Linagliptin

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Linagliptin
Linagliptin.svg
Clinical data
Pronunciation /ˌlɪnəˈɡlɪptɪn/ LIN-ə-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
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability ~30% (Tmax = 1.5 hours)
Protein binding 75–99% (concentration-dependent)
Metabolism Minimal (~10% metabolized)
Metabolites Pharmacologically inactive
Elimination half-life ~24 hours
Excretion Feces (80%), urine (5%)[1]
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
Formula C25H28N8O2
Molar mass 472.54 g/mol
3D model (JSmol)
 NoYesY (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[edit]

Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.[4]

Side effects[edit]

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

The U.S. Food and Drug Administration (FDA) is warning that the type 2 diabetes medicines like sitagliptin, saxagliptin, linagliptin, and alogliptin may cause joint pain that can be severe and disabling. FDA has added a new Warning and Precaution about this risk to the labels of all medicines in this drug class, called dipeptidyl peptidase-4 (DPP-4) inhibitors.

Mechanism of action[edit]

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

See also[edit]

References[edit]

  1. ^ a b "Tradjenta (linagliptin) Tablets. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA. Retrieved 10 November 2016. 
  2. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 61" (PDF). World Health Organization. p. 66. Retrieved 10 November 2016. 
  3. ^ "FDA Approves Type 2 Diabetes Drug from Boehringer Ingelheim and Lilly". 3 May 2011. 
  4. ^ "Four Phase III Trials Confirm Benefits of BI's Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010. 
  5. ^ "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". FDA. 2015-08-28. Retrieved 1 September 2015. 
  • 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. 


External links[edit]