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Home/Compounds/Exenatide
GLP-1 agonistFDA approvedRx required

Exenatide

Also known as: Byetta · Bydureon · Bydureon BCise
Brands: Byetta · Bydureon · Bydureon BCise

GLP-1 receptor agonist derived from exendin-4 (Gila monster peptide); the first GLP-1 drug approved for type 2 diabetes.

A
Grade A
Multiple human RCTs
Human studies25
PubMed citations27
Routesubcutaneous
Regulatory (US)FDA approved · Rx
Last verified2 days ago

Mechanism of action

Synthetic version of exendin-4, a 39-amino-acid peptide from Heloderma suspectum saliva. ~50% sequence homology to human GLP-1 but resistant to DPP-4 degradation. Binds GLP-1 receptor to enhance glucose-dependent insulin release.

Evidence summary

25
Human studies
27
PubMed citations
25
Clinical trials
A
Evidence grade

First-in-class GLP-1 RA. EXSCEL cardiovascular outcomes trial evaluated exenatide ER vs placebo.

Dosing protocols

Educational information only. Consult a licensed provider before using any peptide.
Administration routes
subcutaneous

Side effects & safety

From the FDA label
Source
abdominal painacute kidney injuryastheniaconstipationdecreased appetitedehydrationdiarrheadizzinessdyspepsiaeructationgastroesophageal reflux diseaseheadachehypoglycemianauseapancreatitispruritusrashurticariavomiting

Terms pulled directly from the referenced source. We don't fabricate frequencies — when a label doesn't publish a percentage, we don't either.

Interactions

No documented drug interactions on file.

Regulatory status

United States
FDA approved

FDA approved for type 2 diabetes (Byetta twice-daily, Bydureon weekly)

Compounding
Not permitted

Not available via 503A/503B compounding pharmacies.

Regulatory data last verified 4/19/2026

Clinical trials

NCT07497399Targeting Agonists of Glucagon-like Peptide-1 Receptor for Multiple Sclerosis (TAG-MS): A Phase 2, Randomized, Double-Blind, Parallel-Arm StudyRecruiting · Phase 2 · Multiple Sclerosis · n=120NCT00679042Islet Transplantation in Type 1 Diabetic Patients Using the UIC Protocol, Phase 3Active Not Recruiting · Phase 3 · Type 1 Diabetes Mellitus · n=21NCT07347080A Single-Center, Open-Label, Single Ascending Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Exenatide Circular RNA-Lipid Nanoparticle Injection (CR059) in Chinese Subjects With Type 2 Diabetes MellitusRecruiting · Phase 1 · T2DM · n=9NCT05610800A Randomized Controlled Trial of Exenatide as an Adjunct to Nicotine Patch for Smoking Cessation and Prevention of Post-Cessation Weight GainCompleted · Phase 2 · Smoking Cessation · n=140NCT05663515EXCEED - 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 DrugsRecruiting · Pancreatic Cancer · n=24000NCT06252623A Human Laboratory Study of Exenatide for Reducing the Reinforcing Effects of CocaineWithdrawn · Phase 1 · Cocaine Use DisorderNCT05356104GLP-1 Analogue in Preventing Progression of Small Vessel Disease (GAPP-SVD) - A Pilot StudyRecruiting · Phase 2 · Cerebral Small Vessel Disease · n=110NCT02251431MB001-067 A PROSPECTIVE, DOUBLE BLIND, PLACEBO CONTROLLED, PARALLEL GROUP, RANDOMIZED TRIAL OF EXTENDED RELEASE EXENATIDE VERSUS PLACEBO (COHORT A) AND A PROSPECTIVE, SINGLE GROUP, OPEN-LABEL, BLINDED OUTCOME TRIAL OF EXTENDED RELEASE EXENATIDE (COHORT B) IN DIABETIC PATIENTS WITH TYPE 4 CARDIORENAL SYNDROME (EXTEND-CRS TRIAL) AMENDMENT 3Completed · Phase 3 · Type 2 Diabetes Mellitus · n=57NCT04897802Identification and Clinical Relevance of an Oxytocin Deficient State: a Randomized, Crossover, Placebo-controlled, Proof-of-concept, Physiopathological Study (GLP1 Study)Completed · Phase 4 · Hypopituitarism · n=42NCT07340437Clinical Study of an ¹⁸F-labeled GLP-1R Probe in InsulinomaCompleted · Insulinoma · n=20NCT02586831A Pilot, Safety and Feasibility Trial of Anti-Thymocyte Globulin (ATG), Low Dose Interleukin-2 (IL-2), Adalimumab and Exenatide in the Treatment of New-Onset Type 1 DiabetesWithdrawn · Phase 1 · Diabetes Mellitus, Type 1NCT05482789Pilot Study of Exenatide Pharmacokinetics and Pharmacodynamics in Gestational DiabetesRecruiting · Phase 4 · Gestational Diabetes · n=13

Showing 12 of 25 indexed studies. View all on ClinicalTrials.gov →

Citations

PMID 34452224Benet A, Halseth T et al. · The Effects of pH and Excipients on Exenatide Stability in Solution.Pharmaceutics (2026)HumanPMID 40710038Patton L, Reverdito V et al. · A Case Series on the Efficacy of the Pharmacological Treatment of Lipedema: The Italian Experience with Exenatide.Clinics and practice (2025)PMID 40172827West J, Li M et al. · Are Glucagon-Like Peptide-1 (GLP-1) Receptor Agonists Central Nervous System (CNS) Penetrant: A Narrative Review.Neurology and therapy (2025)HumanPMID 40105430Gilor C, Fleeman LM et al. · Assessment of Exenatide Extended-Release for Maintenance of Diabetic Remission in Cats.Journal of veterinary internal medicine (2025)HumanPMID 39780397Yammine L, de Dios C et al. · Exploring Predictors of Treatment Response to GLP-1 Receptor Agonists for Smoking Cessation.Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco (2025)HumanPMID 38677445Hölscher C · Glucagon-like peptide-1 class drugs show clear protective effects in Parkinson's and Alzheimer's disease clinical trials: A revolution in the making?Neuropharmacology (2024)HumanPMID 38450721Gatta-Cherifi B, Mohammedi K et al. · Impact of exenatide on weight loss and eating behavior in adults with craniopharyngioma-related obesity: the CRANIOEXE randomized placebo-controlled trial.European journal of endocrinology (2024)HumanPMID 37192432Chandrashekar C, Nishiuchi Y et al. · Glycosylation Improves the Proteolytic Stability of Exenatide.Bioconjugate chemistry (2023)HumanPMID 36066977Klausen MK, Jensen ME et al. · Exenatide once weekly for alcohol use disorder investigated in a randomized, placebo-controlled clinical trial.JCI insight (2022)HumanPMID 31518224Mullins RJ, Mustapic M et al. · A Pilot Study of Exenatide Actions in Alzheimer's Disease.Current Alzheimer research (2020)HumanPMID 31748513Li Y, Vaughan KL et al. · Pharmacokinetics of Exenatide in nonhuman primates following its administration in the form of sustained-release PT320 and Bydureon.Scientific reports (2020)HumanPMID 31612934Guyton J, Jeon M et al. · Glucagon-like peptide 1 receptor agonists in type 1 diabetes mellitus.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists (2020)HumanPMID 30156747Gentilella R, Pechtner V et al. · Glucagon-like peptide-1 receptor agonists in type 2 diabetes treatment: are they all the same?Diabetes/metabolism research and reviews (2019)HumanPMID 29949126Sfairopoulos D, Liatis S et al. · Clinical pharmacology of glucagon-like peptide-1 receptor agonists.Hormones (Athens, Greece) (2019)HumanPMID 29260924Molina Vega M, Muñoz-Garach A et al. · Pharmacokinetic drug evaluation of exenatide for the treatment of type 2 diabetes.Expert opinion on drug metabolism & toxicology (2018)HumanPMID 27981757Htike ZZ, Zaccardi F et al. · Efficacy and safety of glucagon-like peptide-1 receptor agonists in type 2 diabetes: A systematic review and mixed-treatment comparison analysis.Diabetes, obesity & metabolism (2017)HumanPMID 28085521Knop FK, Brønden A et al. · Exenatide: pharmacokinetics, clinical use, and future directions.Expert opinion on pharmacotherapy (2017)HumanPMID 26926319Brunton S, Davidson JA · Exenatide Once Weekly: A Review of Pharmacology and Treatment Considerations in Type 2 Diabetes.Clinical therapeutics (2016)HumanPMID 23425609Wysham C, Grimm M et al. · Once weekly exenatide: efficacy, tolerability and place in therapy.Diabetes, obesity & metabolism (2014)HumanPMID 24923102Scheen AJ · [Bydureon: first once weekly GLP-1 receptor agonist (exenatide LAR)].Revue medicale de Liege (2014)Human

Showing 20 of 27 papers. View all on PubMed →