Linagliptin

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Linagliptin
Linagliptin.png
Systematic (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
Clinical data
Trade names Tradjenta, Trajenta
AHFS/Drugs.com Consumer Drug Information
MedlinePlus a611036
Licence data EMA:Link, US FDA:link
Pregnancy
category
  • US: B (No risk in non-human studies)
Legal status
Routes of
administration		 Oral
Pharmacokinetic data
Bioavailability 30% oral
Protein binding 75% to 99% in plasma
Identifiers
CAS Number 668270-12-0 YesY
ATC code A10BH05 (WHO)
PubChem CID: 10096344
IUPHAR/BPS 6318
ChemSpider 8271879 N
UNII 3X29ZEJ4R2 YesY
KEGG D09566 YesY
ChEMBL CHEMBL237500 N
Chemical data
Formula C25H28N8O2
Molecular mass 472.54 g/mol
  • 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
 NYesY (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.[1] 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.[2]

Side effects

They may cause severe joint pain.[3]

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

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External links

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