Linagliptin, sold under the brand name Tradjenta among others, is a medication used to treat type 2 diabetes (but not type 1) in conjunction with exercise and diet.[8][9] It is generally less preferred than metformin and sulfonylureas as an initial treatment.[8][10] It is taken by mouth.[8]
Clinical data | |
---|---|
Pronunciation | /ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin |
Trade names | Tradjenta, Trajenta, Trazenta |
Other names | BI-1356 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a611036 |
License data |
|
Routes of administration | By mouth |
ATC code |
|
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | ~30% (Tmax = 1.5 hours) |
Protein binding | 75–99% (concentration-dependent) |
Metabolism | Minimal (~10% metabolized) |
Metabolites | Pharmacologically inactive |
Elimination half-life | ~24 hours |
Excretion | Feces (80%), urine (5%)[6] |
Identifiers | |
| |
CAS Number |
|
PubChem CID |
|
IUPHAR/BPS |
|
DrugBank |
|
ChemSpider |
|
UNII |
|
KEGG |
|
ChEBI |
|
ChEMBL |
|
Chemical and physical data | |
Formula | C25H28N8O2 |
Molar mass | 472.553 g·mol−1 |
3D model (JSmol) |
|
Melting point | 202 °C (396 °F) |
| |
| |
(what is this?) (verify) |
Common side effects include inflammation of the nose and throat.[8] Serious side effects may include angioedema, pancreatitis, joint pain.[10][8] Use in pregnancy and breastfeeding is not recommended.[10] Linagliptin is a dipeptidyl peptidase-4 inhibitor[8] that works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.[8]
Linagliptin was approved for medical use in the United States,[11] Japan, the European Union, Canada, and Australia in 2011.[8][12] In 2020, it was the 293rd most commonly prescribed medication in the United States, with more than 1 million prescriptions.[13][14] From August 2021 linagliptin became available as a generic medicine in the US.[15]
Linagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.[6]
Common side effects of linagliptin may include:
Upper respiratory tract infection, Headache, Hypoglycemia, Joint pain, Allergic reactions.[6][16]
Linagliptin belongs to a class of drugs called DPP-4 inhibitors.[6] It is a reversible, competitive inhibitor of DPP-4. GLP-1 and the glucose-dependent insulinotropic polypeptide (GIP) are broken down more slowly when this enzyme is inhibited. While glucagon release from pancreatic alpha cells is inhibited, GLP-1 and GIP promote the production of insulin from the organ's beta cells. Together, these effects improve insulin release in response to glucose and decrease the liver's breakdown of glycogen[17]
Linagliptin is the international nonproprietary name (INN).[18] Trade names: Trajenta,[19] Tradjenta.