Summary
Linagliptin has reached the approved stage (maximum clinical phase 4) for at least one indication, so its use in Type 2 Diabetes would be drug repurposing rather than first-in-human development. This does not mean it is approved for Type 2 Diabetes. ClinicalTrials.gov lists 8 registered trials linking Linagliptin to Type 2 Diabetes: 7 have completed; 1 is terminated, withdrawn, suspended or of unknown status. The most advanced is Phase 4 (NCT02106104). The largest enrolment is 615067 participants (NCT02138097). Registration activity spans 2008 to 2015. The literature layer holds 13 publications for this pair: 5 Cochrane reviews, 1 meta-analysis, 2 systematic reviews and 5 clinical trial publications. Publication years run from 2022 to 2026. Because at least one synthesis-level source exists (systematic review, meta-analysis or Cochrane review), this pair has been assessed beyond single studies, although the synthesis may concern a different indication.
The RepurpOS disease-intelligence file for Type 2 Diabetes Mellitus ranks 767 candidate therapeutics from Open Targets, ChEMBL, DGIdb and PubMed; only a minority carry direct clinical evidence, and this page covers one of those. Spontaneous remission context recorded for the condition: 1.6-1.7% at 7 years on standard care (population-level cohorts UK and US).
Evidence table
| Evidence tier | A · Strong |
|---|---|
| Evidence score | 80.0 (trials 30.0, literature 30.0, tier 15, approved bonus 5.0) |
| Registered trials | 8 total: 0 recruiting, 0 active / not yet recruiting, 7 completed, 1 other |
| Linked publications | 13 (5 Cochrane reviews, 5 clinical trial publications, 2 systematic reviews, 1 meta-analysis) |
| Agent type | Drug (Small molecule) |
| Development stage (any indication) | Approved |
| Mechanism / class | Not recorded |
| Data sources | Open Targets, ChEMBL |
How the evidence score is calculated
- Each registered trial scores by status (recruiting / active / enrolling 3, completed 2.5, not yet recruiting 2, unknown 1, terminated / withdrawn / suspended 0.5) plus a phase bonus (phase 3-4 +2, phase 2 +1, phase 1 +0.5). The trial component is capped at 30.
- Each literature item scores by design (Cochrane review 5, meta-analysis 4, systematic review 3, RCT 3, clinical trial publication 2, curated reference 1.5, other PubMed record 1). The literature component is capped at 30.
- The existing evidence tier adds 15 (A / Strong), 10 (B / Moderate), 5 (C / Preliminary) or 0 (D / Anecdotal).
- Agents approved for any indication (max clinical phase 4) add 5, because an approved agent has an established safety profile that lowers the barrier to repurposing trials.
- The score ranks what has been studied, not what works. It does not read effect sizes or directions of effect.
Registered clinical trials
| NCT ID | Title | Status | Phase | Enrolment |
|---|---|---|---|---|
| NCT02106104 | Renal Effects of DPP-4 Inhibitor Linagliptin in Type 2 Diabetes 2014 | completed | Phase 4 | 48 |
| NCT02097342 | Effect of Linagliptin on Insulin Sensitivity and Pancreatic Beta Cell Function in Patients With Type 2 Diabetes Mellitus 2013 | status unknown | Phase 4 | 30 |
| NCT00915772 | Treatment of Type 2 Diabetes With Linagliptin 2.5 mg Bid + Metformin 500 or 1000 mg Bid and Metformin 1000 mg Bid 2009 | completed | Phase 3 | 567 |
| NCT01087502 | Safety and Efficacy of Linagliptin in Type-2-diabetes Mellitus Patients With Moderate to Severe Renal Impairment 2010 | completed | Phase 3 | 241 |
| NCT00622284 | Efficacy and Safety of BI 1356 in Combination With Metformin in Patients With Type 2 Diabetes 2008 | completed | Phase 3 | 1,560 |
| NCT01215097 | Efficacy and Safety Study of Linagliptin (5 mg Administered Orally Once Daily) Over 24 Weeks in Type 2 Diabetic Patients With Insufficient Glycaemic Control Despite Metformin Therapy 2010 | completed | Phase 3 | 306 |
| NCT02138097 | Oral and Non-insulin Injected Hypoglycemic Therapy Utilization Patterns 2014 | completed | Not applicable | 615,067 |
| NCT02608177 | Continuous Glucose Monitoring to Assess Glycemia in Chronic Kidney Disease - Changing Glucose Management 2015 | completed | Not applicable | 3 |
Published literature
- Clinical trial publication Effect of SGLT2 Inhibitors + DPP-4 Inhibitors on Urine Microbiota in Type 2 DiabetesCalvigioni M, Biancalana E, Rossi C et al. · Diabetes/metabolism research and reviews · 2026 · PMID 41566786
- Cochrane review Comparison and Evaluation of Efficacy and Safety of Sitagliptin and Linagliptin in Adults With Type 2 Diabetes Mellitus: A Bayesian Network Meta-AnalysisLi L, Cui S, Chow J et al. · Journal of evidence-based medicine · 2026 · PMID 41918146
- Cochrane review Evaluation and comparison of efficacy and safety of mitochondrial modulator (Imeglimin) and DPP-4 inhibitors in patients with type 2 diabetes mellitus: A Bayesian network meta-analysisChow J, Lim W, Li L et al. · Journal of endocrinological investigation · 2026 · PMID 40936045
- Meta-analysis Dipeptidyl peptidase-4 inhibitors and diabetic retinopathy in type 2 diabetes: A network meta-analysis of randomized clinical trialsOrtiz-Seller A, Real JT, Morcillo E et al. · Journal of diabetes and its complications · 2026 · PMID 41314124
- Clinical trial publication Fasting and postprandial kidney haemodynamic effects of empagliflozin and linagliptin in mono- and combination therapy compared to gliclazide in overweight people with type 2 diabetes (RACELINES): A randomised, double-blind trialvan Baar MJB, Muskiet MHA, Scholtes RA et al. · Diabetes, obesity & metabolism · 2025 · PMID 40326063
- Clinical trial publication Efficacy and safety of a fixed-dose combination of dapagliflozin and linagliptin (AJU-A51) in patients with type 2 diabetes mellitus: A multicentre, randomized, double-blind, parallel-group, placebo-controlled phase III studyHong JH, Kim MJ, Min KW et al. · Diabetes, obesity & metabolism · 2025 · PMID 39375869
- Clinical trial publication Pharmacometrics-Enhanced Bayesian Borrowing for Pediatric Extrapolation - A Case Study of the DINAMO TrialSailer MO, Neubacher D, Johnston C et al. · Therapeutic innovation & regulatory science · 2025 · PMID 39373938
- Cochrane review Impact of DPP-4 Inhibitors on Interleukin Levels in Type 2 Diabetes MellitusFeng Y, Shang B, Yang Y et al. · The Journal of clinical endocrinology and metabolism · 2025 · PMID 39512193
- Clinical trial publication Intense simplified strategy for newly diagnosed type 2 diabetes in patients with severe hyperglycaemia: multicentre, open label, randomised trialLiu L, Ke W, Li H et al. · BMJ (Clinical research ed.) · 2024 · PMID 39406449
- Cochrane review Safety of Linagliptin in Patients with Type 2 Diabetes Mellitus: A Systematic Review and Meta-analysis of Randomized Clinical TrialsAljohani H, Alrubaish FS, Alghamdi WM et al. · Therapeutic innovation & regulatory science · 2024 · PMID 38634983
- Systematic review The effectiveness and safety of linagliptin within elderly type 2 diabetes mellitus: a meta-analysis and systematic reviewWang MJ, Liu JL, Wang N et al. · Minerva endocrinology · 2024 · PMID 35103456
- Cochrane review Comparative efficacy and safety of glucose-lowering drugs in children and adolescents with type 2 diabetes: A systematic review and network meta-analysisWu S, He Y, Wu Y et al. · Frontiers in endocrinology · 2022 · PMID 36034458
- Systematic review The efficacy and safety of evogliptin for type 2 diabetes mellitus: A systematic review and meta-analysisTang Q, Pan W, Peng L · Frontiers in endocrinology · 2022 · PMID 36060938
Mechanism and notes
No mechanism of action is recorded for this pair in the source databases.
OSMF's existing evidence tier for this pair is A (Strong), derived from the strength of the disease association recorded in Open Targets and ChEMBL. The tier describes how well the drug-disease link is documented, not how well the drug works.
Frequently asked questions
Is Linagliptin approved for Type 2 Diabetes?
Linagliptin has reached the approved stage (maximum clinical phase 4) for at least one indication, so its use in Type 2 Diabetes would be drug repurposing rather than first-in-human development. This does not mean it is approved for Type 2 Diabetes. Approval status for the specific indication should always be confirmed with the relevant regulator and prescribing information.
Is Linagliptin in clinical trials for Type 2 Diabetes?
ClinicalTrials.gov lists 8 registered trials linking Linagliptin to Type 2 Diabetes: 7 have completed; 1 is terminated, withdrawn, suspended or of unknown status. The most advanced is Phase 4 (NCT02106104). The largest enrolment is 615067 participants (NCT02138097). Registration activity spans 2008 to 2015.
What does the evidence show for Linagliptin in Type 2 Diabetes?
Linagliptin has both completed registered trials and synthesis-level publications linked to Type 2 Diabetes. That is the strongest profile in this database, but the summaries here do not extract effect sizes, so read the linked reviews for direction and magnitude of benefit. OSMF's existing evidence tier for this pair is A (Strong), derived from the strength of the disease association recorded in Open Targets and ChEMBL. The tier describes how well the drug-disease link is documented, not how well the drug works.
Cite this page
Data: ClinicalTrials.gov, PubMed, Open Targets, ChEMBL, DGIdb and the OSMF therapeutic agent database. Last updated 2026-07-05. Page built 2026-10-07.