Linagliptin

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Linagliptin
File:Linagliptin.svg
Clinical data
Pronunciation/ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin
Trade namesTradjenta, Trajenta, Trazenta
Other namesBI-1356
AHFS/Drugs.comMonograph
MedlinePlusa611036
License data
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability~30% (Tmax = 1.5 hours)
Protein binding75–99% (concentration-dependent)
MetabolismMinimal (~10% metabolized)
MetabolitesPharmacologically inactive
Elimination half-life~24 hours
ExcretionFeces (80%), urine (5%)[5]
Identifiers
  • 8-[(3R)-3-Aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
E number{{#property:P628}}
CompTox Dashboard (EPA)
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Chemical and physical data
FormulaC25H28N8O2
Molar mass472.553 g·mol−1
3D model (JSmol)
Melting point202 °C (396 °F)
  • CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
  • InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1 ☒N
  • Key:LTXREWYXXSTFRX-QGZVFWFLSA-N ☒N
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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.[7][8] Linagliptin is a dipeptidyl peptidase-4 inhibitor[7] that works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.[7] It is generally less preferred than metformin and sulfonylureas as an initial treatment.[7][9] It is taken by mouth.[7]

Common side effects include inflammation of the nose and throat.[7] Serious side effects may include angioedema, pancreatitis, joint pain.[9][7] Use in pregnancy and breastfeeding is not recommended.[9]

Linagliptin was approved for medical use in the United States,[10] Japan, the European Union, Canada, and Australia in 2011.[7][11] In 2023, it was the 254th most commonly prescribed medication in the United States, with more than 1 million prescriptions.[12][13] From August 2021, linagliptin became available as a generic medicine in the US.[14]

Medical uses

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Linagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.[5]

Side effects

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Linagliptin may cause severe joint pain.[5][15]

Mechanism of action

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Linagliptin belongs to a class of drugs called DPP-4 inhibitors.[5]

Names

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Linagliptin is the international nonproprietary name (INN).[16] Brand names: Trajenta,[17] Tradjenta.

See also

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References

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