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exenatide and sitagliptin
This combination drug stimulates insulin secretion through two complementary pathways: exenatide activates GLP-1 receptors to enhance glucose-dependent insulin release, while sitagliptin inhibits DPP-4 to prolong the action of endogenous GLP-1 and GIP.
This combination drug stimulates insulin secretion through two complementary pathways: exenatide activates GLP-1 receptors to enhance glucose-dependent insulin release, while sitagliptin inhibits DPP-4 to prolong the action of endogenous GLP-1 and GIP. Used for Type 2 diabetes mellitus.
At a glance
| Generic name | exenatide and sitagliptin |
|---|---|
| Also known as | exenatide-Byetta; sitagliptin-Januvia |
| Sponsor | AstraZeneca |
| Drug class | GLP-1 receptor agonist and DPP-4 inhibitor combination |
| Target | GLP-1 receptor (exenatide); DPP-4 (sitagliptin) |
| Modality | Small molecule |
| Therapeutic area | Diabetes |
| Phase | FDA-approved |
Mechanism of action
Exenatide is a GLP-1 receptor agonist that mimics glucagon-like peptide-1, promoting insulin secretion in response to elevated blood glucose and slowing gastric emptying. Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that prevents the degradation of endogenous incretin hormones (GLP-1 and GIP), thereby extending their glucose-lowering effects. Together, they provide synergistic glycemic control in type 2 diabetes.
Approved indications
- Type 2 diabetes mellitus
Common side effects
- Nausea
- Vomiting
- Diarrhea
- Headache
- Hypoglycemia
- Injection site reactions
Key clinical trials
- Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study
- Using Secondary Data to Evaluate Sex-based Heterogeneity of GLP-1 Agonists and SGLT2 Inhibitors on Cardiovascular-Kidney-Metabolic Health (CKMH) Outcomes in Real-world Settings (DASH-CKMH)
- A Study for Comparison of Canagliflozin Versus Alternative Antihyperglycemic Treatments on Risk of Heart Failure Hospitalization and Amputation for Participants With Type 2 Diabetes Mellitus and the Subpopulation With Established Cardiovascular Disease
- Real-World Evaluation of Omarigliptin for Type 2 Diabetes Meliitus in Bangladesh (PHASE4)
- BESTMED: Observational Evaluation of Second Line Therapy Medications in Diabetes
- Pathophysiological Study of the Increase in Pancreatic Volume in Type 2 Diabetes Treatments. (NA)
- Effect of Exenatide, Sitagliptin or Glimepiride on Functional ß -Cell Mass (NA)
- A Comparison of Two Treatment Strategies in Older Participants With Type 2 Diabetes Mellitus (T2DM) (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- exenatide and sitagliptin CI brief — competitive landscape report
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- AstraZeneca portfolio CI