Exenatide

Exenatide is a 39-amino-acid peptide with the sequence of exendin-4, a hormone first isolated from the venom of the Gila monster.

Human trialsPeptide research profile

Also known as: Byetta, Bydureon, Exendin-4, AC2993, LY2148568, PT302, UNII 9P1872D4OL, CHEBI:64073

(how we review)

Dosing & scaling, explained

Amounts reported for Exenatide are listed under Reported protocols, each with its source and study kind. No amount ladder is inferred from them. This is educational source context, not a protocol or recommendation.

No source-supported amount ladder is shown

Enter a target amount only from your own reviewed source. The calculator can convert it into concentration, volume and device markings, but it will not infer an amount from product availability or another compound.

Only mcg or mg amounts are retained. The calculator derives mL, syringe units or pen clicks from the current vial strength, water volume and device.

No independently verified schedule

Clinical context

Human study rows are described per source under Reported protocols; they belong to their trial populations and are not a general amount.

Storage, handling and interpretation

Product identity

Verify the exact compound, formulation and amount against the product label or certificate before calculation.

Storage & handling

Follow the product label, certificate and validated laboratory SOP; no universal storage assumption is applied here.

Prepared solutions

Label concentration and preparation date, use sterile technique where applicable, and follow a validated stability protocol.

Reported protocols for Exenatide

What published studies and recent community write-ups report about amounts, timing and course length. 3 clinical, 1 preclinical and 1 community-reported rows, each linked to its source. These are descriptions of what others report, not instructions, and nothing here is medical advice.

ContextDoseFrequencyRouteCourseSource
Clinical3 rows
FDA label (Byetta): type 2 diabetesAdults with type 2 diabetes, as an adjunct to diet and exercise5 mcg per dose to start; 10 mcg per dose after 1 month based on responseTwice daily, within 60 minutes before the morning and evening meals (or the two main meals, at least 6 hours apart)Subcutaneous injection in the thigh, abdomen or upper arm from a 250 mcg/mL prefilled penOpen-endedNone described; a missed dose is skipped, not doubledDailyMed, National Library of Medicine (AstraZeneca label)2025
The label stresses that the drug is never given after a meal and that the step from 5 to 10 mcg waits a month to limit nausea. Its warnings cover pancreatitis, hypoglycemia when combined with insulin or sulfonylureas, kidney injury from dehydration, immune-mediated thrombocytopenia and antibody formation that can blunt the effect.
Pivotal 30-week placebo-controlled trial on top of metformin336 adults with type 2 diabetes not controlled on maximal metformin (mean age 53, BMI 34.2, HbA1c 8.2%)5 mcg for 4 weeks, then 5 or 10 mcgTwice dailySubcutaneous30 weeksNot applicableDiabetes Care (PubMed)2005
HbA1c fell 0.78 points on 10 mcg and 0.40 on 5 mcg versus a 0.08 rise on placebo, with dose-dependent weight loss of 2.8 kg and 1.6 kg. Gastrointestinal effects were the most common adverse events and hypoglycemia was mild and no more frequent than placebo. This is the trial behind the 5-then-10 mcg schedule on the label.
DURATION-1: once-weekly versus twice-daily exenatide295 patients with type 2 diabetes (HbA1c 8.3%, weight 102 kg) on diet or oral agents2 mg extended-release once weekly, or 10 mcg twice dailyOnce weekly versus twice dailySubcutaneous30 weeksNot applicableThe Lancet (PubMed)2008
The weekly formulation lowered HbA1c by 1.9 points against 1.5 for the twice-daily pen, with more patients reaching 7% or below (77% versus 61%), similar weight loss and no extra hypoglycemia. The extended-release product requires reconstitution of a microsphere powder immediately before injection, a different kind of mixing step from a lyophilized research vial.
Preclinical1 row
Intranasal brain-uptake study in miceAdult male and female CD-1 mice and APP/PS1 Alzheimer-model miceRadiolabeled tracer amounts (10 mcg of peptide was iodinated to make the tracer stock; the amount reaching each mouse is tracer-level, not a pharmacological dose)Single intranasal administrationIntranasalSingle exposureNot applicableAlzheimer's Research and Therapy (PubMed)2024
Of five incretin agonists tested, exenatide, dulaglutide and DA4-JC spread through the brain after intranasal delivery, while semaglutide did not; the authors were interested in bypassing the blood-brain barrier for Alzheimer's research, not in glucose control. A tracer study in mice says nothing about what dose a nasal spray would need to deliver in a person.
Community-reported1 row
Intranasal aerosol (research-vendor format)50 mcg per spray; 100 mcg per described serving; 10 mL bottle giving about 100 spraysNot stated beyond the per-serving figurePre-mixed nasal spray, sold for laboratory research onlyNot statedNot statedCommunity resource2026
This is a vendor claim about a product format, not a protocol. A 100 mcg nasal serving is ten times the 10 mcg injected dose, which is consistent with nasal peptides being poorly absorbed, but no published human study measures how much intranasal exenatide actually reaches the blood. The product was listed as out of stock when checked.

How a course is commonly described

  1. Month 1Clinical

    The label starts at 5 mcg twice daily, injected in the hour before the two main meals, and holds there for a month so that nausea settles before any increase.

  2. Month 2 onwardClinical

    Based on response, the dose rises to 10 mcg twice daily and continues open-ended. In the pivotal trial the 10 mcg arm lost more weight and lowered HbA1c further than the 5 mcg arm over 30 weeks.

  3. Weekly alternativeClinical

    The extended-release product replaces the twice-daily schedule with 2 mg once a week from the start, with no titration, and matched or beat the twice-daily pen on HbA1c over 30 weeks.

  • Exenatide doses are in micrograms, two orders of magnitude below the milligram doses of newer GLP-1 drugs, and the twice-daily pen is tied to meals because the drug's effect is short-lived.
  • The nasal aerosol sold by research vendors has no human absorption data behind it. The only intranasal work is a tracer study in mice aimed at brain delivery.
  • Exenatide is a prescription medicine with label warnings about pancreatitis, thrombocytopenia and hypoglycemia in combination with insulin. The rows above record what sources report, not endorsements of use.
Sources for this section (5)
  1. Byetta (exenatide) injection prescribing informationDailyMed, National Library of Medicine (AstraZeneca label)2025Clinical
  2. Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetesDiabetes Care (PubMed)2005Clinical
  3. Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority studyThe Lancet (PubMed)2008Clinical
  4. Comparing regional brain uptake of incretin receptor agonists after intranasal delivery in CD-1 mice and the APP/PS1 mouse model of Alzheimer's diseaseAlzheimer's Research and Therapy (PubMed)2024Preclinical

Plus 1 community resource (a dosing guide, forum thread or vendor write-up), reported above but not linked.

Overview

Exenatide is a 39-amino-acid peptide with the sequence of exendin-4, a hormone first isolated from the venom of the Gila monster, that activates the GLP-1 receptor to raise meal-time insulin release, slow gastric emptying and reduce appetite. It became the first GLP-1 receptor agonist approved for type 2 diabetes in 2005 as Byetta, injected twice daily before meals, followed by the once-weekly extended-release form Bydureon, and it remains a prescription medicine rather than a research chemical. Research vendors now sell it as a pre-mixed nasal aerosol; intranasal delivery has been studied in mice for brain uptake, but no peer-reviewed human study of a nasal spray was found.

What researchers are exploring

These themes describe recurring questions in published research. They are not claims of effectiveness or recommendations for use.

  • 1

    Metabolic research

    Energy balance, body composition and incretin signaling.

  • 2

    FDA label (Byetta): type 2 diabetes

    The label stresses that the drug is never given after a meal and that the step from 5 to 10 mcg waits a month to limit nausea. Its warnings cover pancreatitis, hypoglycemia when combined with insulin or sulfonylureas.

  • 3

    Pivotal 30-week placebo-controlled trial on top of metformin

    HbA1c fell 0.78 points on 10 mcg and 0.40 on 5 mcg versus a 0.08 rise on placebo, with dose-dependent weight loss of 2.8 kg and 1.6 kg. Gastrointestinal effects were the most common adverse events and hypoglycemia was.

  • 4

    DURATION-1: once-weekly versus twice-daily exenatide

    The weekly formulation lowered HbA1c by 1.9 points against 1.5 for the twice-daily pen, with more patients reaching 7% or below (77% versus 61%), similar weight loss and no extra hypoglycemia. The extended-release.

  • 5

    Intranasal brain-uptake study in mice

    Of five incretin agonists tested, exenatide, dulaglutide and DA4-JC spread through the brain after intranasal delivery, while semaglutide did not; the authors were interested in bypassing the blood-brain barrier for.

  • 6

    Intranasal aerosol (research-vendor format)

    This is a vendor claim about a product format, not a protocol. A 100 mcg nasal serving is ten times the 10 mcg injected dose, which is consistent with nasal peptides being poorly absorbed, but no published human study.

What the current evidence can support

Study models remain visible so laboratory and animal findings are not mistaken for established human outcomes.

  • Human

    Human studies and registrations

    3 protocol rows on this page come from human trials, trial registrations, regulator labels or reviews of human data. Approval status and populations are stated per row.

  • Animal

    Preclinical models

    1 protocol row describe animal, cell or toxicology work. Amounts from these rows do not translate to people.

  • Not graded

    Community-reported use

    1 row record what blogs, vendor write-ups or forums describe for Exenatide. None has been verified against primary literature.

Chemistry identifiers

Sequence, synonyms and registry identifiers as recorded in PubChem, the National Library of Medicine's open chemistry database. Formula, mass and CAS number are summarized at the top of the page.

Sequence

His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

Also listed as

Byetta, Bydureon, Exendin-4, AC2993, LY2148568, PT302, UNII 9P1872D4OL, CHEBI:64073

InChIKey

HTQBXNHDCUEHJF-XWLPCZSASA-N

IUPAC name

(4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]acetyl]amino]-5-oxopentanoic acid

Limitations and unknowns

Important limitations

  • Every amount on this page is a report of what a source describes, not a protocol to follow.
  • Preclinical and community rows do not establish a human amount, schedule or route.
  • Formulation, purity and presentation vary by supplier and are not covered by the dossier.

Sources

5 curated references, each with its journal, year and study model, plus 1 community resource reported but not linked.

  1. Exenatide (PubChem CID 45588096)PubChem, National Library of Medicine2026Not graded
  2. Byetta (exenatide) injection prescribing informationDailyMed, National Library of Medicine (AstraZeneca label)2025Human
  3. Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetesDiabetes Care (PubMed)2005Human
  4. Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority studyThe Lancet (PubMed)2008Human
  5. Comparing regional brain uptake of incretin receptor agonists after intranasal delivery in CD-1 mice and the APP/PS1 mouse model of Alzheimer's diseaseAlzheimer's Research and Therapy (PubMed)2024Animal