linagliptin
Trade name: tradjenta
Approved
May 2, 2011
Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor discovered by Boehringer Ingelheim and being developed as an oral once-daily tablet for the treatment of Type 2 diabetes. Linagliptin was first approved by FDA in 2011 under the trade name Tradjenta as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Linagliptin binds to DPP-4 (an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)) in a reversible manner and thus increases the concentrations of incretin hormones. Linagliptin glucose dependently increases insulin secretion and lowers glucagon secretion, thus resulting in better regulation of glucose homeostasis. Linagliptin binds selectively to DPP-4, and selectively inhibits DPP-4 but not DPP-8 or DPP-9 activity in vitro at concentrations approximating therapeutic exposures. — NCATS
Clinical trial activity
176 trials · 104 clinical orgs · 15 marketing orgs
Earliest trial started Oct 1, 2004 (NCT02173665)
Timeline
2000s
- Jan 1, 2004
Boehringer Ingelheim — Earliest Phase 1 Sponsor(trial)
- Jan 1, 2006
Boehringer Ingelheim — Earliest Phase 2 Sponsor(trial)
- Jan 1, 2008
Boehringer Ingelheim — Earliest Phase 3 Sponsor(trial)
2010s
- May 2, 2011
Boehringer Ingelheim — Earliest FDA Approval
- May 2, 2011
Boehringer Ingelheim — NDA Secondary Org
- May 2, 2011
Boehringer Ingelheim — NDA Organization
- Jun 16, 2017
Aurobindo Pharma — Marketing Organization
- Oct 10, 2018
Zydus Discovery DMCC — Marketing Organization
- Nov 1, 2018
Mylan — Marketing Organization
2020s
- May 28, 2020
Sun Pharmaceuticals — Marketing Organization
- Jul 7, 2020
MSN Laboratories — Marketing Organization
- Aug 26, 2020
Kinapse — Marketing Organization
- Aug 26, 2020
Syneos Health — Marketing Organization
- Feb 1, 2021
Dr. Reddy's Laboratories — Marketing Organization
- Mar 30, 2021
Annora Pharma — Marketing Organization
- Aug 30, 2021
Sunshine Lake Pharma Co., Ltd. — Marketing Organization
- Jan 20, 2022
Prinston Inc — Marketing Organization
- Aug 9, 2022
Alkem Labs Ltd — Marketing Organization
- Sep 3, 2024
Invagen Pharms — Marketing Organization
- May 27, 2026
Teva — Marketing Organization
Indications
Approved for
Studied for
- Albuminuria · Phase 3
- Carcinoma, Non-Small-Cell Lung · Phase 1/Phase 2
- Carcinoma, Transitional Cell · Phase 1/Phase 2
- Coronary Artery Disease · Phase 4
- Coronavirus · Phase 3
- Coronavirus Infections · Phase 4
- COVID-19 · Phase 3
- Dipeptidyl-Peptidase IV Inhibitors · Phase 3
- Drug Therapy · Phase 1
- Endocrine System Diseases · Phase 3
- Esophageal Neoplasms · Phase 1/Phase 2
- Glucose Intolerance · Phase 4
- Glucose Metabolism Disorders · Phase 3
- Glycation End Products, Advanced · Phase 4
- Healthy Volunteers · Phase 1
- Heart Failure, Diastolic · Phase 3
- Hepatic Insufficiency · Phase 1
- Hormones · Phase 3
- Hyperglycemia · Phase 3
- Hypertension · Phase 3
- Hypertrophy, Left Ventricular · Phase 3
- Hypoglycemic Agents · Phase 3
- Incretins · Phase 3
- Inflammation · Phase 3
- Insulin Resistance · Phase 4
- Kidney Diseases · Phase 4
- Kidney Failure, Chronic · Phase 4
- Kidney Transplantation · Phase 4
- Linagliptin · Phase 3
- Metabolic Diseases · Phase 3
- Non-alcoholic Fatty Liver Disease · Phase 4
- Osteoporosis · Phase 4
- Peritoneal Dialysis · Phase 4
- Polycystic Ovary Syndrome · Phase 4
- Prediabetic State · Phase 4
- Renal Insufficiency · Phase 2
- Respiratory Tract Diseases · Phase 3
- SARS-CoV-2 · Phase 3
- Schizophrenia · Phase 4
- Sodium-Glucose Transporter 2 Inhibitors · Phase 4
- Urinary Bladder Neoplasms · Phase 1/Phase 2
Mechanism of action
- Dipeptidyl peptidase IVINHIBITOR
DPP4 inhibitor
Combination products
glyxambi
with empagliflozin
jentadueto
with metformin
Also known as jentadueto xr
trijardy xr
with metformin, empagliflozin
Also known as trijardy
Approval history
- approvedMay 2, 2011
Chemistry & pharmacology
SMILES
CC#CCN1C(=NC2=C1C(=O)N(CC3=NC4=CC=CC=C4C(C)=N3)C(=O)N2C)N5CCC[C@@H](N)C5- Mol. weight
- 472.5422 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaLinagliptin ↗
- NCATS3X29ZEJ4R2 ↗
- ChEMBLCHEMBL237500 ↗
Also known as
- bi1356
- bi1356
- bi 1356
- bi 1356
- bi 1356
- bi-1356
- bi-1356
- bi-1356
- bi-1356-bs
- bi-1356-bs
- bs-1356-bs
- bs-1356-bs
- empagliflozin / linagliptin
- empagliflozin / linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin
- linagliptin / metformin
- (r)-8-(3-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methylquinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione
- (r)-8-(3-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methylquinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione
- tradjenta
- tradjenta
- tradjenta
- tradjenta
- trajenta
- trajenta
- trajenta
- trajenta
- trazenta
- trazenta
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07019012 | Phase 4 | Jul 30, 2025 | Huazhong University of Science and Technology, Nanchang University, Shiyan Taihe Hospital, Wuhan Central Hospital, Wuhan University, Xiang Yang NO.1 People's Hospital |
| NCT07213895 | Phase 1 | May 21, 2025 | Humanis Saglık Anonim Sirketi |
| NCT06862739 | Phase 4 | Apr 30, 2025 | Nabiqasim Industries (Pvt) Ltd |
| NCT06851962 | Phase 4 | Apr 30, 2025 | University of Valencia |
| NCT07039890 | Phase 1 | Mar 8, 2025 | Humanis Saglık Anonim Sirketi |
| NCT06932159 | Phase 1 | Dec 23, 2024 | Humanis Saglık Anonim Sirketi |
| NCT06449833 | Phase 4 | Jun 30, 2024 | Southern Medical University |
| NCT06243809 | Phase 1 | Apr 24, 2024 | Mahidol University |
| NCT05886088 | Phase 3 | Feb 29, 2024 | EMS S/A |
| NCT06098625 | N/A | Nov 10, 2023 | Medanta - The Medicity |
| NCT06095492 | N/A | Oct 30, 2023 | Medanta - The Medicity |
| NCT05823883 | Phase 1 | Jun 30, 2023 | DongWha Pharmaceutical Company |
| NCT05823870 | Phase 1 | Feb 24, 2023 | DongWha Pharmaceutical Company |
| NCT05729386 | Phase 1 | Feb 6, 2023 | Green Cross Corporation |
| NCT05703984 | Phase 1 | Jan 17, 2023 | Green Cross Corporation |
| NCT05874180 | Phase 1 | Jan 9, 2023 | DongWha Pharmaceutical Company |
| NCT07247656 | Phase 4 | Dec 1, 2022 | Bahria University |
| NCT05313529 | N/A | Oct 8, 2022 | Nanjing Medical University, Nanjing University, Wuxi People's Hospital |
| NCT05874167 | Phase 1 | Aug 8, 2022 | DongWha Pharmaceutical Company |
| NCT05956522 | Phase 1 | Jul 1, 2022 | Qingdao University |
Organizations
Research & Development (104)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Boehringer Ingelheim | For profit | 94 | 90 | 5 | 2004 |
| Eli Lilly | For profit | 34 | 1 | 5 | 2009 |
| DongWha Pharmaceutical Company | For profit | 5 | 5 | 1 | 2014 |
| Hospital Regional Alta Especialidad Bajio | Academic/Hospital | 5 | 1 | 2 | 2015 |
| Universidad de Guanajuato | Academic/Hospital | 4 | 4 | 2 | 2015 |
| EMS S/A | For profit | 3 | 3 | 1 | 2019 |
| Humanis Saglık Anonim Sirketi | Academic/Hospital | 3 | 3 | 1 | 2024 |
| Profil GmbH | For profit | 3 | 2 | 2 | 2013 |
| Roche | For profit | 3 | 3 | 1 | 2017 |
| American Diabetes Association | Academic/Hospital | 2 | 0 | 2 | 2014 |
| Boryung Pharmaceutical Company | For profit | 2 | 2 | 1 | 2017 |
| Emory University | Academic/Hospital | 2 | 2 | 1 | 2014 |
| Free University of Amsterdam | Academic/Hospital | 2 | 1 | 1 | 2014 |
| Green Cross Corporation | For profit | 2 | 2 | 1 | 2023 |
| ikfe GmbH | For profit | 2 | 2 | 2 | 2012 |
| Korea University | Academic/Hospital | 2 | 1 | 2 | 2013 |
| Medanta - The Medicity | Academic/Hospital | 2 | 2 | 1 | 2023 |
| National University of Malaysia | Academic/Hospital | 2 | 1 | 2 | 2013 |
| Postgraduate Institute of Medical Education and Research | Academic/Hospital | 2 | 2 | 2 | 2013 |
| RWTH Aachen University | Academic/Hospital | 2 | 2 | 1 | 2013 |
Marketing (20)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Alkem Labs Ltd | For profit | MKTG | Aug 9, 2022 |
| Annora Pharma | For profit | MKTG | Mar 30, 2021 |
| Aurobindo Pharma | For profit | MKTG | Jun 16, 2017 |
| Boehringer Ingelheim | For profit | NDA2 | May 2, 2011 |
| Boehringer Ingelheim | For profit | NDA | May 2, 2011 |
| Dr. Reddy's Laboratories | For profit | MKTG | Feb 1, 2021 |
| Dr. Reddy's Laboratories | For profit | SYN | Nov 3, 2025 |
| Invagen Pharms | For profit | MKTG | Sep 3, 2024 |
| Kinapse | For profit | MKTG | Aug 26, 2020 |
| MSN Laboratories | For profit | MKTG | Jul 7, 2020 |
| MSN Laboratories | For profit | SYN | Nov 3, 2025 |
| Mylan | For profit | MKTG | Nov 1, 2018 |
| Mylan | For profit | SYN | Nov 3, 2025 |
| Prinston Inc | For profit | MKTG | Jan 20, 2022 |
| Sun Pharmaceuticals | For profit | MKTG | May 28, 2020 |
| Sunshine Lake Pharma Co., Ltd. | For profit | MKTG | Aug 30, 2021 |
| Syneos Health | For profit | MKTG | Aug 26, 2020 |
| Teva | For profit | MKTG | May 27, 2026 |
| Zydus Discovery DMCC | For profit | MKTG | Oct 10, 2018 |
| Zydus Discovery DMCC | For profit | SYN | Mar 30, 2023 |