Exenatide
Also known as: AC-2993, Bydureon, Bydureon BCise, Byetta, Exenatide, Exendin-4 synthetic, Exendin‑4, LY2148568
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Summary
Exenatide is a synthetic analog of exendin‑4, administered subcutaneously for the treatment of type 2 diabetes mellitus. It improves glycaemic control and can promote modest weight loss.
Mechanism of Action
Mimics endogenous GLP‑1, binds to GLP‑1 receptors on pancreatic β‑cells to enhance glucose‑dependent insulin secretion, suppress glucagon, and slow gastric emptying.
Routes of Administration
Goals & Uses
- Blood pressure reductionCardiovascularModerate
- Cardiovascular risk reductionCardiovascularModerate
- Beta-cell function preservationMetabolicLow
- Weight reductionMetabolicModerate
- Glycemic control in type 2 diabetesMetabolicHigh
- Glycaemic controlDiabetesHigh
Contraindications
- Personal or family history of medullary thyroid carcinomaOncologicHigh
- Severe gastrointestinal diseaseGastrointestinalModerate
- Type 1 diabetes mellitus or diabetic ketoacidosisMetabolicHigh
- Multiple endocrine neoplasia type 2OncologyHigh
- Medullary thyroid carcinomaOncologyHigh
- Severe renal impairment (eGFR <30 mL/min/1.73m²)RenalHigh
- Multiple Endocrine Neoplasia syndrome type 2 (MEN 2)Genetic/EndocrineHigh
- History of hypersensitivity to exenatideImmunologicalHigh
Adverse Effects
- PancreatitisGastrointestinalRareInflammation of the pancreas
- HypoglycemiaMetabolicCommonAbnormally low blood glucose
- Injection site reactionsLocalCommon
- Hypoglycaemia (with sulfonylureas/insulin)MetabolicUncommon
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- VomitingGastrointestinalCommonForceful expulsion of stomach contents
- Acute pancreatitisGastrointestinalRare
- DiarrhoeaGastrointestinalCommon
- DiarrheaGastrointestinalCommonLoose or frequent stools
Drug Interactions
- Antibiotics (time-sensitive oral agents)Low
- Oral contraceptivesLowDelayed gastric emptying may affect absorption timing
- InsulinModerateMay increase risk of low blood sugar
- DPP‑4 inhibitorsLow
- WarfarinModerate
- SulfonylureasModerateMay increase risk of low blood sugar
Population Constraints
- PregnancyReproductive SafetyRelative
- Pediatric patientsAgeRelative
- Pediatrics (<18 y)AgeAbsolute
- Elderly patients (≥75 years)AgeRelative
- Moderate renal impairment (eGFR 30–50 mL/min/1.73m²)RenalRelative
- History of pancreatitisGastrointestinalRelative
Regulatory Status
- European UnionApprovedApproved: type 2 diabetes mellitusSame indications as US.
- United StatesApprovedApproved: type 2 diabetes mellitusByetta (twice‑daily) and Bydureon (once‑weekly) formulations.
- United KingdomApprovedApproved: Type 2 diabetes mellitus as adjunct to diet, exercise, and other antidiabetic agentsApproved via legacy EMA process; MHRA oversight post-Brexit. NICE guidance supports use in specific patient subgroups meeting BMI/HbA1c criteria.
Approved in the US and EU for type 2 diabetes; extended‑release formulation (Bydureon) offers weekly dosing. Not approved for obesity in the US.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Exenatide?
Exenatide is a synthetic analog of exendin‑4, administered subcutaneously for the treatment of type 2 diabetes mellitus. It improves glycaemic control and can promote modest weight loss.
What is Exenatide used for?
Exenatide is educationally associated with: Blood pressure reduction, Cardiovascular risk reduction, Beta-cell function preservation, Weight reduction, Glycemic control in type 2 diabetes, Glycaemic control. Educational only — not medical advice.
How is Exenatide administered?
Recorded routes of administration: Subcutaneous.
What are the potential side effects of Exenatide?
Reported adverse effects include: Pancreatitis, Hypoglycemia, Injection site reactions, Hypoglycaemia (with sulfonylureas/insulin), Nausea, Vomiting, Acute pancreatitis, Diarrhoea, Diarrhea. This list is not exhaustive — consult a qualified clinician.
Who should avoid Exenatide?
Recorded contraindications: Personal or family history of medullary thyroid carcinoma, Severe gastrointestinal disease, Type 1 diabetes mellitus or diabetic ketoacidosis, Multiple endocrine neoplasia type 2, Medullary thyroid carcinoma, Severe renal impairment (eGFR <30 mL/min/1.73m²), Multiple Endocrine Neoplasia syndrome type 2 (MEN 2), History of hypersensitivity to exenatide. Consult a qualified clinician before use.