Exenatide
updated
Exenatide is an FDA-approved injectable for type 2 diabetes, with a 2024 generic approval and a 14,752-patient cardiovascular outcome trial. Injected exenatide lowers weight modestly: 1 to 3 kg over placebo in type 2 diabetes trials, and 5.1 kg versus 1.6 kg on placebo over 24 weeks in nondiabetic adults with obesity. Searches on 9 October 2026 found no published human data for an oral, sublingual, buccal or intranasal exenatide product.
GLP-1 receptor agonist peptide
- FDA approved BYETTA on 28 April 2005 as an adjunct to diet and exercise for glycemic control in adults with type 2 diabetes. It is not labeled for weight loss or obesity.
- Every approved US exenatide product in the FDA record is an injection; a synthetic injection from Amneal was approved on 19 November 2024.
- In 152 obese adults without diabetes, 24 weeks of injected exenatide plus lifestyle intervention gave 5.1 kg of weight loss versus 1.6 kg on placebo.
- EXSCEL (14,752 adults with type 2 diabetes, median 3.2 years) was noninferior for cardiovascular safety (P<0.001) and not superior for efficacy (P=0.06).
- A PubMed search on 9 October 2026 for exenatide with intranasal or nasal use, limited to human studies, returned 12 records; none reported a human nasal exenatide dose.
- In rats, sublingual exenatide reached 0.37% of the intravenous bioavailability; the authors concluded the intestinal tract has limited potential.
What is exenatide approved to do?
FDA approved exenatide as BYETTA in 2005 as an adjunct to diet and exercise for glycemic control in adults with type 2 diabetes. It is not labeled for weight loss or obesity.
Exenatide is synthetic exendin-4, a 39-residue peptide (PubChem CID 45588096, C184H282N50O60S, molecular weight 4187 g/mol, CAS 141758-74-9). Listed synonyms include Byetta, Bydureon, exendin-4 and AC2993. The molecule in every study on this page is the same peptide. Route and formulation are what differ, so a vendor spray is not the injectable product by sharing a name.
BYETTA is a solution for subcutaneous injection, labeled as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. The label version used here took effect on 2 September 2025. FDA approved BYETTA under NDA 021773 on 28 April 2005, and a synthetic exenatide injection from Amneal under ANDA 206697 on 19 November 2024. Every approved US exenatide product in the FDA record is an injection. The current US marketing status of each product is not stated here.
PubChem: exenatide identity
Chemical identity record
National Library of Medicine. PubChem compound record CID 45588096 (exenatide).
Exenatide is synthetic exendin-4, a 39-residue peptide: PubChem CID 45588096, C184H282N50O60S, molecular weight 4187 g/mol, CAS 141758-74-9. Listed synonyms include Byetta, Bydureon, exendin-4 and AC2993.
- Participants / model
- Chemical identity, not a clinical population
- Treatment
- Defined peptide
- Follow-up
- Not applicable
- Study design
- NLM chemical record
- Funding
- not stated in the source
The molecule in every study on this page is the same peptide. Route and formulation differ, so a vendor spray is not the injectable product by sharing a name.
Read the original sourceBYETTA label, version effective 2 September 2025: indication, weight, PK, safety
FDA prescribing information
DailyMed, U.S. National Library of Medicine. BYETTA (exenatide) solution for subcutaneous injection, 5 and 10 mcg per dose, prescribing information, label version effective 2 September 2025. Set ID 53d03c03-ebf7-418d-88a8-533eabd2ee4f.
The label approves BYETTA as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It is not labeled for weight loss or obesity. Weight change was a secondary measure in the glycemic trials: placebo differences of -1.3 and -1.5 kg at 24 weeks, -1.1 and -2.4 kg at 30 weeks with metformin, and -4.5 kg versus insulin lispro. After a 10 mcg subcutaneous dose, median Tmax was 2.1 hours and mean terminal half-life 2.4 hours. In three 30-week placebo-controlled add-on trials (BYETTA n=963, placebo n=483), nausea occurred in 44% versus 18%. Warnings cover acute pancreatitis including fatal cases, hypoglycemia with insulin secretagogues or insulin, acute kidney injury, severe gastrointestinal reactions, immunogenicity, hypersensitivity, thrombocytopenia, acute gallbladder disease and pulmonary aspiration during general anesthesia or deep sedation.
- Participants / model
- Adults with type 2 diabetes; label PK participants
- Treatment
- BYETTA solution for subcutaneous injection, 5 and 10 mcg per dose
- Follow-up
- Label version effective 2 September 2025; label trials of 24 and 30 weeks
- Study design
- FDA prescribing information
- Funding
- not stated in the source
Weight results are secondary measures from glycemic trials. The twice-daily BYETTA label reviewed carries no boxed warning.
Read the original sourceDrugs@FDA: BYETTA 2005 and generic 2024 approval dates
Regulatory record
U.S. Food and Drug Administration. Drugs@FDA application record for NDA 021773 (BYETTA), with ANDA 206697 (Amneal). Dates read from the openFDA Drugs@FDA records on 9 October 2026.
FDA approved BYETTA under NDA 021773 on 28 April 2005. A synthetic exenatide injection from Amneal was approved under ANDA 206697 on 19 November 2024. Every approved US exenatide product in that record is an injection.
- Participants / model
- Not a clinical population
- Treatment
- Drug applications
- Follow-up
- Approvals in 2005 and 2024
- Study design
- FDA application records
- Funding
- not stated in the source
These records give approval dates; current marketing status is not stated here.
Read the original sourceWhat did the diabetes trials find?
In DURATION-1, once-weekly exenatide lowered HbA1c by 1.9% versus 1.5% with twice-daily dosing. In EXSCEL, cardiovascular outcomes were noninferior to placebo but not superior.
DURATION-1 was a 30-week randomized open-label non-inferiority study in 295 patients with type 2 diabetes (baseline HbA1c 8.3%, weight 102 kg). It compared once-weekly 2 mg long-acting release exenatide with 10 mcg twice daily, both subcutaneous. HbA1c fell 1.9% once weekly versus 1.5% twice daily (95% CI -0.54 to -0.12, p=0.0023), and 77% versus 61% reached HbA1c at or below 7.0% (p=0.0039). The authors reported similar bodyweight reductions in both arms. The trial is registered as NCT00308139.
EXSCEL randomized 14,752 adults with type 2 diabetes (73.1% with previous cardiovascular disease) to subcutaneous extended-release exenatide 2 mg once weekly or placebo, with a median follow-up of 3.2 years. The primary composite of cardiovascular death, nonfatal myocardial infarction or nonfatal stroke occurred in 11.4% versus 12.2% (hazard ratio 0.91, 95% CI 0.83 to 1.00): noninferior for safety (P<0.001) but not superior for efficacy (P=0.06). It is the largest safety dataset for the molecule, and a neutral cardiovascular result. The trial is registered as NCT01144338.
DURATION-1: 295 patients, 30 weeks, HbA1c -1.9% versus -1.5%
Randomized controlled trial
Drucker DJ et al. Lancet. 2008;372(9645):1240-50. PMID 18782641.
HbA1c fell 1.9% once weekly versus 1.5% twice daily (95% CI -0.54 to -0.12, p=0.0023), with 77% versus 61% reaching HbA1c at or below 7.0% (p=0.0039). The authors reported similar bodyweight reductions in both arms.
- Participants / model
- 295 patients with type 2 diabetes (baseline HbA1c 8.3%, weight 102 kg)
- Treatment
- Subcutaneous exenatide: once-weekly 2 mg long-acting release versus 10 mcg twice daily
- Follow-up
- 30 weeks
- Study design
- Randomized open-label non-inferiority trial
- Funding
- not stated in the source
Both arms were subcutaneous injections. The study was open-label.
Read the original sourceEXSCEL: 14,752 patients, median 3.2 years, neutral cardiovascular result
Randomized controlled trial
Holman RR et al. N Engl J Med. 2017;377(13):1228-1239. PMID 28910237.
The primary composite of cardiovascular death, nonfatal myocardial infarction or nonfatal stroke occurred in 11.4% versus 12.2% (hazard ratio 0.91, 95% CI 0.83 to 1.00): noninferior for safety (P<0.001) but not superior for efficacy (P=0.06). Rates of acute pancreatitis, pancreatic cancer, medullary thyroid carcinoma and serious adverse events did not differ significantly.
- Participants / model
- 14,752 adults with type 2 diabetes (73.1% with previous cardiovascular disease)
- Treatment
- Extended-release exenatide 2 mg subcutaneously once weekly, or placebo
- Follow-up
- Median follow-up 3.2 years
- Study design
- Randomized placebo-controlled cardiovascular outcome trial
- Funding
- not stated in the source
This is the largest safety dataset for the molecule, and it is a neutral cardiovascular result.
Read the original sourceHow much weight did injected exenatide take off?
In type 2 diabetes trials of 6 to 7 months, 1 to 3 kg more than placebo. In 152 obese adults without diabetes, 5.1 kg versus 1.6 kg on placebo over 24 weeks. All by subcutaneous injection.
Weight was a secondary measure in the BYETTA label's glycemic trials. In the 24-week monotherapy trial, change from baseline was -1.5 kg on placebo, -2.7 kg (5 mcg) and -2.9 kg (10 mcg), with placebo differences of -1.3 kg (95% CI -2.3 to -0.2) and -1.5 kg (-2.5 to -0.4). Added to metformin for 30 weeks, change was -0.2 kg on placebo, -1.3 kg (5 mcg) and -2.6 kg (10 mcg), with placebo differences of -1.1 kg (-2.2 to -0.0) and -2.4 kg (-3.5 to -1.3). Against insulin lispro for 30 weeks, weight rose 1.9 kg on lispro and fell 2.6 kg on BYETTA, a difference of -4.5 kg (-5.2 to -3.9). The doses were given by subcutaneous injection twice daily.
In 152 obese adults without diabetes (mean age 46, 82% female, mean weight 108.6 kg, mean BMI 39.6; 25% with impaired glucose tolerance or impaired fasting glucose), randomized to subcutaneous exenatide or placebo plus lifestyle intervention for 24 weeks, the exenatide group lost 5.1 +/- 0.5 kg versus 1.6 +/- 0.5 kg on placebo (P<0.001). The placebo-subtracted difference was -3.3 +/- 0.5% of body weight, and both groups cut daily calories. This is the trial closest to the supplier's weight-loss claim, and it used the injectable.
BYETTA label, version effective 2 September 2025: indication, weight, PK, safety
FDA prescribing information
DailyMed, U.S. National Library of Medicine. BYETTA (exenatide) solution for subcutaneous injection, 5 and 10 mcg per dose, prescribing information, label version effective 2 September 2025. Set ID 53d03c03-ebf7-418d-88a8-533eabd2ee4f.
The label approves BYETTA as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It is not labeled for weight loss or obesity. Weight change was a secondary measure in the glycemic trials: placebo differences of -1.3 and -1.5 kg at 24 weeks, -1.1 and -2.4 kg at 30 weeks with metformin, and -4.5 kg versus insulin lispro. After a 10 mcg subcutaneous dose, median Tmax was 2.1 hours and mean terminal half-life 2.4 hours. In three 30-week placebo-controlled add-on trials (BYETTA n=963, placebo n=483), nausea occurred in 44% versus 18%. Warnings cover acute pancreatitis including fatal cases, hypoglycemia with insulin secretagogues or insulin, acute kidney injury, severe gastrointestinal reactions, immunogenicity, hypersensitivity, thrombocytopenia, acute gallbladder disease and pulmonary aspiration during general anesthesia or deep sedation.
- Participants / model
- Adults with type 2 diabetes; label PK participants
- Treatment
- BYETTA solution for subcutaneous injection, 5 and 10 mcg per dose
- Follow-up
- Label version effective 2 September 2025; label trials of 24 and 30 weeks
- Study design
- FDA prescribing information
- Funding
- not stated in the source
Weight results are secondary measures from glycemic trials. The twice-daily BYETTA label reviewed carries no boxed warning.
Read the original sourceNondiabetic obesity: 152 adults, 24 weeks, 5.1 kg versus 1.6 kg
Randomized controlled trial
Rosenstock J et al. Diabetes Care. 2010;33(6):1173-5. PMID 20332357.
The exenatide group lost 5.1 +/- 0.5 kg versus 1.6 +/- 0.5 kg on placebo (P<0.001), a placebo-subtracted difference of -3.3 +/- 0.5% of body weight. Both groups cut daily calories.
- Participants / model
- 152 obese adults without diabetes (mean age 46, 82% female, mean weight 108.6 kg, mean BMI 39.6; 25% with impaired glucose tolerance or impaired fasting glucose)
- Treatment
- Subcutaneous exenatide or placebo, plus lifestyle intervention
- Follow-up
- 24 weeks
- Study design
- Randomized trial
- Funding
- not stated in the source
This is the trial closest to the supplier's weight-loss claim, and it used the injectable.
Read the original sourceDoes a pre-made oral or sublingual spray work like the injection?
No human data support it. Searches of PubMed and ClinicalTrials.gov on 9 October 2026 found no published human efficacy, pharmacokinetic or safety data for oral, sublingual, buccal or intranasal exenatide.
Sellers promote exenatide for weight loss and appetite suppression through GLP-1 agonism, as a pre-made oral or sublingual aerosol spray rather than a reconstituted injectable. The weight effect on this page was measured with the injection. The spray is a different dose form.
A PubMed search on 9 October 2026 for exenatide with intranasal or nasal, restricted to the humans MeSH term, returned 12 records: reviews, rodent and ex vivo formulation work, one oral nanoparticle study and one adverse-event database review. None reported a human nasal exenatide dose. A second search for exenatide with sublingual, buccal, oral spray or aerosol returned 5 records: the rat and mouse route-comparison study, two reviews, an analytical chemistry paper and an inhaled microparticle study. None reported a human sublingual, buccal or oral-spray exenatide dose.
On ClinicalTrials.gov the same day, a query for intranasal exenatide returned no studies, and a query for sublingual exenatide returned 2 studies (NCT03010683 and NCT00353834), both of injected GLP-1 receptor agonists in vascular-function populations.
Searches, 9 October 2026: no human data for non-injected exenatide
PubMed search record
PubMed search run on 9 October 2026: exenatide AND (intranasal OR nasal), restricted to the humans MeSH term, 12 records. A second PubMed search for exenatide with sublingual, buccal, oral spray or aerosol returned 5 records. ClinicalTrials.gov queries run the same day.
The nasal search returned 12 records: reviews, rodent and ex vivo formulation work, one oral nanoparticle study and one adverse-event database review. None reported a human nasal exenatide dose. The second search returned 5 records: the rat and mouse route-comparison study, two reviews, an analytical chemistry paper and an inhaled microparticle study; none reported a human sublingual, buccal or oral-spray exenatide dose. On ClinicalTrials.gov, a query for intranasal exenatide returned no studies, and a query for sublingual exenatide returned 2 studies (NCT03010683 and NCT00353834), both of injected GLP-1 receptor agonists in vascular-function populations. No oral, sublingual, buccal or intranasal exenatide product has published human efficacy, pharmacokinetic or safety data among these records.
- Participants / model
- Records returned, not a population
- Treatment
- Not applicable
- Follow-up
- Searches run on 9 October 2026
- Study design
- Literature and registry searches
- Funding
- not stated in the source
A search result shows what the databases returned on that date. It is not proof that no unindexed study exists.
Read the original sourceWhat do animal studies say about non-injected routes?
The only head-to-head route comparison found is in rats and mice. Sublingual delivery reached 0.37% of intravenous bioavailability in rats, and the authors concluded the respiratory tract is more viable than the intestinal tract.
The study was run by the drug's originator. In normoglycemic rats, bioavailability versus intravenous was 0.37% sublingual, 0.0053% intraduodenal, 1.68% nasal and up to 13.6% intratracheal, with similar elimination kinetics for every route (median ke 0.017 per minute). Glucose lowering was obtained in db/db mice by the nasal, intratracheal and high-dose aerosol routes.
The authors concluded that the intestinal tract has limited potential, with sublingual the most promising of the gastrointestinal routes, and that the respiratory tract is more viable. These are rodent numbers and do not transfer to people.
A separate bioanalytical paper validated a UPLC-MS/MS assay for exenatide (lower limit of quantification 5 pg/mL, or 1.2 pM, in 200 microlitres of plasma) and demonstrated it by quantifying exenatide after intravenous and nasal administration to beagle dogs. The paper's abstract states no nasal bioavailability, Cmax or Tmax value, so none is given here. A nasal bioavailability figure attributed to it elsewhere is not in the abstract.
Rodent route comparison: sublingual 0.37% of intravenous in rats
Animal study
Gedulin BR et al. Int J Pharm. 2008;356(1-2):231-8. PMID 18291606.
In normoglycemic rats, bioavailability versus intravenous was 0.37% sublingual, 0.0053% intraduodenal, 1.68% nasal and up to 13.6% intratracheal, with similar elimination kinetics for every route (median ke 0.017 per minute). Glucose lowering was obtained in db/db mice by the nasal, intratracheal and high-dose aerosol routes. The authors concluded the intestinal tract has limited potential, with sublingual the most promising of the gastrointestinal routes, and that the respiratory tract is more viable.
- Participants / model
- Normoglycemic rats (pharmacokinetics) and diabetic db/db mice (glucose lowering)
- Treatment
- Sublingual, intraduodenal, nasal, intratracheal and aerosolized exenatide solutions
- Follow-up
- not stated in the source
- Study design
- Preclinical route comparison
- Funding
- not stated in the source
The only head-to-head route comparison found for exenatide, run by the originator. These are rodent numbers and do not transfer to people.
Read the original sourceExenatide assay paper: beagle dogs, no nasal bioavailability stated
Animal study
Sauter M et al. J Pharm Anal. 2020;10(3):233-239. PMID 32612869.
The assay has a lower limit of quantification of 5 pg/mL (1.2 pM) in 200 microlitres of plasma. Its applicability was shown by quantifying exenatide after intravenous and nasal administration to beagle dogs. The abstract states no nasal bioavailability, Cmax or Tmax value.
- Participants / model
- Beagle dogs (applicability demonstration); human plasma (assay validation)
- Treatment
- Intravenous and nasal exenatide
- Follow-up
- not stated in the source
- Study design
- Bioanalytical method validation
- Funding
- not stated in the source
A secondary source attributed a specific nasal bioavailability figure to this paper. The abstract does not contain one, so none is carried onto this page.
Read the original sourceDo trials of other nasal peptides show what a spray would do?
Not for exenatide. A nasal native GLP-1 trial in 26 patients with type 2 diabetes was exploratory, and a thrice-daily nasal PYY3-36 trial for obesity in 133 adults did not show efficacy.
The one human trial of a nasal incretin peptide found used a different molecule. In 26 Japanese patients with type 2 diabetes, a nasal compound containing 1.2 mg human GLP-1(7-36)amide or placebo before every meal for 2 weeks gave a peak plasma active GLP-1 of 47.2 pmol/L at Tmax 8.1 min. Early-phase insulin secretion recovered, glucagon was suppressed and glycoalbumin fell significantly, and the authors reported no marked adverse events. They called the study exploratory and said long-term use needs evaluation. This is native GLP-1, not exenatide, and the abstract reports no bioavailability figure and no weight outcome.
The closest human test of the product concept, a thrice-daily nasal gut peptide for obesity, did not show efficacy. In 133 obese adults (BMI 30 to 43, age 18 to 65), intranasal PYY3-36 at 200 or 600 mcg three times daily 20 minutes before meals, with a hypocaloric diet, over 12 weeks, completion was 38/43 (88%) on placebo, 31/44 (70%) at 200 mcg and 12/46 (26%) at 600 mcg. In the 600 mcg arm, 27 of 46 (59%) stopped for nausea and vomiting. Mean weight change was -2.8, -3.7 and -1.4 kg across the three arms; the placebo versus 200 mcg difference was -0.9 kg (95% CI -2.6 to 0.7, P=0.251) against a sought difference of 2.11 kg. The published conclusion was that it is not efficacious.
It was a different peptide by the same route, with the same dosing pattern, in the same kind of population as the supplier claim. It does not show what an exenatide spray would do.
Nasal native GLP-1: 26 patients, 2 weeks, different compound
Clinical trial
Ueno H et al. Diabetes Care. 2014;37(7):2024-7. PMID 24667460.
Peak plasma active GLP-1 was 47.2 pmol/L with Tmax 8.1 min. Early-phase insulin secretion recovered, glucagon was suppressed and glycoalbumin fell significantly. The authors reported no marked adverse events, called the study exploratory and said long-term use needs evaluation.
- Participants / model
- 26 Japanese patients with type 2 diabetes
- Treatment
- Nasal compound containing 1.2 mg human GLP-1(7-36)amide, or placebo, before every meal
- Follow-up
- 2 weeks
- Study design
- Placebo-controlled clinical trial
- Funding
- not stated in the source
This is native GLP-1, not exenatide. The abstract reports no bioavailability figure and no weight outcome.
Read the original sourceNasal PYY3-36: 133 obese adults, 12 weeks, not efficacious
Randomized controlled trial
Gantz I et al. J Clin Endocrinol Metab. 2007;92(5):1754-7. PMID 17341568.
Completion was 38/43 (88%) on placebo, 31/44 (70%) at 200 mcg and 12/46 (26%) at 600 mcg, with 27 of 46 (59%) on 600 mcg stopping for nausea and vomiting. Mean weight change was -2.8, -3.7 and -1.4 kg across the three arms; the placebo versus 200 mcg difference was -0.9 kg (95% CI -2.6 to 0.7, P=0.251) against a sought difference of 2.11 kg. The published conclusion was that it is not efficacious.
- Participants / model
- 133 obese adults (BMI 30 to 43, age 18 to 65)
- Treatment
- Intranasal PYY3-36 spray, 200 or 600 mcg three times daily 20 minutes before meals, or placebo, with a hypocaloric diet
- Follow-up
- 12 weeks
- Study design
- Randomized placebo-controlled trial
- Funding
- not stated in the source
A different peptide by the same route, with the same dosing pattern, in the same kind of population as the supplier claim. It does not show what an exenatide spray would do.
Read the original sourceHow does exenatide work, and what happens to it in the body?
Exenatide acts as a GLP-1 receptor agonist. After a 10 mcg subcutaneous dose in the label's PK participants, median Tmax was 2.1 hours and mean terminal half-life 2.4 hours.
GLP-1 agonism is the mechanism sellers cite for appetite and weight effects. The weight and glycemic results on this page are for injected exenatide. Whether a sprayed or sublingual dose form delivers enough peptide to act is a question of exposure, and the searches found no human exposure data for non-injected exenatide.
After a 10 mcg subcutaneous dose, label PK participants had a median Tmax of 2.1 hours, mean Cmax of 211 pg/mL, mean AUC(0-inf) of 1036 pg.h/mL, mean apparent clearance of 9.1 L/hour and a mean terminal half-life of 2.4 hours. Exenatide was measurable for about 10 hours. Elimination is predominantly glomerular filtration with subsequent proteolytic degradation.
BYETTA label, version effective 2 September 2025: indication, weight, PK, safety
FDA prescribing information
DailyMed, U.S. National Library of Medicine. BYETTA (exenatide) solution for subcutaneous injection, 5 and 10 mcg per dose, prescribing information, label version effective 2 September 2025. Set ID 53d03c03-ebf7-418d-88a8-533eabd2ee4f.
The label approves BYETTA as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It is not labeled for weight loss or obesity. Weight change was a secondary measure in the glycemic trials: placebo differences of -1.3 and -1.5 kg at 24 weeks, -1.1 and -2.4 kg at 30 weeks with metformin, and -4.5 kg versus insulin lispro. After a 10 mcg subcutaneous dose, median Tmax was 2.1 hours and mean terminal half-life 2.4 hours. In three 30-week placebo-controlled add-on trials (BYETTA n=963, placebo n=483), nausea occurred in 44% versus 18%. Warnings cover acute pancreatitis including fatal cases, hypoglycemia with insulin secretagogues or insulin, acute kidney injury, severe gastrointestinal reactions, immunogenicity, hypersensitivity, thrombocytopenia, acute gallbladder disease and pulmonary aspiration during general anesthesia or deep sedation.
- Participants / model
- Adults with type 2 diabetes; label PK participants
- Treatment
- BYETTA solution for subcutaneous injection, 5 and 10 mcg per dose
- Follow-up
- Label version effective 2 September 2025; label trials of 24 and 30 weeks
- Study design
- FDA prescribing information
- Funding
- not stated in the source
Weight results are secondary measures from glycemic trials. The twice-daily BYETTA label reviewed carries no boxed warning.
Read the original sourcePubChem: exenatide identity
Chemical identity record
National Library of Medicine. PubChem compound record CID 45588096 (exenatide).
Exenatide is synthetic exendin-4, a 39-residue peptide: PubChem CID 45588096, C184H282N50O60S, molecular weight 4187 g/mol, CAS 141758-74-9. Listed synonyms include Byetta, Bydureon, exendin-4 and AC2993.
- Participants / model
- Chemical identity, not a clinical population
- Treatment
- Defined peptide
- Follow-up
- Not applicable
- Study design
- NLM chemical record
- Funding
- not stated in the source
The molecule in every study on this page is the same peptide. Route and formulation differ, so a vendor spray is not the injectable product by sharing a name.
Read the original sourceSearches, 9 October 2026: no human data for non-injected exenatide
PubMed search record
PubMed search run on 9 October 2026: exenatide AND (intranasal OR nasal), restricted to the humans MeSH term, 12 records. A second PubMed search for exenatide with sublingual, buccal, oral spray or aerosol returned 5 records. ClinicalTrials.gov queries run the same day.
The nasal search returned 12 records: reviews, rodent and ex vivo formulation work, one oral nanoparticle study and one adverse-event database review. None reported a human nasal exenatide dose. The second search returned 5 records: the rat and mouse route-comparison study, two reviews, an analytical chemistry paper and an inhaled microparticle study; none reported a human sublingual, buccal or oral-spray exenatide dose. On ClinicalTrials.gov, a query for intranasal exenatide returned no studies, and a query for sublingual exenatide returned 2 studies (NCT03010683 and NCT00353834), both of injected GLP-1 receptor agonists in vascular-function populations. No oral, sublingual, buccal or intranasal exenatide product has published human efficacy, pharmacokinetic or safety data among these records.
- Participants / model
- Records returned, not a population
- Treatment
- Not applicable
- Follow-up
- Searches run on 9 October 2026
- Study design
- Literature and registry searches
- Funding
- not stated in the source
A search result shows what the databases returned on that date. It is not proof that no unindexed study exists.
Read the original sourceWhat risks do the label and trials report?
The BYETTA label warns about acute pancreatitis, hypoglycemia with insulin or insulin secretagogues, acute kidney injury, severe gastrointestinal reactions, hypersensitivity and other serious events. Nausea occurred in 44% versus 18% on placebo.
In three 30-week placebo-controlled add-on trials (BYETTA n=963, placebo n=483), nausea occurred in 44% versus 18%, vomiting in 13% versus 4%, diarrhea in 13% versus 6%, feeling jittery in 9% versus 4%, dizziness in 9% versus 6% and headache in 9% versus 6%. Nausea was dose-dependent. The most common withdrawals were for nausea (3%) and vomiting (1%). Gallbladder events occurred in 1.9% of exenatide-treated versus 1.4% of placebo-treated patients.
Label warnings cover acute pancreatitis including fatal hemorrhagic or necrotizing cases, hypoglycemia with insulin secretagogues or insulin, acute kidney injury from volume depletion, severe gastrointestinal reactions, immunogenicity, hypersensitivity including anaphylaxis and angioedema, drug-induced immune-mediated thrombocytopenia with fatal bleeding, acute gallbladder disease, and pulmonary aspiration during general anesthesia or deep sedation. At 30 weeks, 360 patients (38%) had low-titer anti-exenatide antibodies and 59 (6%) had higher titer; attenuated glycemic response linked to antibodies occurred in 3, 4, 1 and 1% of patients across four trials.
The twice-daily BYETTA label reviewed for this page carries no boxed warning. The label for the once-weekly extended-release product was not reviewed here, so its warnings are not summarized. In EXSCEL, rates of acute pancreatitis, pancreatic cancer, medullary thyroid carcinoma and serious adverse events did not differ significantly between extended-release exenatide and placebo.
All of these data come from injected exenatide. The searches found no safety data for an oral, sublingual, buccal or intranasal exenatide product.
BYETTA label, version effective 2 September 2025: indication, weight, PK, safety
FDA prescribing information
DailyMed, U.S. National Library of Medicine. BYETTA (exenatide) solution for subcutaneous injection, 5 and 10 mcg per dose, prescribing information, label version effective 2 September 2025. Set ID 53d03c03-ebf7-418d-88a8-533eabd2ee4f.
The label approves BYETTA as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It is not labeled for weight loss or obesity. Weight change was a secondary measure in the glycemic trials: placebo differences of -1.3 and -1.5 kg at 24 weeks, -1.1 and -2.4 kg at 30 weeks with metformin, and -4.5 kg versus insulin lispro. After a 10 mcg subcutaneous dose, median Tmax was 2.1 hours and mean terminal half-life 2.4 hours. In three 30-week placebo-controlled add-on trials (BYETTA n=963, placebo n=483), nausea occurred in 44% versus 18%. Warnings cover acute pancreatitis including fatal cases, hypoglycemia with insulin secretagogues or insulin, acute kidney injury, severe gastrointestinal reactions, immunogenicity, hypersensitivity, thrombocytopenia, acute gallbladder disease and pulmonary aspiration during general anesthesia or deep sedation.
- Participants / model
- Adults with type 2 diabetes; label PK participants
- Treatment
- BYETTA solution for subcutaneous injection, 5 and 10 mcg per dose
- Follow-up
- Label version effective 2 September 2025; label trials of 24 and 30 weeks
- Study design
- FDA prescribing information
- Funding
- not stated in the source
Weight results are secondary measures from glycemic trials. The twice-daily BYETTA label reviewed carries no boxed warning.
Read the original sourceEXSCEL: 14,752 patients, median 3.2 years, neutral cardiovascular result
Randomized controlled trial
Holman RR et al. N Engl J Med. 2017;377(13):1228-1239. PMID 28910237.
The primary composite of cardiovascular death, nonfatal myocardial infarction or nonfatal stroke occurred in 11.4% versus 12.2% (hazard ratio 0.91, 95% CI 0.83 to 1.00): noninferior for safety (P<0.001) but not superior for efficacy (P=0.06). Rates of acute pancreatitis, pancreatic cancer, medullary thyroid carcinoma and serious adverse events did not differ significantly.
- Participants / model
- 14,752 adults with type 2 diabetes (73.1% with previous cardiovascular disease)
- Treatment
- Extended-release exenatide 2 mg subcutaneously once weekly, or placebo
- Follow-up
- Median follow-up 3.2 years
- Study design
- Randomized placebo-controlled cardiovascular outcome trial
- Funding
- not stated in the source
This is the largest safety dataset for the molecule, and it is a neutral cardiovascular result.
Read the original sourceSearches, 9 October 2026: no human data for non-injected exenatide
PubMed search record
PubMed search run on 9 October 2026: exenatide AND (intranasal OR nasal), restricted to the humans MeSH term, 12 records. A second PubMed search for exenatide with sublingual, buccal, oral spray or aerosol returned 5 records. ClinicalTrials.gov queries run the same day.
The nasal search returned 12 records: reviews, rodent and ex vivo formulation work, one oral nanoparticle study and one adverse-event database review. None reported a human nasal exenatide dose. The second search returned 5 records: the rat and mouse route-comparison study, two reviews, an analytical chemistry paper and an inhaled microparticle study; none reported a human sublingual, buccal or oral-spray exenatide dose. On ClinicalTrials.gov, a query for intranasal exenatide returned no studies, and a query for sublingual exenatide returned 2 studies (NCT03010683 and NCT00353834), both of injected GLP-1 receptor agonists in vascular-function populations. No oral, sublingual, buccal or intranasal exenatide product has published human efficacy, pharmacokinetic or safety data among these records.
- Participants / model
- Records returned, not a population
- Treatment
- Not applicable
- Follow-up
- Searches run on 9 October 2026
- Study design
- Literature and registry searches
- Funding
- not stated in the source
A search result shows what the databases returned on that date. It is not proof that no unindexed study exists.
Read the original sourceWhy does exenatide sit in A tier?
The injectable is approved for type 2 diabetes and has a large cardiovascular outcome trial and measured weight effects. The A does not extend to a sprayed or sublingual product, for which the searches found no human data.
The weight effect is real but small in the trials that measured it, and all of it was by subcutaneous injection. The supplier claim rests on a dose form with no published human data: in searches on 9 October 2026, no oral, sublingual, buccal or intranasal exenatide had published human efficacy, pharmacokinetic or safety data, and the only route comparison found is a rat study in which sublingual delivery reached 0.37% of intravenous bioavailability.
The closest human analogue, a thrice-daily nasal gut peptide for obesity, had 27 of 46 adults in its high-dose arm (59%) stop for nausea and vomiting, and its published conclusion was that it is not efficacious.
BYETTA label, version effective 2 September 2025: indication, weight, PK, safety
FDA prescribing information
DailyMed, U.S. National Library of Medicine. BYETTA (exenatide) solution for subcutaneous injection, 5 and 10 mcg per dose, prescribing information, label version effective 2 September 2025. Set ID 53d03c03-ebf7-418d-88a8-533eabd2ee4f.
The label approves BYETTA as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It is not labeled for weight loss or obesity. Weight change was a secondary measure in the glycemic trials: placebo differences of -1.3 and -1.5 kg at 24 weeks, -1.1 and -2.4 kg at 30 weeks with metformin, and -4.5 kg versus insulin lispro. After a 10 mcg subcutaneous dose, median Tmax was 2.1 hours and mean terminal half-life 2.4 hours. In three 30-week placebo-controlled add-on trials (BYETTA n=963, placebo n=483), nausea occurred in 44% versus 18%. Warnings cover acute pancreatitis including fatal cases, hypoglycemia with insulin secretagogues or insulin, acute kidney injury, severe gastrointestinal reactions, immunogenicity, hypersensitivity, thrombocytopenia, acute gallbladder disease and pulmonary aspiration during general anesthesia or deep sedation.
- Participants / model
- Adults with type 2 diabetes; label PK participants
- Treatment
- BYETTA solution for subcutaneous injection, 5 and 10 mcg per dose
- Follow-up
- Label version effective 2 September 2025; label trials of 24 and 30 weeks
- Study design
- FDA prescribing information
- Funding
- not stated in the source
Weight results are secondary measures from glycemic trials. The twice-daily BYETTA label reviewed carries no boxed warning.
Read the original sourceDrugs@FDA: BYETTA 2005 and generic 2024 approval dates
Regulatory record
U.S. Food and Drug Administration. Drugs@FDA application record for NDA 021773 (BYETTA), with ANDA 206697 (Amneal). Dates read from the openFDA Drugs@FDA records on 9 October 2026.
FDA approved BYETTA under NDA 021773 on 28 April 2005. A synthetic exenatide injection from Amneal was approved under ANDA 206697 on 19 November 2024. Every approved US exenatide product in that record is an injection.
- Participants / model
- Not a clinical population
- Treatment
- Drug applications
- Follow-up
- Approvals in 2005 and 2024
- Study design
- FDA application records
- Funding
- not stated in the source
These records give approval dates; current marketing status is not stated here.
Read the original sourceEXSCEL: 14,752 patients, median 3.2 years, neutral cardiovascular result
Randomized controlled trial
Holman RR et al. N Engl J Med. 2017;377(13):1228-1239. PMID 28910237.
The primary composite of cardiovascular death, nonfatal myocardial infarction or nonfatal stroke occurred in 11.4% versus 12.2% (hazard ratio 0.91, 95% CI 0.83 to 1.00): noninferior for safety (P<0.001) but not superior for efficacy (P=0.06). Rates of acute pancreatitis, pancreatic cancer, medullary thyroid carcinoma and serious adverse events did not differ significantly.
- Participants / model
- 14,752 adults with type 2 diabetes (73.1% with previous cardiovascular disease)
- Treatment
- Extended-release exenatide 2 mg subcutaneously once weekly, or placebo
- Follow-up
- Median follow-up 3.2 years
- Study design
- Randomized placebo-controlled cardiovascular outcome trial
- Funding
- not stated in the source
This is the largest safety dataset for the molecule, and it is a neutral cardiovascular result.
Read the original sourceNondiabetic obesity: 152 adults, 24 weeks, 5.1 kg versus 1.6 kg
Randomized controlled trial
Rosenstock J et al. Diabetes Care. 2010;33(6):1173-5. PMID 20332357.
The exenatide group lost 5.1 +/- 0.5 kg versus 1.6 +/- 0.5 kg on placebo (P<0.001), a placebo-subtracted difference of -3.3 +/- 0.5% of body weight. Both groups cut daily calories.
- Participants / model
- 152 obese adults without diabetes (mean age 46, 82% female, mean weight 108.6 kg, mean BMI 39.6; 25% with impaired glucose tolerance or impaired fasting glucose)
- Treatment
- Subcutaneous exenatide or placebo, plus lifestyle intervention
- Follow-up
- 24 weeks
- Study design
- Randomized trial
- Funding
- not stated in the source
This is the trial closest to the supplier's weight-loss claim, and it used the injectable.
Read the original sourceSearches, 9 October 2026: no human data for non-injected exenatide
PubMed search record
PubMed search run on 9 October 2026: exenatide AND (intranasal OR nasal), restricted to the humans MeSH term, 12 records. A second PubMed search for exenatide with sublingual, buccal, oral spray or aerosol returned 5 records. ClinicalTrials.gov queries run the same day.
The nasal search returned 12 records: reviews, rodent and ex vivo formulation work, one oral nanoparticle study and one adverse-event database review. None reported a human nasal exenatide dose. The second search returned 5 records: the rat and mouse route-comparison study, two reviews, an analytical chemistry paper and an inhaled microparticle study; none reported a human sublingual, buccal or oral-spray exenatide dose. On ClinicalTrials.gov, a query for intranasal exenatide returned no studies, and a query for sublingual exenatide returned 2 studies (NCT03010683 and NCT00353834), both of injected GLP-1 receptor agonists in vascular-function populations. No oral, sublingual, buccal or intranasal exenatide product has published human efficacy, pharmacokinetic or safety data among these records.
- Participants / model
- Records returned, not a population
- Treatment
- Not applicable
- Follow-up
- Searches run on 9 October 2026
- Study design
- Literature and registry searches
- Funding
- not stated in the source
A search result shows what the databases returned on that date. It is not proof that no unindexed study exists.
Read the original sourceRodent route comparison: sublingual 0.37% of intravenous in rats
Animal study
Gedulin BR et al. Int J Pharm. 2008;356(1-2):231-8. PMID 18291606.
In normoglycemic rats, bioavailability versus intravenous was 0.37% sublingual, 0.0053% intraduodenal, 1.68% nasal and up to 13.6% intratracheal, with similar elimination kinetics for every route (median ke 0.017 per minute). Glucose lowering was obtained in db/db mice by the nasal, intratracheal and high-dose aerosol routes. The authors concluded the intestinal tract has limited potential, with sublingual the most promising of the gastrointestinal routes, and that the respiratory tract is more viable.
- Participants / model
- Normoglycemic rats (pharmacokinetics) and diabetic db/db mice (glucose lowering)
- Treatment
- Sublingual, intraduodenal, nasal, intratracheal and aerosolized exenatide solutions
- Follow-up
- not stated in the source
- Study design
- Preclinical route comparison
- Funding
- not stated in the source
The only head-to-head route comparison found for exenatide, run by the originator. These are rodent numbers and do not transfer to people.
Read the original sourceNasal PYY3-36: 133 obese adults, 12 weeks, not efficacious
Randomized controlled trial
Gantz I et al. J Clin Endocrinol Metab. 2007;92(5):1754-7. PMID 17341568.
Completion was 38/43 (88%) on placebo, 31/44 (70%) at 200 mcg and 12/46 (26%) at 600 mcg, with 27 of 46 (59%) on 600 mcg stopping for nausea and vomiting. Mean weight change was -2.8, -3.7 and -1.4 kg across the three arms; the placebo versus 200 mcg difference was -0.9 kg (95% CI -2.6 to 0.7, P=0.251) against a sought difference of 2.11 kg. The published conclusion was that it is not efficacious.
- Participants / model
- 133 obese adults (BMI 30 to 43, age 18 to 65)
- Treatment
- Intranasal PYY3-36 spray, 200 or 600 mcg three times daily 20 minutes before meals, or placebo, with a hypocaloric diet
- Follow-up
- 12 weeks
- Study design
- Randomized placebo-controlled trial
- Funding
- not stated in the source
A different peptide by the same route, with the same dosing pattern, in the same kind of population as the supplier claim. It does not show what an exenatide spray would do.
Read the original sourceStudies and sources
PubChem: exenatide identity
Chemical identity record
National Library of Medicine. PubChem compound record CID 45588096 (exenatide).
Exenatide is synthetic exendin-4, a 39-residue peptide: PubChem CID 45588096, C184H282N50O60S, molecular weight 4187 g/mol, CAS 141758-74-9. Listed synonyms include Byetta, Bydureon, exendin-4 and AC2993.
- Participants / model
- Chemical identity, not a clinical population
- Treatment
- Defined peptide
- Follow-up
- Not applicable
- Study design
- NLM chemical record
- Funding
- not stated in the source
The molecule in every study on this page is the same peptide. Route and formulation differ, so a vendor spray is not the injectable product by sharing a name.
Read the original sourceBYETTA label, version effective 2 September 2025: indication, weight, PK, safety
FDA prescribing information
DailyMed, U.S. National Library of Medicine. BYETTA (exenatide) solution for subcutaneous injection, 5 and 10 mcg per dose, prescribing information, label version effective 2 September 2025. Set ID 53d03c03-ebf7-418d-88a8-533eabd2ee4f.
The label approves BYETTA as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It is not labeled for weight loss or obesity. Weight change was a secondary measure in the glycemic trials: placebo differences of -1.3 and -1.5 kg at 24 weeks, -1.1 and -2.4 kg at 30 weeks with metformin, and -4.5 kg versus insulin lispro. After a 10 mcg subcutaneous dose, median Tmax was 2.1 hours and mean terminal half-life 2.4 hours. In three 30-week placebo-controlled add-on trials (BYETTA n=963, placebo n=483), nausea occurred in 44% versus 18%. Warnings cover acute pancreatitis including fatal cases, hypoglycemia with insulin secretagogues or insulin, acute kidney injury, severe gastrointestinal reactions, immunogenicity, hypersensitivity, thrombocytopenia, acute gallbladder disease and pulmonary aspiration during general anesthesia or deep sedation.
- Participants / model
- Adults with type 2 diabetes; label PK participants
- Treatment
- BYETTA solution for subcutaneous injection, 5 and 10 mcg per dose
- Follow-up
- Label version effective 2 September 2025; label trials of 24 and 30 weeks
- Study design
- FDA prescribing information
- Funding
- not stated in the source
Weight results are secondary measures from glycemic trials. The twice-daily BYETTA label reviewed carries no boxed warning.
Read the original sourceDrugs@FDA: BYETTA 2005 and generic 2024 approval dates
Regulatory record
U.S. Food and Drug Administration. Drugs@FDA application record for NDA 021773 (BYETTA), with ANDA 206697 (Amneal). Dates read from the openFDA Drugs@FDA records on 9 October 2026.
FDA approved BYETTA under NDA 021773 on 28 April 2005. A synthetic exenatide injection from Amneal was approved under ANDA 206697 on 19 November 2024. Every approved US exenatide product in that record is an injection.
- Participants / model
- Not a clinical population
- Treatment
- Drug applications
- Follow-up
- Approvals in 2005 and 2024
- Study design
- FDA application records
- Funding
- not stated in the source
These records give approval dates; current marketing status is not stated here.
Read the original sourceDURATION-1: 295 patients, 30 weeks, HbA1c -1.9% versus -1.5%
Randomized controlled trial
Drucker DJ et al. Lancet. 2008;372(9645):1240-50. PMID 18782641.
HbA1c fell 1.9% once weekly versus 1.5% twice daily (95% CI -0.54 to -0.12, p=0.0023), with 77% versus 61% reaching HbA1c at or below 7.0% (p=0.0039). The authors reported similar bodyweight reductions in both arms.
- Participants / model
- 295 patients with type 2 diabetes (baseline HbA1c 8.3%, weight 102 kg)
- Treatment
- Subcutaneous exenatide: once-weekly 2 mg long-acting release versus 10 mcg twice daily
- Follow-up
- 30 weeks
- Study design
- Randomized open-label non-inferiority trial
- Funding
- not stated in the source
Both arms were subcutaneous injections. The study was open-label.
Read the original sourceEXSCEL: 14,752 patients, median 3.2 years, neutral cardiovascular result
Randomized controlled trial
Holman RR et al. N Engl J Med. 2017;377(13):1228-1239. PMID 28910237.
The primary composite of cardiovascular death, nonfatal myocardial infarction or nonfatal stroke occurred in 11.4% versus 12.2% (hazard ratio 0.91, 95% CI 0.83 to 1.00): noninferior for safety (P<0.001) but not superior for efficacy (P=0.06). Rates of acute pancreatitis, pancreatic cancer, medullary thyroid carcinoma and serious adverse events did not differ significantly.
- Participants / model
- 14,752 adults with type 2 diabetes (73.1% with previous cardiovascular disease)
- Treatment
- Extended-release exenatide 2 mg subcutaneously once weekly, or placebo
- Follow-up
- Median follow-up 3.2 years
- Study design
- Randomized placebo-controlled cardiovascular outcome trial
- Funding
- not stated in the source
This is the largest safety dataset for the molecule, and it is a neutral cardiovascular result.
Read the original sourceNondiabetic obesity: 152 adults, 24 weeks, 5.1 kg versus 1.6 kg
Randomized controlled trial
Rosenstock J et al. Diabetes Care. 2010;33(6):1173-5. PMID 20332357.
The exenatide group lost 5.1 +/- 0.5 kg versus 1.6 +/- 0.5 kg on placebo (P<0.001), a placebo-subtracted difference of -3.3 +/- 0.5% of body weight. Both groups cut daily calories.
- Participants / model
- 152 obese adults without diabetes (mean age 46, 82% female, mean weight 108.6 kg, mean BMI 39.6; 25% with impaired glucose tolerance or impaired fasting glucose)
- Treatment
- Subcutaneous exenatide or placebo, plus lifestyle intervention
- Follow-up
- 24 weeks
- Study design
- Randomized trial
- Funding
- not stated in the source
This is the trial closest to the supplier's weight-loss claim, and it used the injectable.
Read the original sourceRodent route comparison: sublingual 0.37% of intravenous in rats
Animal study
Gedulin BR et al. Int J Pharm. 2008;356(1-2):231-8. PMID 18291606.
In normoglycemic rats, bioavailability versus intravenous was 0.37% sublingual, 0.0053% intraduodenal, 1.68% nasal and up to 13.6% intratracheal, with similar elimination kinetics for every route (median ke 0.017 per minute). Glucose lowering was obtained in db/db mice by the nasal, intratracheal and high-dose aerosol routes. The authors concluded the intestinal tract has limited potential, with sublingual the most promising of the gastrointestinal routes, and that the respiratory tract is more viable.
- Participants / model
- Normoglycemic rats (pharmacokinetics) and diabetic db/db mice (glucose lowering)
- Treatment
- Sublingual, intraduodenal, nasal, intratracheal and aerosolized exenatide solutions
- Follow-up
- not stated in the source
- Study design
- Preclinical route comparison
- Funding
- not stated in the source
The only head-to-head route comparison found for exenatide, run by the originator. These are rodent numbers and do not transfer to people.
Read the original sourceNasal native GLP-1: 26 patients, 2 weeks, different compound
Clinical trial
Ueno H et al. Diabetes Care. 2014;37(7):2024-7. PMID 24667460.
Peak plasma active GLP-1 was 47.2 pmol/L with Tmax 8.1 min. Early-phase insulin secretion recovered, glucagon was suppressed and glycoalbumin fell significantly. The authors reported no marked adverse events, called the study exploratory and said long-term use needs evaluation.
- Participants / model
- 26 Japanese patients with type 2 diabetes
- Treatment
- Nasal compound containing 1.2 mg human GLP-1(7-36)amide, or placebo, before every meal
- Follow-up
- 2 weeks
- Study design
- Placebo-controlled clinical trial
- Funding
- not stated in the source
This is native GLP-1, not exenatide. The abstract reports no bioavailability figure and no weight outcome.
Read the original sourceNasal PYY3-36: 133 obese adults, 12 weeks, not efficacious
Randomized controlled trial
Gantz I et al. J Clin Endocrinol Metab. 2007;92(5):1754-7. PMID 17341568.
Completion was 38/43 (88%) on placebo, 31/44 (70%) at 200 mcg and 12/46 (26%) at 600 mcg, with 27 of 46 (59%) on 600 mcg stopping for nausea and vomiting. Mean weight change was -2.8, -3.7 and -1.4 kg across the three arms; the placebo versus 200 mcg difference was -0.9 kg (95% CI -2.6 to 0.7, P=0.251) against a sought difference of 2.11 kg. The published conclusion was that it is not efficacious.
- Participants / model
- 133 obese adults (BMI 30 to 43, age 18 to 65)
- Treatment
- Intranasal PYY3-36 spray, 200 or 600 mcg three times daily 20 minutes before meals, or placebo, with a hypocaloric diet
- Follow-up
- 12 weeks
- Study design
- Randomized placebo-controlled trial
- Funding
- not stated in the source
A different peptide by the same route, with the same dosing pattern, in the same kind of population as the supplier claim. It does not show what an exenatide spray would do.
Read the original sourceExenatide assay paper: beagle dogs, no nasal bioavailability stated
Animal study
Sauter M et al. J Pharm Anal. 2020;10(3):233-239. PMID 32612869.
The assay has a lower limit of quantification of 5 pg/mL (1.2 pM) in 200 microlitres of plasma. Its applicability was shown by quantifying exenatide after intravenous and nasal administration to beagle dogs. The abstract states no nasal bioavailability, Cmax or Tmax value.
- Participants / model
- Beagle dogs (applicability demonstration); human plasma (assay validation)
- Treatment
- Intravenous and nasal exenatide
- Follow-up
- not stated in the source
- Study design
- Bioanalytical method validation
- Funding
- not stated in the source
A secondary source attributed a specific nasal bioavailability figure to this paper. The abstract does not contain one, so none is carried onto this page.
Read the original sourceSearches, 9 October 2026: no human data for non-injected exenatide
PubMed search record
PubMed search run on 9 October 2026: exenatide AND (intranasal OR nasal), restricted to the humans MeSH term, 12 records. A second PubMed search for exenatide with sublingual, buccal, oral spray or aerosol returned 5 records. ClinicalTrials.gov queries run the same day.
The nasal search returned 12 records: reviews, rodent and ex vivo formulation work, one oral nanoparticle study and one adverse-event database review. None reported a human nasal exenatide dose. The second search returned 5 records: the rat and mouse route-comparison study, two reviews, an analytical chemistry paper and an inhaled microparticle study; none reported a human sublingual, buccal or oral-spray exenatide dose. On ClinicalTrials.gov, a query for intranasal exenatide returned no studies, and a query for sublingual exenatide returned 2 studies (NCT03010683 and NCT00353834), both of injected GLP-1 receptor agonists in vascular-function populations. No oral, sublingual, buccal or intranasal exenatide product has published human efficacy, pharmacokinetic or safety data among these records.
- Participants / model
- Records returned, not a population
- Treatment
- Not applicable
- Follow-up
- Searches run on 9 October 2026
- Study design
- Literature and registry searches
- Funding
- not stated in the source
A search result shows what the databases returned on that date. It is not proof that no unindexed study exists.
Read the original sourceWhy is Exenatide in A tier?
A fits an approved drug promoted for an off-label use. The injected form has a 2005 FDA approval, a 2024 generic approval, randomized trials in type 2 diabetes and a 14,752-patient cardiovascular outcome trial. The weight-loss spray sellers describe is off-label and untested: it had no published human data in the searches run on 9 October 2026.