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DPP-4 inhibitor (sitagliptin)
Sitagliptin inhibits dipeptidyl peptidase-4 (DPP-4), an enzyme that breaks down incretin hormones, thereby increasing insulin secretion and reducing glucagon in response to meals.
Sitagliptin inhibits dipeptidyl peptidase-4 (DPP-4), an enzyme that breaks down incretin hormones, thereby increasing insulin secretion and reducing glucagon in response to meals. Used for Type 2 diabetes mellitus.
At a glance
| Generic name | DPP-4 inhibitor (sitagliptin) |
|---|---|
| Also known as | Sitagliptin |
| Sponsor | GRADE Study Group |
| Drug class | DPP-4 inhibitor |
| Target | DPP-4 (dipeptidyl peptidase-4) |
| Modality | Small molecule |
| Therapeutic area | Diabetes |
| Phase | Phase 3 |
Mechanism of action
DPP-4 inhibitors work by blocking the degradation of GLP-1 and GIP, incretin hormones that regulate postprandial glucose levels. By prolonging the activity of these hormones, sitagliptin enhances glucose-dependent insulin secretion and suppresses glucagon secretion, leading to improved glycemic control in type 2 diabetes without causing hypoglycemia when used as monotherapy.
Approved indications
- Type 2 diabetes mellitus
Common side effects
- Nasopharyngitis
- Headache
- Upper respiratory tract infection
- Hypoglycemia (when combined with other agents)
Key clinical trials
- Dose Optimization of Sitagliptin and Duloxetine in Diabetic Cirrhosis (PHASE4)
- Comparative Study Between (SGLT-2i) and (DPP-4i) in the Prevention of DIC (PHASE4)
- Impact of Pharmacogenetic-Guided Treatment on Type 2 Diabetes. (PHASE4)
- A Comparative Effectiveness Study of Major Glycemia-lowering Medications for Treatment of Type 2 Diabetes (PHASE3)
- Triple Hypoglycemic Regimens In Patients With Newly Diagnosed Type 2 Diabetes Mellitus (PHASE1, PHASE2)
- Anti-Diabetic Medications to Fight PD and LBD (PHASE4)
- Neoadjuvant Chemotherapy, Anti-PD-1 Antibody and Sitagliptin for Locally Advanced pMMR CRC (PHASE1, PHASE2)
- Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study
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:
- DPP-4 inhibitor (sitagliptin) CI brief — competitive landscape report
- DPP-4 inhibitor (sitagliptin) updates RSS · CI watch RSS
- GRADE Study Group portfolio CI