Linagliptin
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%)[6]
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
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
 ☒NcheckY (what is this?)  (verify)

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]

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]

Medical uses

Linagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.[6]

Side effects

Common side effects of linagliptin may include:
Upper respiratory tract infection, Headache, Hypoglycemia, Joint pain, Allergic reactions.[6][16]

Mechanism of action

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 beta 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]

Names

Linagliptin is the international nonproprietary name (INN).[18] Trade names: Trajenta,[19] Tradjenta.

See also

References

  1. ↑ "Linagliptin, tablet, 5 mg, Trajenta". Pharmaceutical Benefits Scheme (PBS). July 2012. Archived from the original on 31 March 2015. Retrieved 26 September 2014.
  2. ↑ "AusPAR: Linagliptin". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 9 April 2023.
  3. ↑ "Trajenta Product information". Health Canada. 25 April 2012. Archived from the original on 27 September 2021. Retrieved 3 October 2022.
  4. ↑ "Trajenta 5 mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 27 September 2021. Archived from the original on 19 January 2022. Retrieved 3 October 2022.
  5. ↑ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  6. 1 2 3 4 5 "Tradjenta- linagliptin tablet, film coated". DailyMed. 21 April 2022. Archived from the original on 15 August 2022. Retrieved 3 October 2022.
  7. ↑ "Trajenta EPAR". European Medicines Agency (EMA). 17 September 2018. Archived from the original on 29 December 2019. Retrieved 11 February 2020.
  8. 1 2 3 4 5 6 7 8 "Linagliptin Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 6 April 2019. Retrieved 6 April 2019.
  9. ↑ Neumiller JJ (March 2012). "Pharmacology, efficacy, and safety of linagliptin for the treatment of type 2 diabetes mellitus". The Annals of Pharmacotherapy. 46 (3): 358–67. doi:10.1345/aph.1Q522. PMID 22318932. S2CID 207264493.
  10. 1 2 3 British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN 9780857113382.
  11. ↑ "Drug Approval Package: Tradjenta (linagliptin) Tablets NDA #201280". U.S. Food and Drug Administration (FDA). 7 June 2011. Archived from the original on 3 April 2022. Retrieved 3 October 2022.
  12. ↑ "10 years". Boehringer Ingelheim Limited. Archived from the original on 3 October 2022. Retrieved 3 October 2022.
  13. ↑ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  14. ↑ "Linagliptin - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
  15. ↑ "Linagliptin: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 25 September 2021. Retrieved 24 September 2021.
  16. ↑ "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". U.S. Food and Drug Administration (FDA). 28 August 2015. Archived from the original on 13 December 2019. Retrieved 1 September 2015.
  17. ↑ "Linagliptin". go.drugbank.com. Retrieved 31 December 2023.
  18. ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 61" (PDF). World Health Organization. p. 66. Archived (PDF) from the original on 3 October 2020. Retrieved 10 November 2016.
  19. ↑ "Linagliptin: medicine to treat type 2 diabetes". NHS UK. 25 March 2022. Retrieved 21 November 2022.
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