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Linagliptin

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Linagliptin
Clinical data
Trade namesTradjenta, Trajenta
AHFS/Drugs.comConsumer Drug Information
MedlinePlusa611036
License data
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability30% oral
Protein binding75% to 99% in plasma
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
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC25H28N8O2
Molar mass472.54 g/mol g·mol−1
3D model (JSmol)
  • 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 (BI-1356, trade names Tradjenta (US), Trajenta (worldwide)) is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes.

Linagliptin (once-daily) was approved by the U.S. Food and Drug Administration (FDA) on 2 May 2011 for treatment of type II diabetes.[2] It is being marketed by Boehringer Ingelheim and Lilly.

Medical uses

Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.[3]

Side effects

They may cause severe joint pain.[4]

Mechanism of action

Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Both GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output. Thus, linagliptin stimulates the release of insulin in a glucose-dependent manner and decreases the levels of glucagon in the circulation.

See also

References

  • H. Spreitzer (September 1, 2008). "Neue Wirkstoffe - BI-1356". Österreichische Apothekerzeitung (in German) (18/2008): 918.
  • Wang, Y, Serradell, N, Rosa, E, Castaner, R (2008). "BI-1356". Drugs of the Future. 33 (6): 473–477. doi:10.1358/dof.2008.033.06.1215244.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  1. ^ "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 Oct 2023.
  2. ^ "FDA Approves Type 2 Diabetes Drug from Boehringer Ingelheim and Lilly". 3 May 2011.
  3. ^ "Four Phase III Trials Confirm Benefits of BI's Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010.
  4. ^ "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". FDA. 2015-08-28. Retrieved 1 September 2015.


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