pharmacopeia
GET
/api/v1/drug/linagliptin
2D structure
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
SMILES CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
InChIKey LTXREWYXXSTFRX-QGZVFWFLSA-N

Mechanism of action

Sourced from openFDA

Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation.

Dipeptidyl Peptidase 4

Indications

Sourced from openFDA
  • TRADJENTA is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus . TRADJENTA is a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus ( 1 ) Limitations of Use Not recommended in patients with type 1 diabetes mellitus as it would not be effective ( 1 ) Has not been studied in patients with a history of pancreatitis ( 1 ) Limitations of Use TRADJENTA is not recommended in patients with type 1 diabetes mellitus as it would not be effective.ICD-10: E10.9, E11.9

Contraindications

Sourced from openFDA
  • TRADJENTA is contraindicated in patients with hypersensitivity to linagliptin or any of the excipients in TRADJENTA, reactions such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity have occurred [see Warnings and Precautions (5.3) and Adverse Reactions (6) ].contraindicated

Dosage & administration

Sourced from openFDA

The recommended dosage of TRADJENTA is 5 mg orally once daily ( 2.1 ) TRADJENTA can be taken with or without food ( 2.1 ) 2.1 Recommended Dosage and Administration The recommended dosage of TRADJENTA is 5 mg taken orally once daily, with or without food.

Warnings & precautions

Sourced from openFDA

Pancreatitis: There have been reports of acute pancreatitis, including fatal pancreatitis. If pancreatitis is suspected, promptly discontinue TRADJENTA. ( 5.1 ) Hypoglycemia: Consider lowering the dosage of insulin secretagogue or insulin to reduce the risk of hypoglycemia when initiating TRADJENTA ( 5.2 ) Hypersensitivity reactions: Serious hypersensitivity reactions (e.g., anaphylaxis, angioedema, and exfoliative skin conditions) have occurred with TRADJENTA. If hypersensitivity reactions occur, discontinue TRADJENTA, treat promptly, and monitor until signs and symptoms resolve. ( 5.3 ) Arthralgia: Severe and disabling arthralgia has been reported in patients taking TRADJENTA. Consider as a possible cause for severe joint pain and discontinue drug if appropriate. ( 5.4 ) Bullous pemphigoid: There have been reports of bullous pemphigoid requiring hospitalization. Tell patients to report development of blisters or erosions. If bullous pemphigoid is suspected, discontinue TRADJENTA. ( 5.5 ) Heart failure: Heart failure has been observed with two other members of the DPP-4 inhibitor class. Consider risks and benefits of TRADJENTA in patients who have known risk factors for heart failure. Monitor for signs and symptoms. ( 5.6 ) 5.1 Pancreatitis Acute pancreatitis, including fatal pancreatitis, has been reported in patients treated with TRADJENTA. In the CARMELINA trial [see Clinical Studies (14.2) ] , acute pancreatitis was reported in 9 (0.3%) patients treated with TRADJENTA and in 5 (0.1%) patients treated with placebo.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are described below or elsewhere in the prescribing information: Pancreatitis [see Warnings and Precautions (5.1) ] Hypoglycemia with Concomitant Use with Insulin and Insulin Secretagogues [see Warnings and Precautions (5.2) ] Hypersensitivity Reactions [see Warnings and Precautions (5.3) ] Severe and Disabling Arthralgia [see Warnings and Precautions (5.4) ] Bullous Pemphigoid [see Warnings and Precautions (5.5) ] Heart Failure [see Warnings and Precautions (5.6) ] Most common adverse reaction (incidence ≥5% and more often than placebo) was nasopharyngitis ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Boehringer Ingelheim Pharmaceuticals, Inc. at 1-800-542-6257, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety evaluation of TRADJENTA 5 mg once daily in patients with type 2 diabetes mellitus is based on 14 placebo-controlled trials, 1 active-controlled trial, and one trial in patients with severe renal impairment. In the 14 placebo-controlled studies, a total of 3,625 patients were randomized and treated with TRADJENTA 5 mg daily and 2,176 with placebo. The mean exposure in patients treated with TRADJENTA across studies was 29.6 weeks. The maximum follow-up was 78 weeks.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary The limited data with TRADJENTA use in pregnant women are not sufficient to inform of drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy [see Clinical Considerations ]. In animal reproduction studies, no adverse developmental effects were observed when linagliptin was administered to pregnant rats during the period of organogenesis at doses similar to the maximum recommended clinical dose, based on exposure [see Data ] . The estimated background risk of major birth defects is 6% to 10% in women with pre-gestational diabetes with a HbA1c >7 and has been reported to be as high as 20% to 25% in women with HbA1c >10. The estimated background risk of miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, and delivery complications. Poorly controlled diabetes increases the fetal risk for major birth defects, stillbirth, and macrosomia related morbidity.

Pharmacokinetics

Sourced from openFDA
Metabolism
The pharmacokinetics of linagliptin has been characterized in healthy subjects and patients with type 2 diabetes mellitus. After oral administration of a single 5 mg dose to healthy subjects, peak plasma concentrations of linagliptin occurred at approximately 1.5 hours post dose (T max ); the mean plasma area under the curve (AUC) was 139 nmol*h/L and maximum concentration (C max ) was 8.9 nmol/L.

Overdosage

Sourced from openFDA

In the event of an overdose with TRADJENTA, consider contacting the Poison Help Line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations. Removal of linagliptin by hemodialysis or peritoneal dialysis is unlikely.

Approval history

Sourced from openFDA
  • May 2, 2011NDANDA201280Boehringer Ingelheim
  • Jan 30, 2012NDANDA201281Boehringer Ingelheim
  • Jan 30, 2015NDANDA206073Boehringer Ingelheim
  • May 27, 2016NDANDA208026Boehringer Ingelheim
  • Jan 27, 2020NDANDA212614Boehringer Ingelheim
  • Nov 3, 2025ANDAANDA208459Msn

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
20,890 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Blood Glucose Increased1,5997.7%
  2. 2Diarrhoea1,3706.6%
  3. 3Nausea1,3496.5%
  4. 4Fatigue1,1435.5%
  5. 5Dyspnoea1,0705.1%
  6. 6Dizziness1,0505.0%
  7. 7Off Label Use1,0485.0%
  8. 8Vomiting1,0344.9%
  9. 9Malaise8544.1%
  10. 10Headache8534.1%
  11. 11Acute Kidney Injury8324.0%
  12. 12Arthralgia8013.8%
  13. 13Pruritus7833.7%
  14. 14Drug Ineffective7663.7%
  15. 15Pyrexia7283.5%

Literature

View JSON

Recent PubMed references pinned to Linagliptin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 222 ClinicalTrials.gov registrations naming Linagliptin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Linagliptin work?
Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation.
What is Linagliptin used for?
According to FDA labeling, Linagliptin carries indications including: TRADJENTA is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus . TRADJENTA is a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus ( 1 ) Limitations of Use Not recommended in patients with type 1 diabetes mellitus as it would not be effective ( 1 ) Has not been studied in patients with a history of pancreatitis ( 1 ) Limitations of Use TRADJENTA is not recommended in patients with type 1 diabetes mellitus as it would not be effective.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Linagliptin?
Linagliptin is classified as Dipeptidyl peptidase 4 (DPP-4) inhibitors, Dipeptidyl Peptidase 4 Inhibitor, Dipeptidyl Peptidase 4 Inhibitors, Decreased Glucagon Secretion, Increased Insulin Secretion.
What are the brand names for Linagliptin?
Linagliptin is marketed under brand names including Glyxambi, Jentadueto, Tradjenta, Trijardy.
What are the contraindications for Linagliptin?
Linagliptin labeling lists contraindications including: TRADJENTA is contraindicated in patients with hypersensitivity to linagliptin or any of the excipients in TRADJENTA, reactions such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity have occurred [see Warnings and Precautions (5.3) and Adverse Reactions (6) ].. Always consult the full prescribing information and a clinician.
Note. Data for linagliptin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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