Linagliptin

Linagliptin
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)
     ☒N☑Y (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]

    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.

    Trajenta's Prescribing Information[6] states the drug is contraindicated for people with bronchial hyperreactivity. Asthma is a form of bronchial hyperreactivity[7].

    Mechanism of action

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

    See also

    References

    1. 1 2 "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.
    6. ↑ https://docs.boehringer-ingelheim.com/Prescribing%20Information/PIs/Tradjenta/Tradjenta.pdf?DMW_FORMAT=pdf)
    7. ↑ https://en.wikipedia.org/wiki/Bronchial_hyperresponsiveness
    • 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.


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