Exenatide

Areas of active research — not promised effects

Each tag links to other compounds with research into that goal. Research use only: these are areas of study, not human-use claims.

Related by research scope · open each to compare

Exenatide remains a Schedule-uncontrolled prescription drug that requires physician authorization. However, both Byetta (twice-daily) and Bydureon BCise (once-weekly) were commercially withdrawn by AstraZeneca in October 2024 for business reasons. FDA-approved generic versions were not available as of early 2026, though compounded exenatide from 503A pharmacies may be obtainable under a valid prescription. Exenatide is not subject to the FDA-19 Category 2 peptide compounding restrictions that affect research-use peptides. As an approved drug, compounded versions from 503A/503B pharmacies are subject to FDA's drug shortage and clinical-need framework.

Transparent blend · bci-1.0 · never paid-placement

Primary name

Exenatide

Origin

Exenatide is a synthetic version of exendin-4, a 39-amino-acid peptide originally isolated from the venom of the Gila monster (Heloderma suspectum). It shares approximately 53% sequence homology with human glucagon-like peptide-1 (GLP-1) but is resistant to degradation by dipeptidyl peptidase-4 (DPP-4), conferring a longer duration of action than endogenous GLP-1. It was approved by the FDA as Byetta (twice-daily subcutaneous injection, 2005) and Bydureon (once-weekly microsphere formulation, 2012). AstraZeneca voluntarily withdrew all US-marketed formulations for business reasons; Byetta was discontinued in October 2024 and the last Bydureon BCise formulation in October 2024.

Registry IDs

PubChem CID

45588096

CAS

141758-74-9

InChIKey

HTQBXNHDCUEHJF-XWLPCZSASA-N

ChEMBL

CHEMBL414357

Molecular formula

C184H282N50O60S

Molar mass

4187 g/mol

Monoisotopic

4184.0273075 Da

InChIKey

HTQBXNHDCUEHJF-XWLPCZSASA-N

Appearance

White to off-white lyophilized powder (for reconstitution); pen-injector formulations used clear colorless solution

Solubility

Soluble in water and aqueous buffers; solubility is pH-dependent; isoelectric po…

Sequence not available in current seed.

Stability: Peptide is susceptible to thermal degradation and aggregation above 25°C; DPP-4 resistant in vivo due to amino acid substitutions at position 2 (Ala→Gly analogy

Vial sizes

null mg · null mg

Purity grades

pharmaceutical grade

Salt forms

Free base (primary)

• GHS hazard class on file
• PPE & spill response
• Disposal guidance
• Not-for-human-consumption posture

How much research exists, and of what maturity — never a verdict on whether it works.

Mechanism of action

• Exenatide binds and activates the GLP-1 receptor, a G-protein-coupled receptor (Gs-coupled), elevating intracellular cAMP and triggering glucose-dependent insulin secretion from pancreatic beta cells — importantly, this effect is attenuated as plasma glucose normalizes, reducing hypoglycemia risk compared with sulfonylureas
• Concurrently, exenatide suppresses inappropriate post-meal glucagon release from alpha cells and slows gastric emptying, both of which blunt postprandial glucose excursions
• Central and peripheral GLP-1 receptor signaling also reduces appetite and promotes satiety, contributing to the weight loss observed in treated patients
• Chronic administration has been associated in preclinical models with enhancement of beta-cell mass and improved insulin biosynthesis, although the clinical significance of beta-cell regeneration in humans remains under investigation

Pharmacokinetics (ADME)

Half-life

Immediate-release (Byetta): ~2.4 hours (subcutaneous). Extended-release microsphere (Bydureon): controlled release from PLGA microspheres; apparent terminal half-life ~2 weeks (release-rate limited, not elimination limited).

Clearance

Primarily renal; predominantly glomerular filtration followed by proteolytic degradation. Linear clearance estimated at ~5.1 L/hr in subjects with normal renal function. Dose adjustment required in moderate renal impairment; contraindicated in severe renal impairment (CrCl <30 mL/min) and end-stage renal disease.

PK–PD note: Peak plasma concentration after immediate-release subcutaneous dose reached in ~2.1 hours; mean apparent volume of distribution ~28 L. The extended-release formulation uses PLGA microsphere encapsulat…

Reading the evidence

• Evidence quality and gaps vary by application — see the cited grades above.
• Indexed-article counts span all evidence tiers, not only completed human trials.
• No first-party human-dosing, efficacy, or benefit claims are made here.

Key reviews & evidence-gap sources

• Norris SL et al. Exenatide efficacy and safety: a systematic review. Diabet Med. 2009;26(9):837-46 (PMID 19719703) — Anchoring systematic review; compared exenatide vs oral glucose-lowering agents/insulin.
• Nikfar S et al. Efficacy and tolerability of exenatide vs placebo: systematic review & meta-analysis of RCTs. J Pharm Pharm Sci. 2012;15(1):1-30 (PMID 22365085) — Meta-analysis of randomized clinical trials; reported significant HbA1c and fasting plasma glucose reductions.
• Network meta-analysis comparing exenatide QW vs other GLP-1 RAs in T2DM (PMC4801811) — NMA of GLP-1 receptor agonists at approved doses added to metformin.
• Exenatide for obesity in children and adolescents: systematic review and meta-analysis (Frontiers Pharmacology 2024; PMC11022205) — Pooled 5 RCTs in pediatric overweight/obesity without diabetes.
• Exenatide in obese/overweight patients without diabetes: systematic review & meta-analysis of RCTs (PMID 27343423) — 6 RCTs, 362 patients; weight loss MD -4.47 kg vs control.

5 registered trials — 1 currently recruiting.

Phase 2
NCT02794402
Double-blinded, 6 Months Study With Bydureon® or Placebo in Adolescents With Obesity to Explore Changes in BMI

COMPLETED

Phase 3
NCT04232969
Exenatide Once Weekly Over 2 Years as a Potential Disease Modifying Treatment for Parkinson's Disease

COMPLETED

Phase 1
NCT00612794
A Study to Examine Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Exenatide Once Weekly in Japanese Patients With Type 2 Diabetes

COMPLETED

Phase 4
NCT02288273
Study to Evaluate the Effect of BYDUREON on 24-hour Glucose Control in Metformin Treated Patients With Type 2 Diabetes.

COMPLETED

NA
NCT06256419
Association of Gene Polymorphism With Susceptibility to T2DM and the Therapeutic Responses to Exenatide in Chinese Patients With T2DM

RECRUITING

Summary (literature)

The most common adverse effects are gastrointestinal: nausea (occurring in 8–44% of patients depending on dose and formulation), vomiting, and diarrhea, typically mild to moderate and decreasing over time. Hypoglycemia is infrequent when exenatide is used as monotherapy (due to g…

WADA status

GLP-1 receptor agonists including exenatide are NOT listed on the WADA 2026 Prohibited List as prohibited substances. Semaglutide and tirzepatide are on the 202…

Dominant research route: Subcutaneous (SC)

Approved human route (Byetta BID immediate-release; Bydureon QW extended-release microspheres). Injection sites: abdomen, thigh, or upper arm. Population PK from 8 clinical trials.

Bioavailability: For SC administration, 37% of the dose is absorbed via a zero-order process and the remaining 63% via a nonlinear (Michaelis-Menten) pathway; peak concentrations ~2 h postdose; terminal half-life ~2.4 h; linear clearance ~5.06 L/h in normal renal function.

Dominant and only FDA-approved route. Byetta (IR, 5/10 mcg BID) approved April 28, 2005; Bydureon (ER, 2 mg once weekly) approved January 27, 2012. Both administered as SC injection.

Used as the reference route for bioavailability calculations in normoglycemic rats; also used in human IV infusion studies of glucose-dependent insulin secretion.

Bioavailability: IV served as the 100% bioavailability reference against which SC, oral, and respiratory routes were compared in rats; elimination kinetics similar across routes (median ke 0.017 min-1).

Not an approved/administered route; used experimentally as PK reference and in mechanistic glucose-clamp infusion studies.

Investigated in normoglycemic rats (intestinal epithelial delivery) and diabetic db/db mice; oral nanoparticle/microsphere formulations studied preclinically.

Bioavailability: Oral bioavailability markedly lower than SC; exenatide is DPP-IV resistant (Gly8 substitution) but susceptible to other GI proteases, requiring encapsulation/protease-inhibitor strategies to preserve bioactivity.

No approved oral exenatide product; oral delivery studied only preclinically. Oral-stability (protease susceptibility) is distinct from oral absorption.

Respiratory-tract (intranasal/intratracheal) delivery studied in normoglycemic rats and diabetic db/db mice.

Bioavailability: Respiratory-tract delivery compared favorably with the clinically approved SC route despite minimal formulation optimization; bioavailability favorable relative to other bioactive peptides.

Preclinical alternate-route exploration only; not an approved or marketed route.

Animal & human figures are kept visibly separate so studied animal doses are never misread as human guidance.

Sorted A–Z by vendor — never by price

Researched storefront prices, bucketed

p25 $18.38 · median $46.00 · p75 $90.00 · 6 researched vendors

Legit, COA-backed band: $11.03–$200.00/mg.

Value rule: don't just buy the cheapest — a price under $3/mg is a red flag. Pair price with COA and independent-test grade.

Estimated cost of research (10 mg)

Vial (best researched price)

$110

Bacteriostatic water (generic estimate)

$6

Syringes / supplies (generic estimate)

$12

What each test proves — general guidance, plus this compound's researched purity data

Independent labs cited for this compound

The only exenatide-specific recall identified was the September 2013 voluntary recall of ~92,000 vials of Bydureon (exenatide extended-release) in European countries for under-filled vials; no US FDA Class I/II recalls of exenatide products were found in the sources retrieved. No counterfeit-exenatide events were found (counterfeit GLP-1 enforcement has centered on semaglutide/Ozempic).

Buyer red-flag checklist

• Foreign-sourced GLP-1 APIs (including exenatide) are subject to FDA Import Alert 66-80 DWPE; 21% of 48 GLP-1 API sites FDA evaluated were noncompliant with CGMP.
• Compounded GLP-1 products are not evaluated by FDA for safety, efficacy, or quality; FDA has issued warning letters to compounders and telehealth companies over compounded GLP-1s.
• Cold-chain integrity is a key vulnerability for injectable compounded GLP-1s; shipments arriving warm or with inadequate ice packs may degrade product quality.
• Byetta (NDA 021773) marketing was discontinued (August 2024) and AstraZeneca has discontinued Bydureon BCise, creating supply-shortage conditions that can drive demand to unapproved/compounded sources.
• Acute pancreatitis (including fatal cases) is a recognized postmarketing adverse effect of exenatide; FDA added pancreatitis warnings to labeling.

GMP vs research-grade: the chemistry (SPPS + HPLC + MS) is identical — the difference is the quality system.

Underdosing / mislabeling: The 2013 Bydureon European recall involved under-filled vials (a fill-volume/underdosing defect) but no prevalence figure was published; no independent lab-test aggregate (Janoshik/MZ Biolabs/Finnrick) reporting exenatide-specific underdosing prevalence was found in the sources retrieved.

• Detention Without Physical Examination (DWPE) of Glucagon-Like Peptide-1 (GLP-1) Receptor Agonist Bulk Drug Substances, including exenatide (FDA Product Code 61P[][]75). FDA evaluated 48 GLP-1 API sites and found 21% noncompliant under section 501 of the FD&C Act. Foreign-sourced GLP-1 APIs may be detained unless the manufacturer appears on the Green List.66-80
• An RUO label is not an import exemption — CBP judges actual intended use.
• Lyophilized powder is ambient-stable in transit; temperature control needed for > 7-day transit.
• US-warehouse vendors dodge import scrutiny — they cost more but ship more reliably.

Every item dated & sourced

Not prohibited. USADA states GLP-1 agonists (including exenatide/Byetta) are not prohibited in sport; WADA is monitoring GLP-1 agonist use by athletes to determine future prohibition. No TUE required.

No granted patents identified in current seed. Composition-of-matter coverage is limited given the peptide's synthetic origin.

• IACUC / IRB research context
• RUO buyer responsibilities & documentation
• Veterinary / alternative-use where lawful
• Jurisdiction-aware "who may lawfully obtain"

What people discuss

Reported concerns — discussion, not established effects

Reading caveats

• self-selection bias in voluntary review platforms
• survivorship bias — many users switched to newer GLP-1 agents, leaving skewed residual discussion
• insurance-coverage changes conflate access frustration with drug-effectiveness sentiment

Manually researched from reddit, youtube— theme weights are research estimates, not live counts; aggregated & de-identified. No individual posts, quotes, or usernames are ever shown.

Relative research / market volume — populated once the activity stream is wired

Inline tooltips for lyophilized, RUO, EU/mg, SPPS, 503A and more.

Toggle plain-language ↔ scientific in the header.

• How to read a COA
• Free base vs acetate
• Understanding evidence grades

39-amino-acid GLP-1 receptor agonist derived from Gila monster exendin-4; FDA-approved for type 2 diabetes; both branded formulations withdrawn from US market by 2024. Approximately 4,401 articles are indexed (literature last scanned 2026-05-29). US regulatory status: Prescription drug (branded formulations withdrawn from market). Research use only.

Emitted as JSON-LD: ChemicalSubstance · BreadcrumbList · FAQPage.

• Price-drop & back-in-stock alerts
• Regulatory-change email digest
• Print / share this datasheet