Linagliptin

Linagliptin
Clinical data
Pronunciation LIN-a-GLIP-tin
Trade names Tradjenta, Trajenta
AHFS/Drugs.com Consumer Drug Information
MedlinePlus a611036
License data
Pregnancy
category
  • US: B (No risk in non-human studies)
Routes of
administration
By mouth (tablets)
ATC code A10BH05 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
  • ℞ (Prescription only)
Pharmacokinetic data
Bioavailability ~30% (Tmax = 1.5 hours)
Protein binding 75–99% (concentration-dependent)
Metabolism Minimal (~10% metabolized)
Metabolites Pharmacologically inactive
Biological half-life ~12 hours
Excretion Feces (80%), urine (5%)[1]
Identifiers
CAS Number 668270-12-0 YesY
PubChem (CID) 10096344
IUPHAR/BPS 6318
ChemSpider 8271879 N
UNII 3X29ZEJ4R2 YesY
KEGG D09566 YesY
ChEBI CHEBI:68610 N
ChEMBL CHEMBL237500 N
Chemical and physical data
Formula C25H28N8O2
Molar mass 472.54 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Linagliptin (INN,[2] previously known as BI-1356, marketed under trade names Tradjenta (U.S.) and Trajenta (worldwide)) is a dipeptidyl peptidase-4 inhibitor developed by Boehringer Ingelheim for treatment of diabetes mellitus type 2.

Once-daily linagliptin was approved by the U.S. Food and Drug Administration (FDA) on 2 May 2011 for treatment of type 2 diabetes.[3] 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.[4]

Side effects

Linagliptin may cause severe joint pain.[1][5]

Mechanism of action

Linagliptin belongs to a class of drugs called DPP-4 inhibitors. They work by increasing hormones that stimulate pancreas to produce more insulin and stimulate your liver to produce less glucose. In other words, linagliptin, along with diet and exercise, can help the body produce more insulin and less sugar. Managing blood sugar can mean a lower HbA1c — that's an important goal for anyone with type 2 diabetes.

See also

References


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