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Sitagliptin + Metformin
Sitagliptin inhibits DPP-4 to increase incretin levels and insulin secretion, while metformin reduces hepatic glucose production and improves insulin sensitivity.
Sitagliptin inhibits DPP-4 to increase incretin levels and insulin secretion, while metformin reduces hepatic glucose production and improves insulin sensitivity. Used for Type 2 diabetes mellitus.
At a glance
| Generic name | Sitagliptin + Metformin |
|---|---|
| Also known as | Sitagliptin + Metformin = Janumet, janumet, MK0431A, Janumet™, Sitadin M |
| Sponsor | Baylor College of Medicine |
| Drug class | DPP-4 inhibitor + biguanide combination |
| Target | DPP-4 enzyme; metformin acts on multiple targets including mitochondrial complex I |
| Modality | Small molecule |
| Therapeutic area | Diabetes |
| Phase | FDA-approved |
Mechanism of action
Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that prolongs the action of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), thereby enhancing glucose-dependent insulin secretion and reducing glucagon levels. Metformin is a biguanide that decreases hepatic glucose production and increases peripheral glucose uptake and insulin sensitivity. Together, they provide complementary mechanisms for glycemic control in type 2 diabetes.
Approved indications
- Type 2 diabetes mellitus
Common side effects
- Hypoglycemia
- Gastrointestinal disturbance (nausea, diarrhea, abdominal pain)
- Headache
- Nasopharyngitis
- Lactic acidosis (rare, metformin-related)
Key clinical trials
- Comparative Effectiveness of Two Initial Combination Therapies in Patients With Recent Onset Diabetes (PHASE3)
- Metformin, Empagliflozin With Sitagliptin vs Linagliptin in Type 2 Diabetes (PHASE4)
- Effect of Dapagliflozin vs Sitagliptin on Liver Fat Accumulation and Body Composition in Patients With Diabetes Mellitus and Liver Transplantation (NA)
- Impact of Pharmacogenetic-Guided Treatment on Type 2 Diabetes. (PHASE4)
- Triple Hypoglycemic Regimens In Patients With Newly Diagnosed Type 2 Diabetes Mellitus (PHASE1, PHASE2)
- Evaluate the Efficacy and Safety of Empagliflozin or Glimepiride Combination Therapy in Type 2 Diabetes Mellitus Patients (PHASE4)
- iSGLT2 Inhibitor and a iDPP -4 Inhibitor in Treatment of Type 2 Diabetes Mellitus in Patients Treated With Metformin (TRIAD) (PHASE3)
- Canagliflozin and Myocardial Fibrosis (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:
- Sitagliptin + Metformin CI brief — competitive landscape report
- Sitagliptin + Metformin updates RSS · CI watch RSS
- Baylor College of Medicine portfolio CI