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What is Linagliptin?

Linagliptin is another common oral medication used in the treatment of Type-2 Diabetes. This DPP-4 inhibitor increases insulin production in the body and decreases glucagon production from the pancreas. Linagliptin is also known by the trade names Tradjenta and Trajenta. The drug is suitable for adults who have type-2 diabetes.

Product Description

Molar Mass: 472.553
SMILES: CC#CCn1c(nc2N(C)C(=O)N(Cc3nc(C)c4ccccc4n3)C(=O)c12)N5CCC[C@@H](N)C5
InChIKey: 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
ALogP: 1.15
Bioavailability: ~30% (Tmax = 1.5 hours)
Protein binding: 75–99% (concentration-dependent)
Metabolism: Minimal (~10% metabolized)
CAS Number: 66827-12-0
Chemical Formula: C25H28N8O2
Therapeutic Category: Antidiabetic
Form: Tablet
Assay: NLT 99.0%
Storage: Linaglitpin should be stored in a shady and dry place.
Suitable for: Adults
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. The chemical structure of Linaglitpin is shown below:

Approved Indications: 2

As per the clinical trials, there are majorly two approved indications of Linagliptin drug:
Diabetes Mellitus
Diabetes Mellitus, Type-2

Experimental Indications: 14

As per clinical trials 1-4, the drug can be used in the following categories:

  • Adenocarcinoma (Phase 2)
  • Albuminuria (Phase 4)
  • Carcinoma, Non-Small-Cell Lung (Phase 2)
  • Coronary Artery Disease (Phase 4)
  • Coronavirus Infections (Phase 4)
  • Diabetic Nephropathies (Phase 4)
  • Endocrine System Diseases (Phase 3)
  • Esophageal Neoplasms (Phase 2)
  • Hepatic Insufficiency (Phase 1)
  • Insulin Resistance (Phase 4)
  • Kidney Failure, Chronic (Phase 4)
  • Liver Failure (Phase 1)
  • Malnutrition (Phase 1)
  • Metabolic Diseases (Phase 3)
  • Myocardial Ischemia (Phase 4)
  • Osteoporosis (Phase 4)
  • Prediabetic State (Phase 4)
  • Renal Insufficiency (Phase 4)
  • Renal Insufficiency, Chronic (Phase 4)
  • Respiratory Tract Diseases (Phase 3)
  • Schizophrenia (Phase 4)
  • Severe Acute Respiratory Syndrome (Phase 4)

Clinical Trials:

A total of 160 clinical trials have been held for the Linagliptin drug. 86 Companies took part in these trials, which were carried out in four phases.

Side Effects:

A few common side effects may be seen while interacting with Linagliptin. Those are:

  • Angioedema
  • Pancreatitis
  • Joint Pain

Besides that, the use of Linagliptin during pregnancy, breastfeeding, and asthma is also not recommended.


Linagliptin is a robust gliptin salt readily used to treat Type-2 Diabetes. Decreasing the sugar production in your liver also eliminates kidney, liver, and eyesight failure issues. Linagliptin has a molar mass of 472.553 g·mol−1 and is to be taken in oral tablet form with a 5 mg dosage per day. You may experience side effects like joint pain, pancreatitis, and angioedema with Linagliptin.

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