co-administration of insulin/exenatide enhance insulin secretion in type 2 diabetes.
  International journal of biological macromolecules · 2026 · Nguyen TV, Cao-Luu NH, Nguyen TB, et al.
  PMID 41865922DOI 10.1016/j.ijbiomac.2026.151537
• Exenatide attenuates neuroinflammation and rescues sepsis-induced depressive behavior and cognitive dysfunction in a mouse model.
  Neuroscience · 2026 · Liu S, Chen Q, Liu H, et al.
  PMID 41747818DOI 10.1016/j.neuroscience.2026.02.033
• Exenatide through PPARδ improved hepatic insulin resistance in patients of type 2 diabetes mellitus via suppressing pyroptosis.
  International immunopharmacology · 2026 · Li X, Zhou T, Wu Y, et al.
  PMID 41723896DOI 10.1016/j.intimp.2026.116416
• Exendin-4 alleviates Aβ1-40-induced apoptosis and calcium dysregulation in RPE cells through the CHP1/NHE1 complex.
  Biochemical pharmacology · 2026 · Shu Q, Lin Y, Su W, et al.
  PMID 41679663DOI 10.1016/j.bcp.2026.117789

The 10 most recently updated of 376 ClinicalTrials.gov registrations naming Exenatide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• GLP-1 Analogue in Preventing Progression of Small Vessel Disease (GAPP-SVD)
  Recruiting · Phase 2 · Interventional · 110 enrolled · Chinese University of Hong Kong
  NCT05356104updated 2026-06-05
• A Pan-European Post-Authorisation Safety Study: Risk of Pancreatic Cancer Among Type 2 Diabetes Patients Who Initiated Exenatide as Compared With Those Who Initiated Other Non-Glucagon-Like Peptide 1 Receptor Agonists Based Glucose Lowering Drugs
  Recruiting · Observational · 24,000 enrolled · AstraZeneca
  NCT05663515updated 2026-06-02
• Efficacy and Safety of Exenatide in the Treatment of Hypothalamic Obesity After Craniopharyngioma Therapy
  Completed · Phase 3 · Interventional · 42 enrolled · University Hospital, Bordeaux
  NCT02860923updated 2026-05-22
• Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study
  Active not recruiting · Observational · 781,430 enrolled · Brigham and Women's Hospital
  NCT05220917updated 2026-05-15
• Effect of GLP-1 Receptor (GLP-1R) Agonists on Cardiac Function and on Epicardial Adipose Tissue (EAT) Volume and on Myocardial TG Content in Obese Diabetics
  Completed · Phase 3 · Interventional · 44 enrolled · Assistance Publique Hopitaux De Marseille
  NCT02042664updated 2026-05-07
• Exenatide Once Weekly Over 2 Years as a Potential Disease Modifying Treatment for Parkinson's Disease
  Completed · Phase 3 · Interventional · 194 enrolled · University College, London
  NCT04232969updated 2026-05-06
• Targeting Agonists of Glucagon-like Peptide-1 Receptor for Multiple Sclerosis
  Recruiting · Phase 2 · Interventional · 120 enrolled · Johns Hopkins University
  NCT07497399updated 2026-05-05
• Exenatide Pharmacokinetics and Pharmacodynamics in Gestational Diabetes
  Recruiting · Phase 4 · Interventional · 13 enrolled · Maisa N. Feghali, MD
  NCT05482789updated 2026-04-20
• Islet Transplantation in Type 1 Diabetic Patients Using the University of Illinois at Chicago (UIC) Protocol
  Active not recruiting · Phase 3 · Interventional · 21 enrolled · CellTrans Inc.
  NCT00679042updated 2026-04-06
• A Single-Center, Open-Label, Single Ascending Dose Study of Exenatide Circular RNA-Lipid Nanoparticle Injection (CR059) in Chinese Subjects With Type 2 Diabetes Mellitus
  Recruiting · Early phase 1 · Interventional · 9 enrolled · The First Affiliated Hospital of Henan University of Science and Technology
  NCT07347080updated 2026-04-06

Frequently asked questions

How does Exenatide work?

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. BYETTA 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.

What is Exenatide used for?

According to FDA labeling, Exenatide carries indications including: BYETTA is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use • BYETTA contains exenatide.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Exenatide?

Exenatide is classified as Glucagon-like peptide-1 (GLP-1) analogues, GLP-1 Receptor Agonist, Glucagon-like Peptide-1 (GLP-1) Agonists, Decreased Gastric Motility, Decreased Glucagon Secretion, Increased Insulin Secretion.

What are the brand names for Exenatide?

Exenatide is marketed under brand names including Bydureon, Byetta.

What are the contraindications for Exenatide?

Exenatide labeling lists contraindications including: BYETTA is contraindicated in patients with: • A prior severe hypersensitivity reaction to exenatide or to any of the excipients in BYETTA. Serious hypersensitivity reactions including anaphylaxis and angioedema have been reported with BYETTA [see Warnings and Precautions (5.7) ].. Always consult the full prescribing information and a clinician.