Linagliptin

Linagliptin, sold under the brand name Tradjenta among others, is a medication used to treat type 2 diabetes.[7][8] It is generally less preferred than metformin and sulfonylureas as an initial treatment.[7][9] It is used together with exercise and diet.[7] It is not recommended in type 1 diabetes.[7] It is taken by mouth.[7]

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%)[5]
Identifiers
IUPAC name
  • 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)
SMILES
  • CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
InChI
  • 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
 NY (what is this?)  (verify)

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 is a dipeptidyl peptidase-4 inhibitor.[7] It works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.[7]

Linagliptin was approved for medical use in the United States,[10] Japan, the European Union, Canada, and Australia in 2011.[7][11] In 2020, it was the 293rd most commonly prescribed medication in the United States, with more than 1 million prescriptions.[12][13] As of August 2021, linagliptin is available as a generic medicine.[14]

Medical uses

Results in 2010, from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.[15]

Side effects

Linagliptin may cause severe joint pain.[5][16]

Mechanism of action

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

Names

Linagliptin is the international nonproprietary name (INN).[17]

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. https://www.tga.gov.au/resources/auspar/auspar-linagliptin-0
  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. "Tradjenta- linagliptin tablet, film coated". DailyMed. 21 April 2022. Archived from the original on 15 August 2022. Retrieved 3 October 2022.
  6. "Trajenta EPAR". European Medicines Agency (EMA). Archived from the original on 29 December 2019. Retrieved 11 February 2020.
  7. "Linagliptin Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 6 April 2019. Retrieved 6 April 2019.
  8. 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.
  9. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN 9780857113382.
  10. "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.
  11. "10 years". Boehringer Ingelheim Limited. Archived from the original on 3 October 2022. Retrieved 3 October 2022.
  12. "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  13. "Linagliptin - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
  14. "Linagliptin: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 25 September 2021. Retrieved 24 September 2021.
  15. "Four Phase III Trials Confirm Benefits of BI's Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010. Archived from the original on 10 March 2012.
  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. "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.
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