Drugs / Linagliptin
last change Jul 2026 re-read 2 minutes ago

Linagliptin

Small molecule targets DPP4 via inhibition

Developed for
type 2 diabetes mellitus · diabetes mellitus · prediabetes syndrome · COVID-19 · hypertensive disorder · abdominal obesity-metabolic syndrome · chronic kidney disease · chronic renal failure syndrome
+17 more · cirrhosis of liver · cognitive impairment with or without cerebellar ataxia · congestive heart failure · diabetic kidney disease · digestive system carcinoma · glucose intolerance · hyperglycemia · impaired renal function disease · left ventricular failure · non-small cell lung carcinoma · schizophrenia · diastolic heart failure · disease related to solid organ transplantation · NAFLD1 · polycystic ovary syndrome · proteinuria · type 1 diabetes mellitus
Investigated by
Boehringer Ingelheim · Eli Lilly and Company · AJU Pharm Co., Ltd. · Hospital Regional de Alta Especialidad del Bajio · University of Guanajuato · Dong Wha Pharmaceutical Co. Ltd.
+55 more · American Diabetes Association · Boryung Pharmaceutical Co., Ltd · Emory University · GC Biopharma Corp · Hoffmann-La Roche · Abbott · Aix Marseille Université · Amsterdam UMC, location VUmc · Beth Israel Deaconess Medical Center · BioLineRx, Ltd. · Boston Medical Center · Changzhou No.2 People's Hospital · European Commission · European Union · Evidem Consultores SL · Fondazione dell'Associazione Medici Diabetologi · Fundación para la Investigación del Hospital Clínico de Valencia · Halozyme Therapeutics · Heart Care Foundation · Huashan Hospital · Humanis · Instituto de Biología y Medicina Experimental, IBYME, Buenos Aires, Argentina · Instituto de Salud Carlos III · Korea University Anam Hospital · LG Life Sciences · M.H.H. Kramer · Marcus Borchert · Medtronic · Merck Serono International SA · Metabolic Research Unit · Ministry of Public Health, Argentina · Mitsui Memorial Hospital · Mitsukoshi Health and Welfare Foundation · Monash University · Nabiqasim Industries (Pvt) Ltd · Nanjing First Hospital, Nanjing Medical University · Northwell Health · Pontificia Universidad Catolica de Chile · Post Graduate Institute of Medical Education and Research, Chandigarh · Profil Institute for Metabolic Research GmbH · Rabin Medical Center · Rush University · Steno Diabetes Center Copenhagen · The Affiliated Jiangning Hospital of Nanjing Medical University · The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School · Universiti Kebangsaan Malaysia Medical Centre · University Medical Center Groningen · University of Denver · University of Miami · University of Padova · University of Washington · Wuxi People's Hospital · Yanbing Li · dr. DJ Mulder · ikfe-CRO GmbH

Regulatory milestones approvals, filings & regulatory actions · 8 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Label expansions (6) US (FDA) TRADJENTA 2012-05-22 – 2023-06-20 fda.gov
Approved EU (EMA) Trajenta 2011-08-23 europa.eu
Approved US (FDA) TRADJENTA 2011-05-02 fda.gov

Trials 121 · started per year

today
US approved 2011
EU approved 2011
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20052006200720082009201020112012201320142015201620172018201920202021202220232024202520262027
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 151 trials
Phase 1 NCT07034781 Aug → Nov 2025 overdue type 2 diabetes mellitus AJU Pharm Co., Ltd. Not yet recruiting No outcome recorded
Phase 1 NCT07044765 Aug → Nov 2025 overdue type 2 diabetes mellitus AJU Pharm Co., Ltd. Not yet recruiting No outcome recorded
Phase 1 NCT07039890 Mar → May 2025 type 2 diabetes mellitus Humanis Completed No outcome recorded
Phase 1 NCT05729386 Feb → Apr 2023 GC Biopharma Corp Unknown No outcome recorded
Phase 1 NCT05703984 Jan → Apr 2023 GC Biopharma Corp Unknown No outcome recorded
Phase 1 NCT05874180 Jan → Feb 2023 Dong Wha Pharmaceutical Co. Ltd. Completed No outcome recorded
Phase 1 NCT05874167 Aug → Oct 2022 Dong Wha Pharmaceutical Co. Ltd. Completed No outcome recorded
Phase 1 NCT04972539 Aug → Nov 2020 type 2 diabetes mellitus AJU Pharm Co., Ltd. Completed No outcome recorded
Phase 1 NCT04970940 Jul → Oct 2020 type 2 diabetes mellitus AJU Pharm Co., Ltd. Completed No outcome recorded
Phase 1 NCT05066516 Jun → Aug 2020 diabetes mellitus Korea University Anam Hospital Completed No outcome recorded
Phase 1/22 trials
Phase 1/2 NCT03337698 Dec 2017 → Oct 2025 non-small cell lung carcinoma Hoffmann-La Roche Terminated No outcome recorded
Phase 1/2 NCT03281369 Oct 2017 → Oct 2025 digestive system carcinoma Hoffmann-La Roche Completed No outcome recorded
Phase 26 trials
Phase 2 NCT01342484 Apr 2011 → Feb 2016 type 2 diabetes mellitus Boehringer Ingelheim Completed No outcome recorded
Phase 2 NCT01012037 Nov 2009 → Sep 2010 type 2 diabetes mellitus Boehringer Ingelheim Completed No outcome recorded
Phase 2 NCT00716092 Jul → Nov 2008 type 2 diabetes mellitus Boehringer Ingelheim Completed No outcome recorded
Phase 2 NCT02183324 Feb → Jun 2007 type 2 diabetes mellitus Boehringer Ingelheim Completed No outcome recorded
Phase 2 NCT00328172 May 2006 → Aug 2007 type 2 diabetes mellitus Boehringer Ingelheim Completed No outcome recorded
Phase 2 NCT00309608 Apr 2006 → Aug 2007 type 2 diabetes mellitus Boehringer Ingelheim Completed No outcome recorded
Phase 334 trials
Phase 3 NCT05641337 Oct 2022 → Dec 2025 cirrhosis of liver, diabetes mellitus Huashan Hospital Unknown No outcome recorded
Phase 3 NCT06329674 Apr 2021 → Dec 2022 type 2 diabetes mellitus AJU Pharm Co., Ltd. Completed No outcome recorded
Phase 3 NCT04371978 Oct 2020 → Apr 2021 COVID-19, respiratory system disorder, type 2 diabetes mellitus Rabin Medical Center Terminated No outcome recorded
Phase 3 NCT04542213 Aug 2020 → Feb 2021 COVID-19, hyperglycemia Hospital Regional de Alta Especialidad del Bajio Completed No outcome recorded
Phase 3 NCT04131582 Sep 2019 → Dec 2020 prediabetes syndrome University of Guanajuato Unknown No outcome recorded
Phase 3 NCT04134650 Sep 2019 → Jun 2020 prediabetes syndrome University of Guanajuato Unknown No outcome recorded
Phase 3 NCT03429543 Mar 2018 → Oct 2022 type 2 diabetes mellitus Boehringer Ingelheim Completed No outcome recorded
Phase 3 NCT02897349 Sep 2016 → Jan 2019 type 2 diabetes mellitus Boehringer Ingelheim Completed No outcome recorded
Phase 3 NCT02851745 Jul 2015 → Jul 2019 left ventricular failure, type 2 diabetes mellitus Heart Care Foundation Completed No outcome recorded
Phase 3 NCT02489968 May 2015 → Nov 2016 type 2 diabetes mellitus Boehringer Ingelheim Completed No outcome recorded
Phase 423 trials
Phase 4 NCT06862739 Oct 2025 → Apr 2026 overdue type 2 diabetes mellitus Nabiqasim Industries (Pvt) Ltd Recruiting No outcome recorded
Phase 4 NCT06851962 May 2025 → Jun 2026 overdue type 2 diabetes mellitus Fundación para la Investigación del Hospital Clínico de Valencia Active not recruiting No outcome recorded
Phase 4 NCT04341935 Jun → Dec 2021 COVID-19, type 2 diabetes mellitus University of Miami Withdrawn No outcome recorded
Phase 4 NCT02768220 Dec 2017 → Aug 2018 diabetes mellitus Northwell Health Withdrawn No outcome recorded
Phase 4 NCT03504566 Nov 2017 → Jun 2019 diabetic kidney disease Steno Diabetes Center Copenhagen Withdrawn No outcome recorded
Phase 4 NCT03433248 Nov 2017 → Jun 2021 type 2 diabetes mellitus M.H.H. Kramer Unknown No outcome recorded
Phase 4 NCT03320031 Jun 2017 → Dec 2019 type 2 diabetes mellitus Yanbing Li Unknown No outcome recorded
Phase 4 NCT04088461 Sep 2016 → Sep 2018 glucose intolerance, prediabetes syndrome University of Guanajuato Completed No outcome recorded
Phase 4 NCT03004612 Jan 2016 → May 2019 prediabetes syndrome University of Guanajuato Completed No outcome recorded
Phase 4 NCT02312427 Jan 2015 → Mar 2016 congestive heart failure, diabetes mellitus Mitsui Memorial Hospital Completed No outcome recorded
Phase not applicable5 trials
NCT05313529 Oct 2022 → Dec 2025 overdue cognitive impairment with or without cerebellar ataxia, type 2 diabetes mellitus The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School Active not recruiting No outcome recorded
NCT05032001 Aug 2021 → Aug 2022 abdominal obesity-metabolic syndrome, type 2 diabetes mellitus Metabolic Research Unit Unknown No outcome recorded
NCT02608177 Nov 2015 → Aug 2017 chronic kidney disease, type 2 diabetes mellitus University of Washington Completed No outcome recorded
NCT03222765 Mar 2015 → Dec 2018 prediabetes syndrome Evidem Consultores SL Unknown No outcome recorded
NCT01974544 May 2013 → Dec 2015 type 2 diabetes mellitus Pontificia Universidad Catolica de Chile Unknown No outcome recorded
Also used as a comparator or background therapy in 53 trials
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 12 trials
Phase 1 NCT01845077 Comparator May → Aug 2013 Boehringer Ingelheim Completed No outcome recorded
Phase 1 NCT02173652 Comparator Mar → Apr 2008 Boehringer Ingelheim Completed No outcome recorded
Phase 23 trials
Phase 2 NCT04662866 Comparator Feb 2021 → Dec 2022 glucose intolerance Oslo University Hospital Unknown No outcome recorded
Phase 2 NCT03986073 Comparator Jan → Jun 2020 type 2 diabetes mellitus Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Unknown No outcome recorded
Phase 2 NCT03667300 Comparator Mar 2017 → May 2019 impaired renal function disease, proteinuria, type 2 diabetes mellitus Samsung Medical Center Completed No outcome recorded
Phase 319 trials
Phase 3 NCT07635953 Comparator Jul 2026 → Jul 2029 expected diabetes mellitus Sun Yat-sen University Not yet recruiting No outcome recorded
Phase 3 NCT06946628 Comparator Jun 2025 → Dec 2028 expected diabetes mellitus Sun Yat-sen University Not yet recruiting No outcome recorded
Phase 3 NCT04670666 Comparator Nov 2024 → Jul 2026 overdue type 2 diabetes mellitus EMS Recruiting No outcome recorded
Phase 3 NCT05886088 Comparator Feb 2024 → May 2026 overdue type 2 diabetes mellitus EMS Not yet recruiting No outcome recorded
Phase 3 NCT03766750 Comparator Dec 2021 → Oct 2023 type 2 diabetes mellitus EMS Withdrawn No outcome recorded
Phase 424 trials
Phase 4 NCT07452913 Comparator Jan → Mar 2026 overdue type 2 diabetes mellitus Bahria University Enrolling by invitation No outcome recorded
Phase 4 NCT07442006 Comparator Oct 2025 → Mar 2027 expected type 2 diabetes mellitus JW Pharmaceutical Recruiting No outcome recorded
Phase 4 NCT07019012 Comparator Jul 2025 → Oct 2026 expected type 2 diabetes mellitus Huazhong University of Science and Technology Recruiting No outcome recorded
Phase 4 NCT06449235 Comparator Sep 2024 → Apr 2025 overdue type 2 diabetes mellitus Bangladesh Institute of Research and Rehabilitation in Diabetes, Endocrine and Metabolic Disorders Not yet recruiting No outcome recorded
Phase 4 NCT06449833 Comparator Jun 2024 → Nov 2026 expected NAFLD1, type 2 diabetes mellitus Zhujiang Hospital Recruiting No outcome recorded
Phase not applicable5 trials
NCT06098625 Comparator Nov 2023 → Jul 2025 diabetes mellitus Medanta, The Medicity, India Unknown No outcome recorded
NCT06095492 Comparator Oct 2023 → Oct 2025 overdue diabetes mellitus Medanta, The Medicity, India Recruiting No outcome recorded
NCT02792400 Comparator May → Aug 2016 type 2 diabetes mellitus University Hospital, Gentofte, Copenhagen Completed No outcome recorded
NCT02244164 Comparator Oct 2014 → Feb 2023 type 2 diabetes mellitus Erasme University Hospital Terminated No outcome recorded
NCT02725502 Comparator Jul 2013 → Apr 2016 type 1 diabetes mellitus Post Graduate Institute of Medical Education and Research, Chandigarh Unknown No outcome recorded

Evidence & citations 20 cited values

Every value below carries the sentence it was read from. 182 sources stand behind the page.

FieldValueCited text
Known as Linagliptin “The objective of the current study is to investigate the efficacy, safety and tolerability of Linagliptin (BI 1356) (5 mg or 10 mg / once daily) compared to placebo given for...” NCT00654381
147

“A total of 235 patients with inadequate response to metformin (≥1000 mg/day) plus linagliptin (5 mg/day) were randomized to receive either dapagliflozin/linagliptin fixed-dose...” PMID 39375869 Oct 2024

“To investigate the influence of mild, moderate, and severe liver impairment on the pharmacokinetics and pharmacodynamics of linagliptin in comparison with a control group with...” NCT02183376

“A Randomised, Double-blind, Placebo-controlled, Parallel Group Dose-finding Study of Linagliptin (1 and 5 mg Administered Orally Once Daily) Over 12 Weeks in Children and...” NCT01342484

“Subsequently, those with HbA1c ≥7.0 and ≤10.5% (>53 and ≤91 mmol/mol) (N = 482) were randomized to 24 weeks' double-blind, double-dummy treatment with linagliptin 5 mg or...” PMID 27762093 Nov 2016

“The hypoglycemic scheme of the experimental group was that the initial dose of Insulin Degludec and Insulin Aspart was 0.3U/kg multiplied by the patient's weight, plus 5 mg of...” NCT05641337

“patients with inadequately controlled T2DM on SU monotherapy were randomly assigned to receive treatment with linagliptin 5 mg once daily (n = 161) or placebo (n = 84) for 18 weeks.” PMID 22939034 Aug 2012

“DPP-4 inhibitor (sitagliptin, vildagliptin, alogliptin, linagliptin, teneligliptin, anagliptin or saxagliptin) will be suspended for one month and serum BNP will be measured.” NCT02312427

“Chemical Names: Sitagliptin, Vildagliptin, Saxagliptin, Linagliptin, Alogliptin Class: Dipeptidyl Peptidase-4 (DPP-4) Inhibitors” NCT06449235

“A Pharmacokinetic Study of DW6013 (FDC of Linagliptin and Metformin) in Healthy Adult Volunteers in Fed Condition” NCT05874180

“Single oral dose A51R1(Dapagliflozin) 10 mg tablet and A51R2(Linagliptin) 5 mg tablet taken together” NCT04972539

“All prediabetes and T2DM subjects receive Linagliptin 5mg once daily for a duration of 12 weeks.” NCT05290506

“A Pharmacokinetic Study of DW6013 (FDC of Linagliptin and Metformin) in Healthy Adult Volunteers” NCT05874167

“Alogliptin, anagliptin, linagliptin, saxagliptin, sitagliptin, teneligliptin or vildagliptin” NCT03014479

“short-term intensive CSII followed by Linagliptin 5mg qd and Metformin 0.5g bid for 48 weeks” NCT03194945

“Metformin 1.7-2.5mg per day plus Linagliptin 5mg per day or Sitagliptin 50-100mg per day” NCT05032001

“Efficacy and Safety of 3 Doses of BI1356 (Linagliptin) in Type 2 Diabetes Patients” NCT00328172

“Early Combination Therapy with Linagliptin and Metformin in People with Type 2” PMID 32328953 Apr 2020

Linagliptin 5mg/tab and Metformin Hydrochloride 1000mg/tab (2 tablets)” NCT05729386

Linagliptin 5mg/tab and Metformin Hydrochloride 1000mg/tab (2 tablets)” NCT05703984

“if Metformin is not tolerated, switch to Linagliptin 5 mg qd” NCT06946628

“if Metformin is not tolerated, switch to Linagliptin 5 mg qd” NCT07635953

“Once daily treatment with oral linagliptin (Tradjenta) 5 mg” NCT03433248

“Sitagliptin up to 100 mg daily, Linagliptin up to 5mg daily” NCT02041234

“Dapagliflozin 10mg + Linagliptin 5mg” NCT07034781

“Dapagliflozin 10mg + Linagliptin 5mg” NCT07044765

linagliptin (2.5-5mg daily)” NCT02528019

LinagliptinNCT02041234

NCT01422876

NCT01087502

NCT02792400

NCT01215097

NCT02183636

NCT04564872

NCT00602472

NCT01214239

NCT06095492

NCT02489968

NCT01835678

NCT05886088

NCT01845077

NCT03986073

NCT02725502

NCT02467478

NCT05200793

NCT02280174

NCT02897349

NCT07039890

NCT03609294

NCT05313529

NCT03504566

NCT02401880

NCT03320031

NCT02092597

NCT04371978

NCT02183584

NCT02191228

NCT03667300

NCT01084005

NCT03629054

NCT03011177

NCT02768220

NCT01969084

NCT01383356

NCT01216397

NCT00954447

NCT02004366

NCT06862739

NCT02376075

NCT01243424

NCT01204294

NCT04134650

NCT01792518

NCT02077309

NCT00736099

NCT07442006

NCT02815644

NCT02442817

NCT01617824

NCT04662866

NCT02453555

NCT00309608

NCT04131582

NCT02608177

NCT07019012

NCT02183480

NCT01512979

NCT01974544

NCT06851962

NCT01438814

NCT01897532

NCT03458715

NCT02372630

NCT03281369

NCT04341935

NCT02974504

NCT02429232

NCT03222765

NCT02097342

NCT00641043

NCT02350478

NCT03250052

NCT02172222

NCT00716092

NCT02180334

NCT01194830

NCT02106104

NCT02851745

NCT03429543

NCT02015299

NCT03642184

NCT00996658

NCT01968044

NCT04542213

NCT02821910

NCT05066516

NCT03259490

NCT07452913

NCT06449833

NCT00601250

NCT01547104

NCT06098625

NCT03004612

NCT01888796

NCT04088461

NCT02061969

NCT00621140

NCT02752113

NCT04670666

NCT01708902

NCT01734785

NCT01183013

NCT01903070

NCT00915772

NCT03337698

NCT01189201

NCT02072096

NCT01540487

NCT02223026

NCT03051243

NCT07247656

NCT00935220

NCT01703286

NCT02240680

NCT01943019

NCT02212782

NCT00740051

NCT01012037

Known as - linagliptine (Trajenta). “- linagliptine (Trajenta®).” NCT02244164
Known as A51R2 “Single oral dose A51R1(Dapagliflozin) 10 mg tablet and A51R2(Linagliptin) 5 mg tablet taken together” NCT04972539
Known as B I1356 “The objective of the current study is to investigate the efficacy, safety and tolerability of Linagliptin (BI 1356) (5 mg or 10 mg / once daily) compared to placebo given for...” NCT00654381
27

“An Open Label, Phase I Trial to Investigate the Pharmacokinetics and Pharmacodynamics of Linagliptin (BI 1356) 5 mg After Single and Multiple Oral Administration” NCT00935220

“Efficacy and Safety of B I1356 (Linagliptin) vs. Placebo Added to Metformin Background Therapy in Patients With Type 2 Diabetes” NCT00601250

“Efficacy and Safety of BI 1356 (Linagliptin) Versus Placebo in Type 2 Diabetic Patients With Insufficient Glycemic Control” NCT00621140

“Efficacy and Safety of Linagliptin (BI 1356) in Black/African Americans With Type 2 Diabetes With a MTT Sub-study” NCT01194830

“The Effect of Linagliptin (BI 1356) on 24h-glucose Control and Various Biomarkers in Type 2 Diabetic Patients” NCT00716092

“Safety and Efficacy of Linagliptin (BI 1356) Plus Metformin in Type 2 Diabetes, Factorial Design” NCT00798161

“Efficacy and Safety of 3 Doses of BI1356 (Linagliptin) in Type 2 Diabetes Patients” NCT00328172

“5 mg linagliptin (BI 1356)/45 mg pioglitazone fixed dose combination” NCT02183636

“BI 1356 (Linagliptin) (5 mg / once daily)” NCT00641043

“BI1356 low dose” NCT01342484

NCT02183610

NCT02183389

NCT02173652

NCT02173639

NCT02183493

NCT02175394

NCT02183402

NCT02183467

NCT02183441

NCT00800683

NCT00819091

NCT02183428

NCT00328172

NCT02183298

NCT02183337

NCT00622284

NCT02183363

Known as BI 1356 BS “Efficacy and Safety of BI 1356 BS (Linagliptin) in Combination With Metformin” NCT00309608
9

NCT02183623

NCT02183532

NCT02173665

NCT02183506

NCT02180503

NCT02183415

NCT02183311

NCT02183324

NCT02183350

Known as BS 1356 BS ChEMBL registry synonym — accepted as the source's own label CHEMBL237500
Known as Lina “This double-blind, randomized, placebo-controlled trial (ClinicalTrials.gov NCT02453555) evaluated the efficacy and safety of empagliflozin (Empa) 10 or 25 mg as add-on to...” PMID 29766636 Jun 2018
1

“evaluated the efficacy and safety of empagliflozin (Empa) 10 or 25 mg and linagliptin (Lina) 5 mg fixed-dose combinations (FDCs) in Japanese patients with type 2 diabetes...” PMID 30091172 Sep 2018

Known as Linagliptin component of glyxambi ChEMBL registry synonym — accepted as the source's own label CHEMBL237500
Known as Linagliptin component of jentadueto ChEMBL registry synonym — accepted as the source's own label CHEMBL237500
Known as Linagliptin component of trijardy xr ChEMBL registry synonym — accepted as the source's own label CHEMBL237500
Known as Linagliptina ChEMBL registry synonym — accepted as the source's own label CHEMBL237500
Known as linagliptine “- linagliptine (Trajenta®).” NCT02244164
Known as Tradjenta “5 mg Linagliptin (Tradjenta)” NCT01845077
1

NCT03766750

Known as Trajenta “each group was administered either a single dose of IN-C009 (FCDP, dapagliflozin 10mg/linagliptin 5 mg) (HK inno.N., Seoul, Korea) or co-administration of a single dose of...” NCT05066516
1

“AJU-A51R2: Trajenta 1 Tab., Q.D., single dose, for 11 days” NCT04970940

Known as Trajenta (Linagliptin) Trajenta (Linagliptin)NCT03051243
Known as Trazenta ChEMBL registry synonym — accepted as the source's own label CHEMBL237500
Action Inhibit “the dipeptidyl peptidase-4 inhibitor linagliptin” PMID 21781152 Nov 2011
Modality Small molecule “the dipeptidyl peptidase-4 inhibitor linagliptin” PMID 24169807 Oct 2013
1

CHEMBL237500

Route Oral “1 mg, 5 mg and 10 mg Administered Orally Once Daily” NCT00309608
Target DPP4 “the dipeptidyl peptidase (DPP)-4 inhibitor linagliptin versus comparator treatments” PMID 22234149 Jan 2012