Exenatide

Dosing from the Literature

Published for fat loss: trial doses of 5–10 µg twice a day or 2 mg once a week, for 5 to 52 weeks, in adults and in adolescents aged 10 to 19 with overweight or obesity; in a 24-week trial of 152 adults without diabetes, 5.1 kg lost against 1.6 kg on placebo. Not published: a weight-loss dose on any label read for this page; all are for type 2 diabetes.

The table gives the doses as the labels and trials gave them, all injected under the skin. The label doses are for type 2 diabetes; the weight trials used the same two schedules. They are not recommendations.

What It Is

Exenatide is the synthetic form of exendin-4, a peptide of 39 amino acids with an amidated end (HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2), formula C184H282N50O60S, molecular weight 4186.6 Da (Byetta label). A Veterans Affairs research laboratory in the Bronx, New York, reported isolating exendin-4 from the venom of the Gila monster, Heloderma suspectum, in 1992 (Eng et al., 1992). It is 53% similar in sequence to GLP-1, a hormone the gut releases after meals (Young et al., 1999), and it acts on the same receptor (Göke et al., 1993). GLP-1 itself is broken down quickly by the enzyme dipeptidyl peptidase IV (DPP-4); the much greater stability of exendin-4 is what led to its testing as a diabetes drug (Furman, 2012). Its development code was AC2993 (Kolterman et al., 2003).

Amylin Pharmaceuticals developed it, with Eli Lilly as its partner (Kolterman et al., 2003; Buse et al., 2011). FDA approved Byetta, a twice-daily pen, on April 28, 2005, as a new molecular entity, and in a second application on October 30, 2009, for use with diet and exercise as the only diabetes drug (Drugs@FDA). Exenatide was the first drug of the GLP-1 receptor agonist class (Lundkvist et al., 2017). The once-weekly Bydureon, which releases exenatide from polymer microspheres, followed on January 27, 2012, and the Bydureon BCise autoinjector on October 20, 2017 (Drugs@FDA; Bydureon BCise label). The European Union authorised Byetta in 2006 and Bydureon in 2011 (EMA, 2026). An implanted mini-pump that releases exenatide for months, Intarcia Therapeutics’ ITCA 650, was refused by FDA in 2024 because its developer had not shown that it was safe; FDA’s reviewers had found more acute kidney injury on it than on placebo, and data suggesting a possible rise in major cardiovascular events (Federal Register, 2024).

The brand-name products are no longer marketed. AstraZeneca, the applicant on record for Byetta’s first application and for Bydureon and Bydureon BCise (Drugs@FDA), told FDA that these products were no longer marketed and asked it to withdraw their approvals; FDA did so as of September 3, 2025, and listed the two Bydureon applications as withdrawn again as of April 8, 2026 (Federal Register, 2025; Federal Register, 2026). A second Byetta application, NDA 021919, approved in 2009, is in neither notice and is still listed with prescription status (Drugs@FDA). The European Commission withdrew the EU authorisations of Byetta and Bydureon on January 1, 2026, at the request of AstraZeneca, which had decided to stop marketing them for commercial reasons (EMA, 2026). In the US, a generic twice-daily pen from Amneal, approved November 19, 2024, is listed with prescription status (Drugs@FDA; Amneal exenatide label).

PubMed returns 4,525 records for “exenatide” (searched October 4, 2026); 1,287 have the word in the title, and 309 of those are tagged as randomized controlled trials. Another 750 records name exendin-4 but not exenatide (searched October 4, 2026).

Mechanism of Action

The receptor work below comes from rodent cells and tissue (Göke et al., 1993); the effects on insulin, glucagon, stomach emptying and eating were measured in people (Kolterman et al., 2003; Linnebjerg et al., 2008; Basolo et al., 2018); the brain findings come from rats (Harkavyi et al., 2008).

• GLP-1 receptor (GLP-1R) — In rat insulin-secreting cells and isolated rat islets, exendin-4 displaced GLP-1 from its receptor, raised cyclic AMP and increased glucose-induced insulin release, and a shortened fragment, exendin-(9-39), reduced these effects (Göke et al., 1993). The label states that exenatide binds and activates the human GLP-1 receptor in vitro and that its sequence partly overlaps human GLP-1 (Byetta label).
• Resistance to DPP-4 breakdown — GLP-1 is broken down rapidly by DPP-4; exendin-4 is far more stable (Furman, 2012). In diabetic db/db mice it was 5,530 times as potent as GLP-1 at lowering glucose at one hour, and its effect lasted more than 4 hours where GLP-1’s vanished within an hour at most doses (Young et al., 1999). In people with type 2 diabetes, a 10 µg injection peaks at 2.1 hours, has a half-life of 2.4 hours and stays measurable for about 10 hours; the label states that it is cleared mainly by the kidneys (Byetta label).
• Insulin and glucagon, mainly when glucose is high — In people with type 2 diabetes, injections lowered fasting and after-meal glucose and after-meal glucagon; the authors attribute the fasting effect to glucose-dependent insulin release and lower glucagon, and the after-meal effect also to slower stomach emptying (Kolterman et al., 2003). The label states that it does not impair the normal glucagon response to low blood sugar (Byetta label).
• Slower stomach emptying — In 17 people with type 2 diabetes, over 5-day periods, 10 µg twice a day lengthened the time for half of a solid meal to leave the stomach from 60 to 169 minutes (111 minutes on 5 µg), and the two doses cut after-meal glucose (6-hour area under the curve) by 69–76% against placebo (Linnebjerg et al., 2008).
• Eating less — In healthy volunteers, an infusion of exendin-4 into a vein cut the calories eaten at a buffet lunch by 19% (Edwards et al., 2001). In 80 adults with obesity, in an inpatient vending-machine test in the first days, food intake fell by 1,016 kcal a day on 10 µg twice a day against 245 kcal on placebo, leaving them 367 kcal a day below the calories needed to keep weight steady, against 8 kcal on placebo; 24-hour energy expenditure did not differ, and at 24 weeks, in the 30 people measured, intake no longer differed (Basolo et al., 2018).
• Weekly release from microspheres — In the weekly forms, exenatide sits in microspheres of a lactide–glycolide polymer; with 2 mg a week, blood levels build up over about 10 weeks to about 208 pg/mL and generally fall below 20 pg/mL, the lowest level the assay measures, about 10 weeks after the last dose (Bydureon BCise label).
• Antibodies to exenatide — In the label’s 30-week trials, 38% of patients had low-titer antibodies and 6% higher titers at 30 weeks; in 3% of patients overall, antibodies came with a weaker glucose response (Byetta label).
• Dopamine neurons (a hypothesis) — In rats with toxin-induced damage to dopamine neurons, exendin-4 given into the abdomen from a week after the toxin raised striatal dopamine and reduced drug-induced circling (Harkavyi et al., 2008). The Parkinson’s trials were built on such animal findings (Athauda et al., 2017); the Phase 3 found no effect (Vijiaratnam et al., 2025).

What the Research Shows

The results below come from animals. The human trials are in the next section.

• Blood sugar and weight in diabetic animals — In a study from Amylin Pharmaceuticals, its developer, exendin-4 lowered glucose in db/db and ob/ob mice at doses thousands of times smaller than GLP-1; in diabetic rhesus monkeys it sped glucose lowering by up to 37%; in diabetic fatty Zucker rats injected under the skin twice a day for 5–6 weeks, HbA1c fell, weight fell, and insulin sensitivity rose by up to 49% (Young et al., 1999).
• Food intake and fat in rats — In Zucker fatty rats, once-daily injections cut food intake for about 5 days before it caught up; twice-daily injections, 56 days of treatment in all, kept food intake and weight gain lower, with less fat under the skin on MRI at 4 weeks and less visceral fat at 8 weeks (Szayna et al., 2000).
• Parkinson’s models — In rats with 6-OHDA or LPS lesions, 0.1 or 0.5 µg/kg into the abdomen twice a day for seven days, starting a week after the toxin, reduced drug-induced circling, raised striatal dopamine and preserved tyrosine hydroxylase staining in the substantia nigra (Harkavyi et al., 2008).
• The pancreas: two rat studies disagree — In 20 male rats, 10 of them given exendin-4 for 75 days, the treated rats had more pancreatic acinar inflammation and higher serum lipase (Nachnani et al., 2010). A study from Amylin Pharmaceuticals, its developer, found that exenatide did not change amylase or lipase in normal or diabetic rodents and lessened chemically induced pancreatitis at its highest doses (Tatarkiewicz et al., 2010).
• Thyroid C-cells in rats — In the twice-daily product’s 104-week study, rats were injected under the skin with 18, 70 or 250 µg/kg a day, and benign thyroid C-cell adenomas appeared in females at all doses (14%, 11% and 23%, against 8% and 5% in two control groups); mice given the same doses showed no tumours (Byetta label). The extended-release form raised C-cell adenomas and carcinomas at all doses in a 2-year rat study, at 2 to 27 times human exposure (Bydureon BCise label).

Human Data

Published: the placebo-controlled diabetes trials behind the labels, a cardiovascular outcomes trial, the randomized weight trials below, and trials in Parkinson’s disease and alcohol use disorder. PubMed lists 309 records with exenatide in the title tagged as randomized controlled trials (searched October 4, 2026). The main ones:

• Diabetes, twice a day (the label’s trials) — In three 30-week placebo-controlled trials in 1,446 adults whose diabetes was not controlled on metformin, a sulfonylurea or both, 10 µg twice a day lowered HbA1c 0.9 to 1.0 points more than placebo and weight 0.7 to 2.4 kg more (Byetta label; DeFronzo et al., 2005; Buse et al., 2004; Kendall et al., 2005). As the only diabetes drug for 24 weeks, it lowered HbA1c 0.7 points and weight 1.5 kg more than placebo (Byetta label).
• Diabetes, once a week — In DURATION-1, in 295 people with type 2 diabetes, 2 mg once a week lowered HbA1c more than 10 µg twice a day at 30 weeks (1.9 against 1.5 points), with similar weight loss (Drucker et al., 2008). In a 28-week trial of 375 adults, the BCise autoinjector lowered HbA1c more than Byetta (1.39 against 1.03 points), with weight losses of 1.4 and 1.9 kg (Bydureon BCise label). In 82 young people aged 10 to 17 with type 2 diabetes, weekly exenatide lowered HbA1c more than placebo over 24 weeks; weight changed by −0.17 kg against +0.88 kg (Bydureon BCise label).
• Three years, no control group (Klonoff et al., 2008) — 217 patients who completed three years of open-label twice-daily exenatide had lost 5.3 kg on average; the authors name the lack of a placebo group as the study’s main limitation.
• Heart outcomes: EXSCEL (Holman et al., 2017) — 14,752 people with type 2 diabetes, 73.1% with earlier cardiovascular disease, were followed for a median 3.2 years on weekly exenatide or placebo. A cardiovascular death, nonfatal heart attack or nonfatal stroke occurred in 11.4% against 12.2% (hazard ratio 0.91, 95% CI 0.83 to 1.00): noninferior to placebo for safety, not superior (P = 0.06). Weight averaged 1.27 kg lower on exenatide.
• Obesity without diabetes (Rosenstock et al., 2010) — 152 adults, 82% of them women, mean BMI 39.6, took 10 µg twice a day or placebo with a lifestyle program for 24 weeks: 5.1 kg lost against 1.6 kg, a placebo-subtracted 3.5 kg, or 3.3% of body weight. Impaired glucose tolerance or fasting glucose returned to normal in 77% against 56%. Nausea affected 25% against 4%. Eli Lilly and Amylin supported the trial, and four of its authors were their employees (Rosenstock et al., 2010).
• Obesity without diabetes (Dushay et al., 2012) — 41 women, two 16-week crossover periods, no lifestyle program: 2.49 kg lost on exenatide against 0.43 kg gained on placebo. Responses varied: 30% lost at least 5% of their weight, and 31% gained weight.
• Obesity without diabetes (Basolo et al., 2018) — 80 adults on 10 µg twice a day or placebo for 5 weeks (24 weeks for a subset enrolled before a 2012 protocol change): in the first days, in an inpatient vending-machine test, food intake fell by 1,016 kcal a day against 245 kcal; at 5 weeks weight was 1.48 kg lower than on placebo (P = 0.06), though it had fallen faster on exenatide (P = 0.02); at 24 weeks, in 13 against 20 people, it was 1.72 kg lower (P = 0.39).
• Against a low-calorie diet (Rodgers et al., 2021) — 182 women with overweight or obesity and no diabetes were randomized, 127 to exenatide, 5 µg twice a day for 2 weeks, then 10 µg (NCT01590433), and 55 to placebo injections with a low-calorie diet; the exenatide group was not put on a low-calorie diet. 40% of each group dropped out before week 12. At 12 weeks, in the 75 and 33 who remained, weight had fallen 6.5% on exenatide against 7.5% on the diet (P < 0.05), the registry’s posted primary result (NCT01590433), and 56% against 76% had lost at least 5% (P = 0.05). Women who had lost 5% stayed on for up to 52 weeks, and their peak weight loss was similar (11.65 kg on exenatide, 11.91 kg on the diet). Nausea affected 70% against 25%.
• Adolescents (Kelly et al., 2013) — 26 adolescents aged 12 to 19 with severe obesity, 3 months with lifestyle counseling: BMI fell 2.70% more and weight 3.26 kg more than on placebo; 22 completed. Nausea affected 62% against 31%.
• Adolescents, weekly (Weghuber et al., 2020) — 44 adolescents aged 10 to 18 with obesity, 2 mg a week with a lifestyle intervention for 6 months: 3 kg more weight lost than on placebo, and BMI-SDS, the main outcome, 0.09 lower than on placebo (95% CI −0.18 to 0.00), with no significant change in liver fat.
• Adolescents, keeping weight off (Fox et al., 2022) — 100 adolescents with severe obesity began a meal-replacement diet; the 66 who cut their BMI by at least 5% (mean age 16) were randomized to 2 mg a week or placebo for 52 weeks, with lifestyle therapy. BMI rose 4.6% on exenatide and 10.1% on placebo (NCT02496611); the main outcome, the adjusted difference of −4.1 percentage points (95% CI −8.6 to 0.5), was not significant (P = 0.078). A 2023 correction to the paper could not be read for this page.
• Hypothalamic obesity (Roth et al., 2021) — 42 people aged 10 to 25 with obesity after hypothalamic injury from a brain tumour, 2 mg a week for 36 weeks: the change in BMI did not differ significantly from placebo (−1.7%, P = .40), but body fat fell 3.1 kg more and waist 3.5 cm more.
• Craniopharyngioma (Gatta-Cherifi et al., 2024) — Adults with obesity after craniopharyngioma, at 11 French university hospitals, 26 weeks of twice-daily exenatide or placebo with intensive lifestyle measures: 3.8 kg against 1.6 kg lost, an adjusted difference of 3.1 kg that was not significant (P = 0.11). Adverse events affected 95% against 70%.
• Schizophrenia, on antipsychotics (Ishøy et al., 2017) — 45 adults with obesity and no diabetes, 2 mg a week for 3 months: 2.24 kg against 2.23 kg lost (P = .98). A 2018 erratum corrected the paper’s secondary metabolic analyses; the authors state the weight result was unaffected.
• On clozapine, open-label (Siskind et al., 2018) — 28 adults with schizophrenia and obesity, weekly exenatide or routine care for 24 weeks: 5.29 kg against 1.12 kg lost; 6 of 14 against 1 of 14 lost more than 5%.
• On olanzapine (Patino et al., 2025) — Adults with overweight or obesity and a mood or psychotic disorder, 16 weeks: 0.5 kg lost on exenatide against 2.6 kg gained on placebo.
• With dapagliflozin (Lundkvist et al., 2017) — 50 adults with obesity and no diabetes took dapagliflozin 10 mg a day plus exenatide 2 mg a week, or placebo, for 24 weeks: 4.13 kg more weight lost on the pair, and 36.0% against 4.2% lost at least 5%.
• Parkinson’s disease, two early trials — In a trial in which patients knew their treatment and only the raters, scoring from video, were blinded (open-label in the registry, single-blind in the paper), 45 people were randomized to exenatide or no added treatment for 12 months: scores on the MDS-UPDRS rating scale were 2.7 points better on exenatide against 2.2 points worse in controls (Aviles-Olmos et al., 2013); the registered dose was 5 µg twice a day for a month, then 10 µg twice a day (NCT01174810). In a double-blind trial in 62 people, 2 mg a week for 48 weeks left off-medication motor scores 3.5 points better than placebo at 60 weeks (Athauda et al., 2017).
• Parkinson’s disease, Phase 3 (Vijiaratnam et al., 2025) — 194 people at six UK hospitals, 2 mg a week or placebo for 96 weeks (NCT04232969): off-medication motor scores worsened 5.7 points on exenatide and 4.5 on placebo (P = 0.47), no evidence of slowed disease. Serious adverse events affected 9% against 11%. All three Parkinson’s trials on this page were led by one group at University College London, with Foltynie as senior author (Aviles-Olmos et al., 2013; Athauda et al., 2017; Vijiaratnam et al., 2025; NCT01174810; NCT01971242; NCT04232969).
• An expression of concern — In June 2026 The Lancet published an expression of concern about the Phase 3 paper (The Editors of The Lancet, 2026). A news report quotes the notice: a regulatory inspection at King’s College Hospital, one of the trial’s sites, found “department-wide concerns relating to trial conduct, oversight and governance, including findings classified by regulators as critical and major,” and the expression of concern stands pending the hospital trust’s investigations and an assessment of whether the findings could affect the study’s data or conclusions (Chipman, 2026).
• Alcohol use disorder (Klausen et al., 2022) — 127 patients seeking treatment, 2 mg a week with cognitive-behavioral therapy for 26 weeks: heavy drinking days did not fall significantly more than on placebo; in an exploratory analysis they did in patients with a BMI above 30.
• Registered, no results posted — A Phase 3 of weekly exenatide or placebo, both with family-based behavioral treatment, in children aged 10 to 12 with obesity reached primary completion in August 2025 (NCT04520490), and a single-dose study in gestational diabetes in December 2025 (NCT05482789); neither had posted results by October 5, 2026 (ClinicalTrials.gov).

The evidence meter on the Exenatide card reads “Controlled trials”: it rates published human data for fat loss, and exenatide is approved for blood sugar in type 2 diabetes, not for weight (Byetta label). Placebo-controlled weight trials in people without diabetes are published (Rosenstock et al., 2010; Kelly et al., 2013; Weghuber et al., 2020); a 52-week trial in adolescents missed significance (Fox et al., 2022), a low-calorie diet did slightly better in one trial (Rodgers et al., 2021), and several trials in special groups found no significant difference (Roth et al., 2021; Ishøy et al., 2017; Gatta-Cherifi et al., 2024).

Reconstitution & Storage

There is nothing to reconstitute in the twice-daily form: Byetta and the generic come as a ready solution of 250 µg/mL in a prefilled pen, 1.2 mL for 60 doses of 5 µg or 2.4 mL for 60 doses of 10 µg, 30 days of twice-daily doses (Byetta label; Amneal exenatide label).

• Storage on the labels — Refrigeration at 2–8 °C before first use; after first use, up to 25 °C; no freezing; protection from light; the pen discarded 30 days after first use (Byetta label; Amneal exenatide label).
• The weekly autoinjector — Bydureon BCise held 2 mg in 0.85 mL, as microspheres in an oil-based vehicle of medium-chain triglycerides, mixed inside the device just before the injection (Bydureon BCise label). Its label lists storage flat in the refrigerator, with up to 4 weeks at room temperature not above 30 °C (Bydureon BCise label). Its approval has been withdrawn (Federal Register, 2026).
• Laboratory powder — Laboratory suppliers list exenatide as freeze-dried powder, 1 mg to 50 mg, labelled for research use only and not for human consumption (supplier catalogues, searched October 4, 2026). No label or trial document read for this page describes a dose or preparation of such powder for people.

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Side Effects & Risks

• Stomach and gut — In the label’s three 30-week trials, nausea occurred in 44% on twice-daily exenatide against 18% on placebo, vomiting in 13% against 4% and diarrhea in 13% against 6%; nausea led 3% to stop (Byetta label). On the weekly autoinjector, injection-site nodules (10.5%) and nausea (8.2%) were the most common reactions (Bydureon BCise label). In adults with obesity and no diabetes, nausea affected 25% against 4% (Rosenstock et al., 2010); in adolescents, 62% against 31% (Kelly et al., 2013).
• Low blood sugar — With a sulfonylurea, hypoglycemia occurred in 35.7% on 10 µg twice a day against 3.3% on placebo; as the only diabetes drug, in 3.8% against 1.3% (Byetta label). The label warns of a higher risk with insulin or insulin secretagogues (Byetta label).
• Pancreatitis and cancers — The labels report acute pancreatitis, including fatal hemorrhagic or necrotizing cases, with GLP-1 receptor agonists including exenatide (Byetta label). In EXSCEL, confirmed acute pancreatitis occurred in 26 people on exenatide and 22 on placebo, pancreatic cancer in 15 and 16, medullary thyroid carcinoma in 2 and 1 (all three with raised calcitonin at baseline), and papillary thyroid cancer in 10 and 4 (Holman et al., 2017).
• Kidneys — The label reports acute kidney injury after approval, some cases needing dialysis, mostly after nausea, vomiting or diarrhea led to dehydration; it advises against the twice-daily form when creatinine clearance is below 30 mL/min or in end-stage kidney disease (Byetta label). FDA refused the implanted exenatide pump ITCA 650 in 2024; its reviewers had found more acute kidney injury on it than on placebo (Federal Register, 2024).
• Platelets — Drug-induced immune thrombocytopenia, in which exenatide-dependent antibodies destroy platelets, has been reported after approval with serious bleeding, which may be fatal; a history of it is a contraindication, and with the weekly form low platelets can persist for about 10 weeks after the last dose (Byetta label; Bydureon BCise label).
• Gallbladder — In EXSCEL, 1.9% on exenatide and 1.4% on placebo reported an acute gallbladder event such as gallstones or cholecystitis (Bydureon BCise label).
• Allergy and injection sites — Anaphylaxis and angioedema have been reported after approval (Byetta label); with the weekly form, serious injection-site reactions such as abscess, cellulitis and necrosis, a few needing surgery (Bydureon BCise label).
• Heart rate — In the weekly autoinjector’s adult trials, heart rate rose by 2.4 beats per minute on average (Bydureon BCise label).
• Anaesthesia — Rare reports of pulmonary aspiration under general anaesthesia or deep sedation in people taking GLP-1 receptor agonists who had food left in the stomach despite fasting (Byetta label).
• Pregnancy — Human data are too limited to judge the risk; in mice, exenatide during pregnancy and nursing increased newborn deaths at 3 times the human exposure (Byetta label).
• Other drugs — Slower stomach emptying delays drugs taken by mouth: acetaminophen peak levels fell 37–56% when taken with or up to 4 hours after a 10 µg dose (Byetta label). Higher INR, sometimes with bleeding, has been reported with warfarin after approval (Byetta label).
• In the Parkinson’s Phase 3 — Over 96 weeks, serious adverse events affected 9% on exenatide and 11% on placebo (Vijiaratnam et al., 2025).
• WADA — Exenatide is not named on the 2026 Prohibited List, and the List names no GLP-1 drug (World Anti-Doping Agency, 2026). Class S0 covers substances “with no current approval by any governmental regulatory health authority for human therapeutic use”; exenatide is approved in the US (Drugs@FDA), so S0 does not apply. It is not prohibited.

Bloodwork & Monitoring

What the labels describe, and what the trials measured:

• Glucose and HbA1c — The labels’ trials measured HbA1c and fasting glucose, and the label links worsening glucose control in some patients to antibodies against exenatide (Byetta label).
• Kidney function — The label calls for kidney function to be checked in patients with side effects that can cause fluid loss, especially when the drug is started or the dose raised (Byetta label).
• INR with warfarin — The label calls for frequent INR checks until stable when exenatide is started or changed in patients taking warfarin (Byetta label).
• Calcitonin and thyroid ultrasound — The weekly form’s label calls routine calcitonin or thyroid ultrasound monitoring of uncertain value for finding medullary thyroid carcinoma early (Bydureon BCise label).
• Platelets and gallbladder — The labels describe stopping exenatide if drug-induced thrombocytopenia is suspected, and gallbladder studies if gallstones or cholecystitis are suspected (Byetta label).
• What the weight trials measured — Weight, BMI, waist, body fat by DXA, glucose tolerance and lipids (Rosenstock et al., 2010; Roth et al., 2021; Weghuber et al., 2020); a three-year open-label extension of the diabetes trials also tracked liver enzymes (Klonoff et al., 2008).
• Which tests fit a given person — A question for a licensed healthcare provider. This page can’t answer it.

Commonly Stacked With

Exenatide has been tested on top of other diabetes drugs and lifestyle programs, and with dapagliflozin in obesity without diabetes. No human study has tested it with pramlintide, BPC-157, thymosin beta-4, tesamorelin, ipamorelin, sermorelin or CJC-1295 (PubMed, searched October 4, 2026).

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Legal Status

Related Compounds

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Next Steps

References

1. AstraZeneca Pharmaceuticals LP. BYETTA (exenatide) injection, for subcutaneous use. Prescribing information and Medication Guide (revised September 2025; initial U.S. approval 2005). DailyMed set ID 53d03c03-ebf7-418d-88a8-533eabd2ee4f, SPL version 26 (effective September 2, 2025). dailymed.nlm.nih.gov. Read October 4, 2026.
2. Amneal Pharmaceuticals LLC. Exenatide injection, for subcutaneous use (ANDA 206697). Prescribing information (initial U.S. approval 2005). DailyMed set ID e6cb5c8f-e97f-4a6a-95a4-939fd2393949, SPL version 17 (effective May 27, 2026; published June 30, 2026). dailymed.nlm.nih.gov. Read October 4, 2026.
3. AstraZeneca. BYDUREON BCISE (exenatide) extended-release injectable suspension, for subcutaneous use. Prescribing information (revised May 2025; FDA reference ID 5598377). accessdata.fda.gov/drugsatfda_docs/label/2025/209210s025lbl.pdf. Read October 4, 2026.
4. FDA. Drugs@FDA through openFDA (api.fda.gov/drug/drugsfda.json, data of October 2, 2026), searched for exenatide: NDA 021773, BYETTA (AstraZeneca AB; approved April 28, 2005, new molecular entity; discontinued); NDA 021919, BYETTA (Amylin; approved October 30, 2009, as an adjunct to diet and exercise; prescription); NDA 022200, BYDUREON and BYDUREON PEN (AstraZeneca AB; approved January 27, 2012; discontinued); NDA 209210, BYDUREON BCISE (AstraZeneca AB; approved October 20, 2017; discontinued); ANDA 206697, exenatide synthetic injection (Amneal; approved November 19, 2024; prescription; therapeutic equivalence code AP). FDA approval letter for NDA 21-919 and NDA 21-773 supplements, to Amylin Pharmaceuticals, 2009: accessdata.fda.gov/drugsatfda_docs/appletter/2009/021773s009s011s017s018s022s025021919ltr.pdf. Read October 4, 2026.
5. FDA. Teva Branded Pharmaceutical Products R&D, Inc., et al.; Withdrawal of Approval of 39 New Drug Applications. Federal Register. 2025;90(147):36440-36441 (FR Doc. 2025-14683, August 4, 2025): NDA 021773 (Byetta), NDA 022200 (Bydureon, Bydureon Pen) and NDA 209210 (Bydureon BCise), AstraZeneca AB, withdrawn as of September 3, 2025, at the applicants’ request because the products were no longer marketed. A correction of October 3, 2025 (90 FR 48056) concerns another application. federalregister.gov. Read October 4, 2026.
6. FDA. Aspen Global Inc. c/o Lachman Consultant Services, Inc., et al.; Withdrawal of Approval of 46 New Drug Applications. Federal Register. 2026;91(45):11321-11323 (FR Doc. 2026-04546, March 9, 2026): NDA 022200 (Bydureon, Bydureon Pen) and NDA 209210 (Bydureon BCise), AstraZeneca Pharmaceuticals LP, withdrawn as of April 8, 2026. federalregister.gov. Read October 4, 2026.
7. FDA. Final Decision on the Proposal To Refuse To Approve a New Drug Application for ITCA 650. Federal Register. 2024;89(164):68168-68177 (FR Doc. 2024-18898, August 23, 2024): Intarcia Therapeutics’ NDA 209053, exenatide in DUROS device. federalregister.gov. Read October 4, 2026.
8. European Medicines Agency (EMA). Byetta (exenatide): authorised in the EU November 20, 2006; marketing authorisation withdrawn January 1, 2026 at the request of AstraZeneca AB, which had decided “to permanently discontinue the marketing of the product for commercial reasons” (ema.europa.eu/en/medicines/human/EPAR/byetta). Bydureon (exenatide): authorised June 17, 2011; withdrawn January 1, 2026 for the same reason (ema.europa.eu/en/medicines/human/EPAR/bydureon). Read October 4, 2026.
9. PMDA (Pharmaceuticals and Medical Devices Agency, Japan). List of Approved Products, New Drugs: April 2004 to February 2026 (“List of Approved Drugs”), entries for exenatide: October 27, 2010, Byetta Subcutaneous Injection 5 μg Pen 300, 10 μg Pen 600 and 10 μg Pen 300 (Eli Lilly Japan K.K.), a drug with a new active ingredient for type 2 diabetes in patients who had not responded sufficiently to a sulfonylurea (alone or with a biguanide or a thiazolidinedione) with diet and exercise; March 30, 2012, Bydureon for Subcutaneous Injection 2 mg (Eli Lilly Japan K.K.), a drug with a new additional indication and a new dosage in a new dosage form for the treatment of type 2 diabetes mellitus. pmda.go.jp/files/000281190.pdf. Read October 5, 2026.
10. FDA. Import Alert 66-80: Detention Without Physical Examination of Glucagon-Like Peptide-1 (GLP-1) Receptor Agonist Bulk Drug Substances (published date September 21, 2026); exenatide among its product codes, with exenatide makers in Belgium and India on its green list. accessdata.fda.gov/CMS_IA/importalert_1186.html. Read October 4, 2026.
11. Eng J, Kleinman WA, Singh L, Singh G, Raufman JP. Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom. Further evidence for an exendin receptor on dispersed acini from guinea pig pancreas. J Biol Chem. 1992;267(11):7402-7405. PMID: 1313797.
12. Göke R, Fehmann HC, Linn T, et al. Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting beta-cells. J Biol Chem. 1993;268(26):19650-19655. PMID: 8396143.
13. Young AA, Gedulin BR, Bhavsar S, et al. Glucose-lowering and insulin-sensitizing actions of exendin-4: studies in obese diabetic (ob/ob, db/db) mice, diabetic fatty Zucker rats, and diabetic rhesus monkeys (Macaca mulatta). Diabetes. 1999;48(5):1026-1034. PMID: 10331407. DOI: 10.2337/diabetes.48.5.1026.
14. Szayna M, Doyle ME, Betkey JA, et al. Exendin-4 decelerates food intake, weight gain, and fat deposition in Zucker rats. Endocrinology. 2000;141(6):1936-1941. PMID: 10830274. DOI: 10.1210/endo.141.6.7490.
15. Edwards CM, Stanley SA, Davis R, et al. Exendin-4 reduces fasting and postprandial glucose and decreases energy intake in healthy volunteers. Am J Physiol Endocrinol Metab. 2001;281(1):E155-E161. PMID: 11404233. DOI: 10.1152/ajpendo.2001.281.1.E155.
16. Kolterman OG, Buse JB, Fineman MS, et al. Synthetic exendin-4 (exenatide) significantly reduces postprandial and fasting plasma glucose in subjects with type 2 diabetes. J Clin Endocrinol Metab. 2003;88(7):3082-3089. PMID: 12843147. DOI: 10.1210/jc.2002-021545.
17. Linnebjerg H, Park S, Kothare PA, et al. Effect of exenatide on gastric emptying and relationship to postprandial glycemia in type 2 diabetes. Regul Pept. 2008;151(1-3):123-129. PMID: 18675854. DOI: 10.1016/j.regpep.2008.07.003.
18. Furman BL. The development of Byetta (exenatide) from the venom of the Gila monster as an anti-diabetic agent. Toxicon. 2012;59(4):464-471. PMID: 21194543. DOI: 10.1016/j.toxicon.2010.12.016.
19. Harkavyi A, Abuirmeileh A, Lever R, et al. Glucagon-like peptide 1 receptor stimulation reverses key deficits in distinct rodent models of Parkinson's disease. J Neuroinflammation. 2008;5:19. PMID: 18492290. DOI: 10.1186/1742-2094-5-19.
20. Nachnani JS, Bulchandani DG, Nookala A, et al. Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreas. Diabetologia. 2010;53(1):153-159. PMID: 19756486. DOI: 10.1007/s00125-009-1515-4.
21. Tatarkiewicz K, Smith PA, Sablan EJ, et al. Exenatide does not evoke pancreatitis and attenuates chemically induced pancreatitis in normal and diabetic rodents. Am J Physiol Endocrinol Metab. 2010;299(6):E1076-E1086. PMID: 20923958. DOI: 10.1152/ajpendo.00479.2010.
22. Buse JB, Henry RR, Han J, et al. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes. Diabetes Care. 2004;27(11):2628-2635. PMID: 15504997. DOI: 10.2337/diacare.27.11.2628.
23. DeFronzo RA, Ratner RE, Han J, et al. Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes. Diabetes Care. 2005;28(5):1092-1100. PMID: 15855572. DOI: 10.2337/diacare.28.5.1092.
24. Kendall DM, Riddle MC, Rosenstock J, et al. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in patients with type 2 diabetes treated with metformin and a sulfonylurea. Diabetes Care. 2005;28(5):1083-1091. PMID: 15855571. DOI: 10.2337/diacare.28.5.1083.
25. Klonoff DC, Buse JB, Nielsen LL, et al. Exenatide effects on diabetes, obesity, cardiovascular risk factors and hepatic biomarkers in patients with type 2 diabetes treated for at least 3 years. Curr Med Res Opin. 2008;24(1):275-286. PMID: 18053320. DOI: 10.1185/030079908x253870.
26. Drucker DJ, Buse JB, Taylor K, et al. Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study. Lancet. 2008;372(9645):1240-1250. PMID: 18782641. DOI: 10.1016/S0140-6736(08)61206-4.
27. Buse JB, Rosenstock J, Sesti G, et al. Liraglutide once a day versus exenatide twice a day for type 2 diabetes: a 26-week randomised, parallel-group, multinational, open-label trial (LEAD-6). Lancet. 2009;374(9683):39-47. PMID: 19515413. DOI: 10.1016/S0140-6736(09)60659-0.
28. Buse JB, Bergenstal RM, Glass LC, et al. Use of twice-daily exenatide in Basal insulin-treated patients with type 2 diabetes: a randomized, controlled trial. Ann Intern Med. 2011;154(2):103-112. PMID: 21138825. DOI: 10.7326/0003-4819-154-2-201101180-00300.
29. Buse JB, Nauck M, Forst T, et al. Exenatide once weekly versus liraglutide once daily in patients with type 2 diabetes (DURATION-6): a randomised, open-label study. Lancet. 2013;381(9861):117-124. PMID: 23141817. DOI: 10.1016/S0140-6736(12)61267-7.
30. Wysham C, Blevins T, Arakaki R, et al. Efficacy and safety of dulaglutide added onto pioglitazone and metformin versus exenatide in type 2 diabetes in a randomized controlled trial (AWARD-1). Diabetes Care. 2014;37(8):2159-2167. PMID: 24879836. DOI: 10.2337/dc13-2760.
31. Holman RR, Bethel MA, Mentz RJ, et al. Effects of Once-Weekly Exenatide on Cardiovascular Outcomes in Type 2 Diabetes. N Engl J Med. 2017;377(13):1228-1239. PMID: 28910237. DOI: 10.1056/NEJMoa1612917.
32. Ahmann AJ, Capehorn M, Charpentier G, et al. Efficacy and Safety of Once-Weekly Semaglutide Versus Exenatide ER in Subjects With Type 2 Diabetes (SUSTAIN 3): A 56-Week, Open-Label, Randomized Clinical Trial. Diabetes Care. 2018;41(2):258-266. PMID: 29246950. DOI: 10.2337/dc17-0417. (Funder: Novo Nordisk A/S, in the publisher’s Crossref record; sponsor in the registry, NCT01885208.)
33. Rosenstock J, Klaff LJ, Schwartz S, et al. Effects of exenatide and lifestyle modification on body weight and glucose tolerance in obese subjects with and without pre-diabetes. Diabetes Care. 2010;33(6):1173-1175. PMID: 20332357. DOI: 10.2337/dc09-1203.
34. Apovian CM, Bergenstal RM, Cuddihy RM, et al. Effects of exenatide combined with lifestyle modification in patients with type 2 diabetes. Am J Med. 2010;123(5):468.e9-468.e17. PMID: 20399326. DOI: 10.1016/j.amjmed.2009.11.019.
35. Dushay J, Gao C, Gopalakrishnan GS, et al. Short-term exenatide treatment leads to significant weight loss in a subset of obese women without diabetes. Diabetes Care. 2012;35(1):4-11. PMID: 22040840. DOI: 10.2337/dc11-0931.
36. Kelly AS, Rudser KD, Nathan BM, et al. The effect of glucagon-like peptide-1 receptor agonist therapy on body mass index in adolescents with severe obesity: a randomized, placebo-controlled, clinical trial. JAMA Pediatr. 2013;167(4):355-360. PMID: 23380890. DOI: 10.1001/jamapediatrics.2013.1045.
37. Lundkvist P, Sjöström CD, Amini S, et al. Dapagliflozin once-daily and exenatide once-weekly dual therapy: A 24-week randomized, placebo-controlled, phase II study examining effects on body weight and prediabetes in obese adults without diabetes. Diabetes Obes Metab. 2017;19(1):49-60. PMID: 27550386. DOI: 10.1111/dom.12779. (Full text at PMC5215525: “Exenatide, the first‐in‐class GLP‐1RA.”)
38. Ishøy PL, Knop FK, Broberg BV, et al. Effect of GLP-1 receptor agonist treatment on body weight in obese antipsychotic-treated patients with schizophrenia: a randomized, placebo-controlled trial. Diabetes Obes Metab. 2017;19(2):162-171. PMID: 27717222. DOI: 10.1111/dom.12795. (Erratum in Diabetes Obes Metab. 2018;20(5):1327-1328: corrected secondary metabolic analyses; “the error did not influence the results of the primary endpoint.”)
39. Siskind DJ, Russell AW, Gamble C, et al. Treatment of clozapine-associated obesity and diabetes with exenatide in adults with schizophrenia: A randomized controlled trial (CODEX). Diabetes Obes Metab. 2018;20(4):1050-1055. PMID: 29194917. DOI: 10.1111/dom.13167.
40. Basolo A, Burkholder J, Osgood K, et al. Exenatide has a pronounced effect on energy intake but not energy expenditure in non-diabetic subjects with obesity: A randomized, double-blind, placebo-controlled trial. Metabolism. 2018;85:116-125. PMID: 29596853. DOI: 10.1016/j.metabol.2018.03.017.
41. Rodgers M, Migdal AL, Rodríguez TG, et al. Weight Loss Outcomes Among Early High Responders to Exenatide Treatment: A Randomized, Placebo Controlled Study in Overweight and Obese Women. Front Endocrinol (Lausanne). 2021;12:742873. PMID: 34867786. DOI: 10.3389/fendo.2021.742873.
42. Weghuber D, Forslund A, Ahlström H, et al. A 6-month randomized, double-blind, placebo-controlled trial of weekly exenatide in adolescents with obesity. Pediatr Obes. 2020;15(7):e12624. PMID: 32062862. DOI: 10.1111/ijpo.12624.
43. Fox CK, Clark JM, Rudser KD, et al. Exenatide for weight-loss maintenance in adolescents with severe obesity: A randomized, placebo-controlled trial. Obesity (Silver Spring). 2022;30(5):1105-1115. PMID: 35403350. DOI: 10.1002/oby.23395. (A correction appeared in Obesity (Silver Spring) 2023;31(9):2440; the publisher’s page could not be read for this page.)
44. Roth CL, Perez FA, Whitlock KB, et al. A phase 3 randomized clinical trial using a once-weekly glucagon-like peptide-1 receptor agonist in adolescents and young adults with hypothalamic obesity. Diabetes Obes Metab. 2021;23(2):363-373. PMID: 33026160. DOI: 10.1111/dom.14224.
45. Gatta-Cherifi B, Mohammedi K, Cariou T, et al. Impact of exenatide on weight loss and eating behavior in adults with craniopharyngioma-related obesity: the CRANIOEXE randomized placebo-controlled trial. Eur J Endocrinol. 2024;190(4):257-265. PMID: 38450721. DOI: 10.1093/ejendo/lvae024.
46. Patino LR, Strawn JR, Adler CM, et al. A double-blind, placebo-controlled trial of exenatide for the treatment of olanzapine-related weight gain in obese and overweight adults. J Affect Disord. 2025;382:116-122. PMID: 40203970. DOI: 10.1016/j.jad.2025.04.046.
47. Aviles-Olmos I, Dickson J, Kefalopoulou Z, et al. Exenatide and the treatment of patients with Parkinson's disease. J Clin Invest. 2013;123(6):2730-2736. PMID: 23728174. DOI: 10.1172/JCI68295.
48. Athauda D, Maclagan K, Skene SS, et al. Exenatide once weekly versus placebo in Parkinson's disease: a randomised, double-blind, placebo-controlled trial. Lancet. 2017;390(10103):1664-1675. PMID: 28781108. DOI: 10.1016/S0140-6736(17)31585-4.
49. Vijiaratnam N, Girges C, Auld G, et al. Exenatide once a week versus placebo as a potential disease-modifying treatment for people with Parkinson's disease in the UK: a phase 3, multicentre, double-blind, parallel-group, randomised, placebo-controlled trial. Lancet. 2025;405(10479):627-636. PMID: 39919773. DOI: 10.1016/S0140-6736(24)02808-3.
50. The Editors of The Lancet. Expression of Concern: Exenatide once a week versus placebo as a potential disease-modifying treatment for people with Parkinson's disease in the UK: a phase 3, multicentre, double-blind, parallel-group, randomised, placebo-controlled trial. Lancet. 2026;407(10548):2588. PMID: 42330995. DOI: 10.1016/S0140-6736(26)01241-9. (Behind a paywall; its wording on this page is quoted from the news report below.)
51. Chipman A. Lancet issues ‘Expression of Concern’ on exenatide trial. The Limbic, July 2, 2026. thelimbic.com/?p=20669549. Read October 4, 2026.
52. Klausen MK, Jensen ME, Møller M, et al. Exenatide once weekly for alcohol use disorder investigated in a randomized, placebo-controlled clinical trial. JCI Insight. 2022;7(19):e159863. PMID: 36066977. DOI: 10.1172/jci.insight.159863.
53. ClinicalTrials.gov. Registrations cited on this page: NCT01174810 (Parkinson’s pilot, “An Open Label, Single Site, 12 Month, Phase II, Randomised Controlled Trial”; University College London; exenatide 5 µg twice a day for 1 month, then 10 µg twice a day for 11 months; status unknown), NCT01971242 (Parkinson’s, double-blind, single centre; University College London; completed), NCT04232969 (Exenatide-PD3; University College London; 194 enrolled; completed July 31, 2024; no results posted), NCT01590433 (exenatide against placebo injections with a low-calorie diet in women without diabetes; collaborator AstraZeneca; 249 consented, 182 started treatment, 127 on exenatide and 55 on placebo; posted primary result, change in body weight at 12 weeks: 6.5% on exenatide, n = 75, against 7.5% on placebo, n = 33, P < 0.05), NCT02496611 (exenatide extended-release for keeping weight off in adolescents; posted primary result, BMI change from randomization to week 52: +4.6% on exenatide, n = 33, against +10.1% on placebo, n = 33), NCT01064687 (AWARD-1; sponsor Eli Lilly and Company; begun February 2010; exenatide 5 µg twice a day for 4 weeks, then 10 µg twice a day, in patients on metformin and pioglitazone), NCT01885208 (SUSTAIN 3; sponsor Novo Nordisk A/S), NCT00308139 (DURATION-1; sponsor now listed as AstraZeneca; study code 2993LAR-105; begun April 2006, primary completion July 2008), NCT02860923 (CRANIOEXE; 42 enrolled; 5 µg twice a day for 4 weeks, then 10 µg twice a day for 5 months), NCT00845507 (olanzapine-related weight gain; sponsor University of Cincinnati, collaborator Eli Lilly and Company; begun December 2008; 54 enrolled; 5 µg twice a day for 28 days, then 10 µg as tolerated), NCT05356104 (GAPP-SVD, recruiting; weekly exenatide or semaglutide against standard therapy; primary completion estimated May 2027), NCT04520490 (BASIC2; Phase 3; Seattle Children’s Hospital; exenatide 2 mg or placebo once a week for 24 weeks, both arms with family-based behavioral treatment, in children aged 10 to 12 with obesity; active, not recruiting; primary completion August 21, 2025; no results posted), NCT05482789 (Phase 4 pilot in gestational diabetes; a single 10 µg dose; still listed as recruiting; primary completion December 31, 2025; no results posted), NCT07497399 (TAG-MS; NLY01, a pegylated exenatide; recruiting). clinicaltrials.gov, API v2. Read October 4–5, 2026.
54. Code of Federal Regulations. 21 CFR 216.23, Bulk drug substances that can be used to compound drug products in accordance with section 503A of the Federal Food, Drug, and Cosmetic Act; and 21 CFR 216.24, drug products withdrawn or removed from the market for reasons of safety or effectiveness. ecfr.gov. Read October 4, 2026.
55. 21 U.S.C. 353a, Pharmacy compounding (section 503A of the Federal Food, Drug, and Cosmetic Act), subsection (b)(1). law.cornell.edu/uscode/text/21/353a. Read October 5, 2026.
56. FDA. Bulk Drug Substances Nominated for Use in Compounding Under Section 503A of the Federal Food, Drug, and Cosmetic Act (categories 1–3). Updated May 14, 2026. fda.gov/media/94155/download.
57. FDA. Bulk Drug Substances Nominated for Use in Compounding Under Section 503B of the Federal Food, Drug, and Cosmetic Act (categories 1–3). Updated March 21, 2025. fda.gov/media/94164/download.
58. World Anti-Doping Agency. Prohibited List 2026 (in effect January 1, 2026). S0, Non-approved substances. wada-ama.org.
59. Searches of October 4, 2026: PubMed, “exenatide” (4,525 records; 1,287 with exenatide in the title, 309 of them tagged as randomized controlled trials), “exendin-4 NOT exenatide” (750 records); PubMed, exenatide with pramlintide, BPC-157, thymosin, tesamorelin, ipamorelin, sermorelin or CJC-1295 (no human study of a combination) and tirzepatide with exenatide (no randomized trial); ClinicalTrials.gov, “exenatide” (408 records; the active ones that give exenatide itself are listed above), “exendin” and “Byetta”; Drugs@FDA, “exenatide” (five applications); DailyMed, “exenatide” (three labels); Federal Register, “exenatide” (14 documents) and “Bydureon” (5); laboratory-supplier catalogues listing exenatide powder for research use only (suppliers not named). Searches of October 5, 2026: PMDA’s list of approved new drugs, April 2004 to February 2026 (Byetta, 2010; Bydureon, 2012); the funding statements and registry sponsors of the trials named in the research-limits box (Crossref and Europe PMC funder records; ClinicalTrials.gov); ClinicalTrials.gov, NCT04520490, NCT05482789 and NCT05356104 rechecked.

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