Last reviewed 2026-04-20 · How we verify

Byetta (EXENATIDE)

Byetta works by mimicking the action of a natural hormone in the body to regulate blood sugar levels.

Byetta (Exenatide) is a GLP-1 Receptor Agonist developed by AstraZeneca AB, targeting the glucagon-like peptide 1 receptor to treat Type 2 Diabetes Mellitus as an adjunct therapy. It was FDA approved in 2005 and remains under the ownership of AstraZeneca AB. Byetta is a small molecule modality with off-patent status, allowing generic manufacturers to produce the drug. As an adjunct therapy, Byetta is used in conjunction with diet and exercise to improve glycemic control. Key safety considerations include potential gastrointestinal side effects.

At a glance

Mechanism of action

Incretins, such as glucagon-like peptide-1 (GLP-1), enhance glucose-dependent insulin secretion and exhibit other antihyperglycemic actions following their release into the circulation from the gut. BYETTA is GLP-1 receptor agonist that enhances glucose-dependent insulin secretion by the pancreatic beta-cell, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying.The amino acid sequence of exenatide partially overlaps that of human GLP-1. Exenatide has been shown to bind and activate the human GLP-1 receptor in vitro. This leads to an increase in both glucose-dependent synthesis of insulin, and in vivo secretion of insulin from pancreatic beta cells, by mechanisms involving cyclic AMP and/or other intracellular signaling pathways.BYETTA improves glycemic control by reducing fasting and postprandial glucose concentrations in patients with type diabetes through the actions described below.

Approved indications

• Type 2 Diabetes Mellitus Treatment Adjunct

Common side effects

• Hypoglycemia
• Nausea
• Diarrhea
• Vomiting
• Feeling jittery
• Dizziness
• Headache
• Dyspepsia
• Constipation
• Asthenia
• Bleeding
• Increased international normalized ratio (INR)

Drug interactions

• ciprofloxacin
• gatifloxacin
• levofloxacin
• norfloxacin
• ofloxacin

Key clinical trials

• Targeting Agonists of Glucagon-like Peptide-1 Receptor for Multiple Sclerosis (PHASE2)
• Exenatide for Smoking Cessation and Prevention of Weight Gain (PHASE2)
• A Pan-European Post-Authorisation Safety Study: Risk of Pancreatic Cancer Among Type 2 Diabetes Patients Who Initiated Exenatide as Compared With Those Who Initiated Other Non-Glucagon-Like Peptide 1 Receptor Agonists Based Glucose Lowering Drugs
• Exenatide For Reducing the Reinforcing Effects of Cocaine (PHASE1)
• GLP-1 Analogue in Preventing Progression of Small Vessel Disease (GAPP-SVD) (PHASE2)
• Extended Release Exenatide Versus Placebo In Diabetic Patients With Type 4 Cardiorenal Syndrome (PHASE3)
• Identification and Clinical Relevance of an Oxytocin Deficient State (GLP1 Study) (PHASE4)
• A Single-Center, Open-Label, Single Ascending Dose Study of Exenatide Circular RNA-Lipid Nanoparticle Injection (CR059) in Chinese Subjects With Type 2 Diabetes Mellitus (EARLY_PHASE1)

Primary sources

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