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sitagliptin (MK0431)
sitagliptin (MK0431) is a DPP-4 inhibitor Small molecule drug developed by Merck Sharp & Dohme LLC. It is currently in Phase 3 development for Type 2 diabetes mellitus, Diabetic nephropathy. Also known as: MK0431, Januvia, sitagliptin phosphate.
Sitagliptin works by inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4), which is involved in the inactivation of incretin hormones.
Sitagliptin (MK0431) is a small molecule dipeptidyl peptidase IV inhibitor used to treat conditions such as Type 2 Diabetes and Type 1 Diabetes. It belongs to the drug class of inhibitors and is classified as a dipeptidyl peptidase 4 inhibitor.
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Baseline phase 3 → approval rate
+58.3pp
Industry-wide phase 3 drugs reach approval ~58.3% of the time (BIO/Informa 2023 industry benchmark across all therapeutic areas). -
Big-pharma sponsor
+3.0pp
Merck Sharp & Dohme LLC is a top-20 pharma sponsor — historical approval rates run ~3pp above average due to scale, regulatory experience, and trial-design quality.
| Regulator | Country | Likely year | Lag vs FDA |
|---|---|---|---|
| FDA | US | 2028–2030 | — |
| EMA | EU | 2029–2031 | +0.7 yr |
| MHRA | GB | 2029–2031 | +0.7 yr |
| Health Canada | CA | 2029–2032 | +0.9 yr |
| TGA | AU | 2029–2032 | +1.2 yr |
| PMDA | JP | 2029–2032 | +1.5 yr |
| NMPA | CN | 2030–2033 | +2.3 yr |
| MFDS | KR | 2029–2032 | +1.4 yr |
| CDSCO | IN | 2029–2033 | +1.8 yr |
| ANVISA | BR | 2030–2033 | +2.3 yr |
Hover any row for the lag rationale. Lag estimates are reduced when the drug has FDA Breakthrough or EMA PRIME designation (sponsors file globally in parallel).
Estimate based on the BIO/Informa industry phase transition rates plus per-drug modifiers for therapeutic area, sponsor type, FDA designations, mechanism, and trial design. Per-jurisdiction lags from Tufts CSDD international approval studies. Not investment, clinical or regulatory advice. Methodology: /methodology#likelihood.
At a glance
| Generic name | sitagliptin (MK0431) |
|---|---|
| Also known as | MK0431, Januvia, sitagliptin phosphate |
| Sponsor | Merck Sharp & Dohme LLC |
| Drug class | DPP-4 inhibitor |
| Target | DPP-4 |
| Modality | Small molecule |
| Therapeutic area | Diabetes |
| Phase | Phase 3 |
Mechanism of action
Incretin hormones, such as GLP-1 and GIP, are released in response to meals and are involved in the regulation of glucose metabolism. By inhibiting DPP-4, sitagliptin increases the levels of active incretin hormones, which in turn increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner.
Approved indications
- Type 2 diabetes mellitus
- Diabetic nephropathy
Common side effects
- Nausea
- Diarrhea
- Headache
- Upper respiratory tract infection
- Musculoskeletal pain
Key clinical trials
- The Role of Phosphodiesterase Inhibitors in Incretin Secretion (PHASE1)
- Comparative Effectiveness of Oral Semaglutide vs Sitagliptin Among Individuals With Heart Failure With Preserved Ejection Fraction (STEP-HFpEF DM ORAL)
- 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)
- 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)
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 (MK0431) CI brief — competitive landscape report
- sitagliptin (MK0431) updates RSS · CI watch RSS
- Merck Sharp & Dohme LLC portfolio CI
Frequently asked questions about sitagliptin (MK0431)
What is sitagliptin (MK0431)?
How does sitagliptin (MK0431) work?
What is sitagliptin (MK0431) used for?
Who makes sitagliptin (MK0431)?
Is sitagliptin (MK0431) also known as anything else?
What drug class is sitagliptin (MK0431) in?
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What are the side effects of sitagliptin (MK0431)?
What does sitagliptin (MK0431) target?
Related
- Drug class: All DPP-4 inhibitor drugs
- Target: All drugs targeting DPP-4
- Manufacturer: Merck Sharp & Dohme LLC — full pipeline
- Therapeutic area: All drugs in Diabetes
- Indication: Drugs for Type 2 diabetes mellitus
- Indication: Drugs for Diabetic nephropathy
- Also known as: MK0431, Januvia, sitagliptin phosphate
Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing