Linagliptin 5mg tablets
Requires a prescription from a doctor or prescriber
Linagliptin is a DPP-4 inhibitor developed by Boehringer Ingelheim for the treatment of type II diabetes [L9557].
Official documents, adverse reaction reporting, and safety monitoring
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Official medicine documents
Safety monitoring data
Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Linagliptin
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Submit a Yellow Card report to the MHRA
Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
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Suspected adverse reactions reported for Linagliptin
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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
4 branded products available
MHRA licensed products
View all licensed products for Linagliptin on the MHRA register
Trajenta 5mg tablets
Trajenta 5mg tablets
Trajenta 5mg tablets
This is the NHS Drug Tariff indicative price used for reimbursement purposes. It may not reflect the price paid by patients or pharmacies.
View full Drug TariffSource: NHS Drug Tariff via NHSBSA. Derived from dm+d VMPP (Virtual Medicinal Product Pack) pricing data. Contains public sector information licensed under the Open Government Licence v3.0.
WHO defined daily dose (DDD)
5 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via the NHS dm+d supplementary BNF/ATC mapping files (NHSBSA). Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Guidelines from the National Institute for Health and Care Excellence
NICE clinical guidance(1)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Supply & safety information
Official UK regulator monitoring and safety alerts
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Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF code shown is the factual mapping value distributed by NHS Business Services Authority (NHSBSA) in the dm+d supplementary file under OGL v3.0; it is not affiliated with, nor licensed from, the publishers of the British National Formulary. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing the 50 most relevant studies.
Reviews & meta-analyses: 6 · Randomised trials: 29 · 2010–2026
Showing the 50 most relevant studies, sorted by most relevant.
Odd Erik Johansen, Dietmar Neubacher, Maximilian von Eynatten, et al.
Cardiovascular Diabetology, 2012
- Linagliptin
- Angina, Unstable
- Blood Glucose
Baptist Gallwitz, Julio Rosenstock, T. Rauch, et al.
The Lancet, 2012
- Linagliptin
- Blood Glucose
- Diabetes Mellitus, Type 2
Stefano Del Prato, Anthony Barnett, Holger Huisman, et al.
Diabetes Obesity and Metabolism, 2010
- Linagliptin
- Diabetes Mellitus, Type 2
- Glycated Hemoglobin
Per‐Henrik Groop, Mark E. Cooper, Vlado Perkovic, et al.
Diabetes Obesity and Metabolism, 2017
- Linagliptin
- Albuminuria
- Blood Glucose
Lori M. Laffel, Thomas Danne, Georgeanna J. Klingensmith, et al.
The Lancet Diabetes & Endocrinology, 2023
- Sodium-Glucose Transporter 2 Inhibitors
- Diabetes Mellitus, Type 2
- Hypoglycemia
Anthony Barnett, Holger Huisman, Russell Jones, et al.
The Lancet, 2013
- Linagliptin
- Analysis of Variance
- Blood Glucose
Eirik Søfteland, Juris J. Meier, Bente Vangen, et al.
Diabetes Care, 2016
- Linagliptin
- Benzhydryl Compounds
- Diabetes Mellitus, Type 2
Hadir Aljohani, Fares S Alrubaish, Waad Alghamdi, et al.
Therapeutic Innovation & Regulatory Science, 2024
Panda PS, Mohapatra I, Padhee S, et al.
2025
Geert Jan Biessels, C. Verhagen, Jolien Janssen, et al.
Diabetes Care, 2019
- Linagliptin
- Blood Glucose
- Cardiovascular Diseases
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
155 hours
Mechanism
Linagliptin is a competitive, reversible DPP-4 inhibitor.
Food interactions
2 warnings
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
30%
[A37050]
Half-life
155 hours
[A176948]
Protein binding
99%
[A37050]
Volume of distribution
5mg
[A37050]…
Metabolism
90%
[A176948]…
Elimination
84.7%
[A176948][A37050]
Clearance
374mL/min
[A176948]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
[L9557]
It should not be used to treat type I diabetes or in diabetic ketoacidosis.
[L9557]
An extended-release combination product containing empagliflozin, linagliptin, and metformin was approved by the FDA in January 2020 for the improvement of glycemic control in adults with type 2 diabetes mellitus when used adjunctively with diet and exercise.
[L11479]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 1457 interactions
[A37050]
Studies of efficacy and safety in pediatric populations were not included in the original drug approval[L9557] but recent clinical trials show linagliptin to be well tolerated in patients 10 to 18 years old.
[A176960]
Animal studies showed an increased risk of lymphoma in female rats at over 200 times the clinical dose.
[L9557]
Aside from this effect, linagliptin was not shown to be mutagenic, clastogenic, or have an effect on fertility.
[L9557]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[A37050]
[A176948]
[A37050]
[A37050]
However an intravenous infusion of 0.5-10mg results in a volume of distribution of 380-1540L.
[A37050]
[A176948]
90% of an oral dose is excreted unchanged in the urine and feces.
[A176948][A37050]
The predominant metabolite in the plasma is CD1790 and the predominant metabolite recovered after excretion was M489(1).
[A176948]
Other metabolites are produced through oxidation, oxidative degradation, N-acetylation, glucuronidation, and cysteine adduct formation.
[A176948]
Other metabolites have been identified through mass spectrometry though no structures were determined.
[A176948]
Metabolism of linagliptin is mediated by cytochrome P450 3A4, aldo-keto reductases, and carbonyl reductases.
[A176948]
[A176948][A37050]
[A176948]
Proteins and enzymes this drug interacts with in the body
PMID:10900005 PMID:10951221 PMID:11772392 PMID:17287217
Acts as a positive regulator of T-cell coactivation, by binding at least ADA, CAV1, IGF2R, and PTPRC .
PMID:10900005 PMID:10951221 PMID:11772392 PMID:14691230
Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor/CD3-dependent manner .
PMID:17287217
Its interaction with ADA also regulates lymphocyte-epithelial cell adhesion .
PMID:11772392
In association with FAP is involved in the pericellular proteolysis of the extracellular matrix (ECM), the migration and invasion of endothelial cells into the ECM .
PMID:10593948 PMID:16651416
May be involved in the promotion of lymphatic endothelial cells adhesion, migration and tube formation .
PMID:18708048
When overexpressed, enhanced cell proliferation, a process inhibited by GPC3 .
PMID:17549790
Also acts as a serine exopeptidase with a dipeptidyl peptidase activity that regulates various physiological processes by cleaving peptides in the circulation, including many chemokines, mitogenic growth factors, neuropeptides and peptide hormones such as brain natriuretic peptide 32 .
PMID:10570924 PMID:16254193
Removes N-terminal dipeptides sequentially from polypeptides having unsubstituted N-termini provided that the penultimate residue is proline PMID:10593948
Enzymes involved in drug metabolism — important for understanding drug interactions
Proteins that transport this drug across cell membranes
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
PMID:11388889 PMID:11408531 PMID:12439218 PMID:12719534 PMID:15389554 PMID:16263091 PMID:16272756 PMID:16581093 PMID:19536068 PMID:21128598 PMID:23680637 PMID:24961373 PMID:34040533 PMID:9187257 PMID:9260930 PMID:9655880
Functions as a pH- and Na(+)-independent, bidirectional transporter (By similarity). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (By similarity). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity).
Primarily expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (By similarity). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal elimination of organic cations from the systemic circulation .
PMID:16263091
Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline .
PMID:12439218 PMID:24961373 PMID:35469921 PMID:9260930
Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover .
PMID:21128598
Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism .
PMID:24961373
Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium .
PMID:15817714
Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency .
PMID:17460754
Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID:11907186
May contribute to the transport of cationic compounds in testes across the blood-testis-barrier (Probable). Also involved in the uptake of xenobiotics tributylmethylammonium (TBuMA), quinidine, N-methyl-quinine (NMQ), N-methyl-quinidine (NMQD) N-(4,4-azo-n-pentyl)-quinuclidine (APQ), azidoprocainamide methoiodide (AMP), N-(4,4-azo-n-pentyl)-21-deoxyajmalinium (APDA) and 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) PMID:11408531 PMID:15389554 PMID:35469921 PMID:9260930
PMID:9260930 PMID:9687576
Functions as a Na(+)-independent, bidirectional uniporter .
PMID:21128598 PMID:9687576
Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient .
PMID:15212162 PMID:9260930 PMID:9687576
However, may also engage electroneutral cation exchange when saturating concentrations of cation substrates are reached (By similarity). Predominantly expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow .
PMID:15783073
Implicated in monoamine neurotransmitters uptake such as histamine, dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, serotonin and tyramine, thereby supporting a physiological role in the central nervous system by regulating interstitial concentrations of neurotransmitters .
PMID:16581093 PMID:17460754 PMID:9687576
Also capable of transporting dopaminergic neuromodulators cyclo(his-pro), salsolinol and N-methyl-salsolinol, thereby involved in the maintenance of dopaminergic cell integrity in the central nervous system .
PMID:17460754
Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium .
PMID:15817714
Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) .
PMID:12089365 PMID:15212162 PMID:17072098 PMID:24961373 PMID:9260930
Mediates the uptake and efflux of quaternary ammonium compound choline .
PMID:9260930
Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine .
PMID:12538837 PMID:21128598
Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID:11907186
Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) .
PMID:12395288 PMID:16394027
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
PMID:10196521 PMID:10966924 PMID:12538837 PMID:17460754 PMID:20858707
Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient .
PMID:10966924
Functions as a Na(+)- and Cl(-)-independent, bidirectional uniporter .
PMID:12538837
Implicated in monoamine neurotransmitters uptake such as dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, histamine, serotonin and tyramine, thereby supporting a role in homeostatic regulation of aminergic neurotransmission in the brain .
PMID:10196521 PMID:16581093 PMID:20858707
Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with low efficiency .
PMID:17460754
May be involved in the uptake and disposition of cationic compounds by renal clearance from the blood flow .
PMID:10966924
May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable). Mediates the transport of polyamine spermidine and putrescine (By similarity). Mediates the bidirectional transport of polyamine agmatine .
PMID:12538837
Also transports guanidine .
PMID:10966924
May also mediate intracellular transport of organic cations, thereby playing a role in amine metabolism and intracellular signaling (By similarity)
ATC A10BH05
ATC A10BD19
ATC A10BD11
ATC A10BD27
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Linagliptin
Additional database identifiers
Drugs Product Database (DPD)
20882
ChemSpider
8271879
BindingDB
50228403
PDB
356
ZINC
ZINC000003820029
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3009
GenAtlas
DPP4
GeneCards
DPP4
GenBank Gene Database
U13735
GenBank Protein Database
535388
Guide to Pharmacology
1612
UniProt Accession
DPP4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10963
GeneCards
SLC22A1
GenBank Gene Database
X98332
GenBank Protein Database
2511670
Guide to Pharmacology
1019
UniProt Accession
S22A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10966
GeneCards
SLC22A2
GenBank Gene Database
X98333
GenBank Protein Database
2281942
Guide to Pharmacology
1020
UniProt Accession
S22A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10967
GeneCards
SLC22A3
GenBank Gene Database
AJ001417
GenBank Protein Database
3581982
Guide to Pharmacology
1021
UniProt Accession
S22A3_HUMAN
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
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Structured knowledge from the free knowledge base
ATC classifications (Wikidata)
Linked open data from Wikidata (Q909745), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication. WHO INN from the World Health Organization.