DPP-4 Inhibitors
18 drugsAbout DPP-4
Dipeptidyl Peptidase-4 (DPP-4) is an enzyme that inactivates incretin hormones, which regulate blood glucose. Inhibiting DPP-4 prolongs incretin action, improving glucose control. This makes DPP-4 a clinically validated target for type 2 diabetes.
Human genetic studies provide strong support for DPP4 as a therapeutic target (max score 0.77). Variants are linked to intelligence (0.77) and smoking initiation (0.74). Strong eQTL/pQTL signals further support the link between DPP4 and disease.
DPP-4 is targeted by 16 FDA-approved small molecule drugs, including NESINA, JENTADUETO and GLYXAMBI. These drugs primarily address metabolic conditions, though some are being explored in other therapeutic areas.
Human Genetic Evidence Strong
DPP4 has strong genetic support with a max score of 0.77 linked to intelligence.
The strong genetic support suggests a higher probability of clinical success for DPP4-targeting drugs.
Evidence Across Diseases
20 totalGWAS and other genetic studies link DPP4 to 23 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for DPP4 colocalize with these GWAS traits, providing causal evidence that gene expression changes drive disease risk.
Understanding these scores
Association Score (0-1): Combines all evidence types (genetic, literature, drugs, animal models). Higher = more evidence linking target to disease. This is a ranking heuristic, not a confidence score.
L2G Score: Open Targets uses a machine learning model (Locus-to-Gene) to predict which gene is causal at each GWAS locus. L2G=0.5 means ~50% probability of being the causal gene. Only associations with L2G > 0.05 are included.
Odds Ratio (OR): From gene burden studies (UK Biobank, AstraZeneca PheWAS). Measures how loss-of-function variants affect disease risk. OR<1 = protective (inhibiting target may help), OR>1 = risk (losing function causes disease).
Beta (β): Effect size for continuous traits. β<0 = protective, β>0 = risk.
Clinical Translation (~1.8x): Based on Nelson et al. 2015: drug targets with genetic evidence have ~2x higher success rates in clinical trials. We estimate: Strong support (score ≥0.7) → ~1.8x, Moderate (0.3-0.7) → ~1.3x, Weak → baseline.
Colocalization (H4): Tests whether a GWAS signal and an eQTL/pQTL signal share the same causal variant. H4 is the posterior probability that both traits are associated AND share a causal variant. H4 > 0.8 = strong evidence that gene expression/protein levels drive disease risk. This links genetic variation → gene expression → disease, supporting the target-disease connection.
Top Drugs
Six companies have approved DPP-4 drugs, including Takeda, Boehringer Ingelheim and Dr. Reddy's.
The presence of multiple established players suggests a moderately competitive market with potential entry barriers.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| JANUVIA | Merck | 2006 | 1 |
| GLYXAMBI | Boehringer Ingelheim | 2015 | 1 |
| STEGLUJAN | Merck | 2017 | 1 |
| ZITUVIMET | ZYDUS LIFESCIENCES | 2023 | 1 |
| TRIJARDY XR | Boehringer Ingelheim | 2020 | 1 |
| NESINA | Takeda | 2013 | 1 |
| ZITUVIO | ZYDUS LIFESCIENCES | 2023 | 1 |
| JENTADUETO | Boehringer Ingelheim | 2012 | 1 |
| JANUMET XR | Merck | 2012 | 1 |
| KAZANO | Takeda | 2013 | 1 |
| JENTADUETO XR | Boehringer Ingelheim | 2016 | 1 |
| JANUMET | Merck | 2007 | 1 |
| TRADJENTA | Boehringer Ingelheim | 2011 | 1 |
| SITAGLIPTIN PHOSPHATE | Novartis | 2025 | - |
| DAPAGLIFLOZIN AND SAXAGLIPTIN HYDROCHLORIDE | TORRENT | 2026 | - |
Drug Modality Landscape
Modalities
Routes of Administration
DPP-4 is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides could provide a competitive advantage.
Clinical Trials 1,594 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 377 | 311 | 24 | 41 | 93% |
| Phase 2 | 396 | 217 | 76 | 101 | 74% |
| Phase 3 | 390 | 293 | 39 | 54 | 88% |
| Phase 4 | 431 | 300 | 54 | 74 | 85% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
8 Phase 3 trials testing approved DPP-4 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting DPP-4. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
Drug Approval Timeline (2006 - 2025)
Type 2 Diabetes
The first DPP-4 inhibitor, JANUVIA, was approved in 2006, with the most recent, BRYNOVIN, in 2025.
The continued approval of DPP-4 inhibitors indicates sustained interest and potential for further market growth.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 9 companies competing
- • Market share by company
Full Drug Portfolio
- • All 18 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 18-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Competition: High (15 sponsors)
- • Success rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Calculate These Metrics
Target Attractiveness Score
A 0-100 score based on trial activity, sponsor diversity, and completion rates. Calculated from 899 clinical trials targeting DPP-4.
Completion rate: Percentage of trials that reached their planned endpoint. Trials terminated early, withdrawn, or suspended are not counted—these often indicate safety issues, lack of efficacy, or strategic pivots.
- Highly Attractive (80+): High trial activity, many sponsors, strong completion rates
- Attractive (60-79): Good trial activity and validation
- Moderate (40-59): Moderate interest from sponsors
- Low (under 40): Limited trial activity or validation concerns
Strategic Insights
Auto-generated insights based on trial analytics including competition intensity, white space opportunities, modality shifts, and failure patterns. We analyze trial sponsors, phases, indications, and outcomes.
Risk Signals
- High Competition: Many sponsors competing for this target (may reduce market opportunity)
- High Failure Risk: Low trial completion rates suggest development challenges
- Low Validation: Limited trial activity or poor outcomes indicate uncertain viability
- White Space Available: Underexplored indications present opportunities