Linagliptin

Linagliptin, sold under the brand name Trajenta among others, is a medication used to treat diabetes mellitus type 2.[4][5] It is generally less preferred than metformin and sulfonylureas as an initial treatment.[4][6] It is used together with exercise and diet.[4] It is not recommended in type 1 diabetes.[4] It is taken by mouth.[4]

Linagliptin
Clinical data
Pronunciation/ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin
Trade namesTradjenta, Trajenta, others
Other namesBI-1356
AHFS/Drugs.comMonograph
MedlinePlusa611036
License data
Routes of
administration		By mouth (tablets)
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only) [1]
  • UK: POM (Prescription only)
  • US: ℞-only
  • EU: Rx-only [2]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability~30% (Tmax = 1.5 hours)
Protein binding75–99% (concentration-dependent)
MetabolismMinimal (~10% metabolized)
MetabolitesPharmacologically inactive
Elimination half-life~24 hours
ExcretionFeces (80%), urine (5%)[3]
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
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC25H28N8O2
Molar mass472.553 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
 NY (what is this?)  (verify)

Common side effects include inflammation of the nose and throat.[4] Serious side effects may include angioedema, pancreatitis, joint pain.[6][4] Use in pregnancy and breastfeeding is not recommended.[6] Linagliptin is a dipeptidyl peptidase-4 inhibitor.[4] It works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.[4]

Linagliptin was approved for medical use in the United States in 2011.[4] In 2018, it was the 177th most commonly prescribed medication in the United States, with more than 3 million prescriptions.[7][8] As of August 2021, linagliptin is available as a generic medicine in the US.[9]

Medical uses

Results in 2010, from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.[10]

Side effects

Linagliptin may cause severe joint pain.[3][11]

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. The 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[12] states the drug is contraindicated for people with bronchial hyperreactivity (for example, asthma).

Mechanism of action

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

Terminology

Linagliptin is the INN.[13]

See also

References
  1. "Pharmaceutical Benefits Scheme (PBS) | Linagliptin, tablet, 5 mg, Trajenta® - July 2012".
  2. "Trajenta EPAR". European Medicines Agency (EMA).
  3. "Tradjenta (linagliptin) Tablets. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA. Retrieved 10 November 2016.
  4. "Linagliptin Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 6 April 2019.
  5. Neumiller JJ (March 2012). "Pharmacology, efficacy, and safety of linagliptin for the treatment of type 2 diabetes mellitus". The Annals of Pharmacotherapy. 46 (3): 358–67. doi:10.1345/aph.1Q522. PMID 22318932.
  6. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN 9780857113382.
  7. "The Top 300 of 2021". ClinCalc. Retrieved 18 February 2021.
  8. "Linagliptin - Drug Usage Statistics". ClinCalc. Retrieved 18 February 2021.
  9. "Linagliptin: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 24 September 2021.
  10. "Four Phase III Trials Confirm Benefits of BI's Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010. Archived from the original on 10 March 2012.
  11. "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". U.S. Food and Drug Administration (FDA). 2015-08-28. Retrieved 1 September 2015.
  12. "Highlights of Prescribing Information: TRADJENTA (linagliptin tablets), for oral use" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc.
  13. "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 61" (PDF). World Health Organization. p. 66. Retrieved 10 November 2016.
  • "Linagliptin". Drug Information Portal. U.S. National Library of Medicine.
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