Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor used to manage hyperglycemia in patients with type 2 diabetes mellitus. Linagliptin differs from other DPP-4 inhibitors in that it has a non-linear pharmacokinetic profile, is not primarily eliminated by the renal system, and obeys concentration dependant protein binding.
- Mechanism
- Curator reviewed · 5 references
Linagliptin is a competitive, reversible DPP-4 inhibitor. Inhibition of this enzyme slows the breakdown of GLP-1 and glucose-dependant insulinotropic polypeptide (GIP). GLP-1 and GIP stimulate the release of insulin from beta cells in the pancreas while inhibiting release of glucagon from pancreatic beta cells. These effects together reduce the breakdown of glycogen in the liver and increase insulin release in response to glucose.
- Primary indication
- Linagliptin is indicated for the treatment of type II diabetes in addition to diet and exercise.Curator reviewed · 4 structured indications
- Formula / weight
- C25H28N8O2 · 472.5422 g/mol (avg)
- First approval
- Canada, 2011 · United States, 2011 · European Union, 2016
- Code names
- BI-1356 · BI-1356-BS · BS-1356-BS
- Brand names
Resolves to
LTXREWYXXSTFRX-QGZVFWFLSA-NSMILESCC#CCN1C(=NC2=C1C(=O)N(CC1=NC3=C(C=CC=C3)C(C)=N1)C(=O)N2C)N1CCC[C@@H](N)C1What you can answer from here — as of September 15, 2026
Which drugs share a target with Linagliptin, and which of those have an active Phase 3 trial?
Create a free account or log in to explore the full data card.
Create Account