Last reviewed 2026-04-20 · How we verify

Byetta

Byetta works by activating the glucagon-like peptide 1 receptor, which helps regulate blood sugar levels.

Byetta is a GLP-1 Receptor Agonist, a small molecule developed by AstraZeneca AB, targeting the glucagon-like peptide 1 receptor. It was FDA-approved in 2005 for the treatment of Type 2 Diabetes Mellitus as an adjunct therapy. Byetta works by mimicking the action of the natural hormone GLP-1, which helps regulate blood sugar levels. It is still patented and commercially available. Key safety considerations include pancreatitis and thyroid C-cell tumors.

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
• Dyspepsia
• Diarrhea
• Vomiting
• Constipation
• Asthenia
• Dizziness
• Headache
• Feeling jittery

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)

Patents

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.