Identification
- Summary
Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor used to manage hyperglycemia in patients with type 2 diabetes mellitus.
- Brand Names
- Glyxambi, Jentadueto, Tradjenta, Trajenta, Trijardy
- Generic Name
- Linagliptin
- DrugBank Accession Number
- DB08882
- Background
Linagliptin is a DPP-4 inhibitor developed by Boehringer Ingelheim for the treatment of type II diabetes 5. Linagliptin differs from other DPP-4 inhibitors in that it has a non-linear pharmacokinetic profile, is not primarily eliminated by the renal system, and obeys concentration dependant protein binding3. Linagliptin was approved by the FDA on May 2, 20115.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Linagliptin (DB08882)
- Weight
- Average: 472.5422
Monoisotopic: 472.23352218 - Chemical Formula
- C25H28N8O2
- Synonyms
- (R)-8-(3-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methylquinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione
- Linagliptin
- Linagliptina
- External IDs
- BI 1356
- BI 1356 BS
- BI-1356
- BI-1356-BS
- BI-1356BS
- BS 1356 BS
- BS-1356-BS
Pharmacology
- Indication
Linagliptin is indicated for the treatment of type II diabetes in addition to diet and exercise5. It should not be used to treat type I diabetes or in diabetic ketoacidosis.5 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.6
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used as adjunct in combination to manage Type 2 diabetes mellitus Combination Product in combination with: Empagliflozin (DB09038) •••••••••••• ••••• •••••• Used as adjunct in combination to manage Type 2 diabetes mellitus Combination Product in combination with: Empagliflozin (DB09038), Metformin (DB00331) •••••••••••• ••••• ••••••• •••••••• ••••••• Used as adjunct in combination to manage Type 2 diabetes mellitus Combination Product in combination with: Metformin (DB00331) •••••••••••• ••••• Management of Type 2 diabetes mellitus •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
A 5mg oral dose of linagliptin results in >80% inhibition of dipeptidyl peptidase 4 (DPP-4) for ≥24 hours3. Inhibition of DPP-4 increases the concentration of glucagon-like peptide 1 (GLP-1), leading to decreased glycosylated hemoglobin and fasting plasma glucose3.
- Mechanism of action
Linagliptin is a competitive, reversible DPP-4 inhibitor. Inhibition of this enzyme slows the breakdown of GLP-1 and glucose-dependant insulinotropic polypeptide (GIP)3,5. GLP-1 and GIP stimulate the release of insulin from beta cells in the pancreas while inhibiting release of glucagon from pancreatic beta cells5. These effects together reduce the breakdown of glycogen in the liver and increase insulin release in response to glucose53.
Target Actions Organism ADipeptidyl peptidase 4 inhibitorHumans - Absorption
Oral bioavailability of linagliptin is 30%3.
- Volume of distribution
A single intravenous dose of 5mg results in a volume of distribution of 1110L3. However an intravenous infusion of 0.5-10mg results in a volume of distribution of 380-1540L3.
- Protein binding
Linagliptin is 99% protein bound at a concentration of 1nmol/L and 75-89% protein bound at a concentration of >30nmol/L3.
- Metabolism
An oral dose of linagliptin is excreted primarily in the feces2. 90% of an oral dose is excreted unchanged in the urine and feces2,3. The predominant metabolite in the plasma is CD1790 and the predominant metabolite recovered after excretion was M489(1)2. Other metabolites are produced through oxidation, oxidative degradation, N-acetylation, glucuronidation, and cysteine adduct formation2. Other metabolites have been identified through mass spectrometry though no structures were determined2. Metabolism of linagliptin is mediated by cytochrome P450 3A4, aldo-keto reductases, and carbonyl reductases2.
Hover over products below to view reaction partners
- Route of elimination
84.7% of linagliptin is eliminated in the feces and 5.4% is eliminated in the urine2,3.
- Half-life
The terminal half life of linagliptin is 155 hours2.
- Clearance
Total clearance of linagliptin is 374mL/min2.
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
No dosage adjustment is necessary based on race, age, weight, sex, renal impairment, or hepatic impairment3.
Studies of efficacy and safety in pediatric populations were not included in the original drug approval5 but recent clinical trials show linagliptin to be well tolerated in patients 10 to 18 years old4.
Animal studies showed an increased risk of lymphoma in female rats at over 200 times the clinical dose5. Aside from this effect, linagliptin was not shown to be mutagenic, clastogenic, or have an effect on fertility5.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be decreased when combined with Linagliptin. Abametapir The serum concentration of Linagliptin can be increased when it is combined with Abametapir. Abatacept The metabolism of Linagliptin can be increased when combined with Abatacept. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Linagliptin. Abiraterone The metabolism of Linagliptin can be decreased when combined with Abiraterone. - Food Interactions
- Avoid excessive or chronic alcohol consumption. Chronic or binge drinking can increase the risk of serious side effects.
- Take with or without food. High fat meals reduce the maximum concentration and increase the AUC, but not to a clinically significant extent.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Images
- International/Other Brands
- Tradjenta
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Tradjenta Tablet, film coated 5 mg/1 Oral A-S Medication Solutions 2011-05-09 Not applicable US 
Tradjenta Tablet, film coated 5 mg/1 Oral Cardinal Health 107, LLC 2011-05-09 Not applicable US 
Tradjenta Tablet, film coated 5 mg/1 Oral Boehringer Ingelheim Pharmaceuticals, Inc. 2011-05-09 Not applicable US 
Trajenta Tablet, film coated 5 mg Oral Boehringer Ingelheim 2016-09-08 Not applicable EU 
Trajenta Tablet, film coated 5 mg Oral Boehringer Ingelheim 2016-09-08 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image GLYXAMBI Linagliptin (5 MG) + Empagliflozin (10 MG) Tablet, film coated Oral Boehringer Ingelheim International Gmbh 2017-03-10 Not applicable Italy 
Glyxambi Linagliptin (5 mg) + Empagliflozin (25 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU GLYXAMBI Linagliptin (5 MG) + Empagliflozin (10 MG) Tablet, film coated Oral Boehringer Ingelheim International Gmbh 2017-03-10 Not applicable Italy Glyxambi Linagliptin (5 mg) + Empagliflozin (25 mg) Tablet, film coated Oral Boehringer Ingelheim 2020-12-16 Not applicable EU GLYXAMBI Linagliptin (5 MG) + Empagliflozin (25 MG) Tablet, film coated Oral Boehringer Ingelheim International Gmbh 2017-03-10 Not applicable Italy
Categories
- ATC Codes
- A10BH05 — Linagliptin
- A10BH — Dipeptidyl peptidase 4 (DPP-4) inhibitors
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- A10BD — Combinations of oral blood glucose lowering drugs
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- A10BD — Combinations of oral blood glucose lowering drugs
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Agents causing angioedema
- Alimentary Tract and Metabolism
- Blood Glucose Lowering Agents
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (moderate)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- DPP-IV Inhibitors
- Drugs Used in Diabetes
- Enzyme Inhibitors
- Heterocyclic Compounds, Fused-Ring
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Incretins
- OCT1 inhibitors
- OCT2 Inhibitors
- OCT2 Substrates
- Oral Hypoglycemics
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Protease Inhibitors
- Purines
- Quinazolines
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as xanthines. These are purine derivatives with a ketone group conjugated at carbons 2 and 6 of the purine moiety.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Imidazopyrimidines
- Sub Class
- Purines and purine derivatives
- Direct Parent
- Xanthines
- Alternative Parents
- Quinazolines / 6-oxopurines / Alkaloids and derivatives / Dialkylarylamines / Pyrimidones / Aminopiperidines / Aminoimidazoles / N-substituted imidazoles / Benzenoids / Vinylogous amides show 9 more
- Substituents
- 3-aminopiperidine / 6-oxopurine / Alkaloid or derivatives / Amine / Aminoimidazole / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Dialkylarylamine show 22 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- aminopiperidine, quinazolines (CHEBI:68610)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 3X29ZEJ4R2
- CAS number
- 668270-12-0
- InChI Key
- LTXREWYXXSTFRX-QGZVFWFLSA-N
- InChI
- 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
- IUPAC Name
- 8-[(3R)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,3,6,7-tetrahydro-1H-purine-2,6-dione
- SMILES
- CC#CCN1C(=NC2=C1C(=O)N(CC1=NC3=C(C=CC=C3)C(C)=N1)C(=O)N2C)N1CCC[C@@H](N)C1
References
- Synthesis Reference
Pietro ALLEGRINI, Emanuele ATTOLINO, Marco ARTICO, "PROCESS FOR THE PREPARATION OF LINAGLIPTIN." U.S. Patent US20120165525, issued June 28, 2012.
US20120165525- General References
- Forst T, Pfutzner A: Linagliptin, a dipeptidyl peptidase-4 inhibitor with a unique pharmacological profile, and efficacy in a broad range of patients with type 2 diabetes. Expert Opin Pharmacother. 2012 Jan;13(1):101-10. doi: 10.1517/14656566.2012.642863. [Article]
- Blech S, Ludwig-Schwellinger E, Grafe-Mody EU, Withopf B, Wagner K: The metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin, in humans. Drug Metab Dispos. 2010 Apr;38(4):667-78. doi: 10.1124/dmd.109.031476. Epub 2010 Jan 19. [Article]
- Graefe-Mody U, Retlich S, Friedrich C: Clinical pharmacokinetics and pharmacodynamics of linagliptin. Clin Pharmacokinet. 2012 Jul 1;51(7):411-27. doi: 10.2165/11630900-000000000-00000. [Article]
- Tamborlane WV, Laffel LM, Weill J, Gordat M, Neubacher D, Retlich S, Hettema W, Hoesl CE, Kaspers S, Marquard J: Randomized, double-blind, placebo-controlled dose-finding study of the dipeptidyl peptidase-4 inhibitor linagliptin in pediatric patients with type 2 diabetes. Pediatr Diabetes. 2018 Jun;19(4):640-648. doi: 10.1111/pedi.12616. Epub 2017 Nov 24. [Article]
- FDA Approved Drug Products: Linagliptin Oral Tablets [Link]
- FDA Approved Drug Products: Trijardy XR (empagliflozin/linagliptin/metformin) extended-release tablets [Link]
- FDA Approved Drug Products: Linagliptin Oral Tablets (2022) [Link]
- External Links
- KEGG Drug
- D09566
- PubChem Compound
- 10096344
- PubChem Substance
- 175427132
- ChemSpider
- 8271879
- BindingDB
- 50228403
- 1100699
- ChEBI
- 68610
- ChEMBL
- CHEMBL237500
- ZINC
- ZINC000003820029
- PDBe Ligand
- 356
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Linagliptin
- PDB Entries
- 2rgu / 6y0f
- FDA label
- Download (353 KB)
- MSDS
- Download (104 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Type 2 Diabetes Mellitus 1 4 Completed Basic Science Schizophrenia 1 4 Completed Basic Science Type 2 Diabetes Mellitus 2 4 Completed Prevention Impaired Glucose Tolerance / Resistance, Insulin 2 4 Completed Prevention Renal Failure, Chronic Renal Failure / Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 10.00 mg Tablet, film coated Oral 25.00 mg Tablet Oral Tablet, film coated Oral Tablet, film coated, extended release Oral Tablet, film coated Oral 5 MG Tablet, film coated Oral 5 mg/1 Tablet Oral 5 mg Tablet, film coated Oral Tablet, film coated Oral 5.000 mg Tablet Oral 5.000 mg Tablet, coated Oral 500000 mg Tablet, extended release Oral Tablet, coated Oral Tablet, coated Oral 5 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2435730 No 2011-03-29 2022-02-21 Canada 
CA2496249 No 2012-01-24 2023-08-18 Canada US7407955 Yes 2008-08-05 2025-11-02 US US6340475 No 2002-01-22 2016-09-19 US US6635280 No 2003-10-21 2016-09-19 US US6488962 No 2002-12-03 2020-06-20 US US6303661 No 2001-10-16 2017-04-24 US US6890898 No 2005-05-10 2019-02-02 US US7078381 No 2006-07-18 2019-02-02 US US7459428 No 2008-12-02 2019-02-02 US US8119648 No 2012-02-21 2023-08-12 US US8178541 No 2012-05-15 2023-08-12 US US8846695 Yes 2014-09-30 2030-12-04 US US9173859 Yes 2015-11-03 2027-11-04 US US8853156 Yes 2014-10-07 2031-09-05 US US8673927 Yes 2014-03-18 2027-11-04 US US8883805 Yes 2014-11-11 2026-05-26 US US9155705 Yes 2015-10-13 2030-11-21 US US8551957 Yes 2013-10-08 2030-04-14 US US7713938 Yes 2010-05-11 2027-10-15 US US7579449 Yes 2009-08-25 2029-02-01 US US9486526 Yes 2016-11-08 2030-02-05 US US9415016 Yes 2016-08-16 2029-10-02 US US9555001 Yes 2017-01-31 2033-09-06 US US9949998 Yes 2018-04-24 2034-12-11 US US10034877 Yes 2018-07-31 2030-02-05 US US10022379 Yes 2018-07-17 2029-10-02 US US10258637 Yes 2019-04-16 2034-10-03 US US10406172 No 2019-09-10 2030-06-15 US US10596120 Yes 2020-03-24 2032-09-07 US US10973827 Yes 2021-04-13 2029-10-02 US US11090323 Yes 2021-08-17 2034-10-03 US US11033552 Yes 2021-06-15 2027-11-04 US US11564886 No 2012-03-07 2032-03-07 US US11833166 No 2014-04-03 2034-04-03 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 190-196 http://www.chemspider.com/Chemical-Structure.8271879.html?rid=e059df1a-34ab-48c0-9c24-9d6c4d699c47&page_num=0 water solubility <1 mg/mL MSDS - Predicted Properties
Property Value Source Water Solubility 0.0502 mg/mL ALOGPS logP 2.62 ALOGPS logP 2.8 Chemaxon logS -4 ALOGPS pKa (Strongest Basic) 9.86 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 113.48 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 133.43 m3·mol-1 Chemaxon Polarizability 51.24 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9513 Caco-2 permeable - 0.5842 P-glycoprotein substrate Substrate 0.774 P-glycoprotein inhibitor I Inhibitor 0.5185 P-glycoprotein inhibitor II Non-inhibitor 0.7716 Renal organic cation transporter Non-inhibitor 0.6658 CYP450 2C9 substrate Non-substrate 0.803 CYP450 2D6 substrate Non-substrate 0.7335 CYP450 3A4 substrate Substrate 0.7013 CYP450 1A2 substrate Non-inhibitor 0.9273 CYP450 2C9 inhibitor Non-inhibitor 0.8474 CYP450 2D6 inhibitor Non-inhibitor 0.9176 CYP450 2C19 inhibitor Non-inhibitor 0.8163 CYP450 3A4 inhibitor Non-inhibitor 0.5548 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8562 Ames test Non AMES toxic 0.5444 Carcinogenicity Non-carcinogens 0.8587 Biodegradation Not ready biodegradable 0.9966 Rat acute toxicity 2.7553 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6109 hERG inhibition (predictor II) Inhibitor 0.8116
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 203.0022 predictedDeepCCS 1.0 (2019) [M+H]+ 205.39778 predictedDeepCCS 1.0 (2019) [M+Na]+ 211.59209 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Virus receptor activity
- Specific Function
- Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by bindi...
- Gene Name
- DPP4
- Uniprot ID
- P27487
- Uniprot Name
- Dipeptidyl peptidase 4
- Molecular Weight
- 88277.935 Da
References
- Forst T, Pfutzner A: Linagliptin, a dipeptidyl peptidase-4 inhibitor with a unique pharmacological profile, and efficacy in a broad range of patients with type 2 diabetes. Expert Opin Pharmacother. 2012 Jan;13(1):101-10. doi: 10.1517/14656566.2012.642863. [Article]
- Nadkarni P, Chepurny OG, Holz GG: Regulation of glucose homeostasis by GLP-1. Prog Mol Biol Transl Sci. 2014;121:23-65. doi: 10.1016/B978-0-12-800101-1.00002-8. [Article]
- Gallwitz B: Novel Therapeutic Approaches in Diabetes. Endocr Dev. 2016;31:43-56. doi: 10.1159/000439372. Epub 2016 Jan 19. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Blech S, Ludwig-Schwellinger E, Grafe-Mody EU, Withopf B, Wagner K: The metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin, in humans. Drug Metab Dispos. 2010 Apr;38(4):667-78. doi: 10.1124/dmd.109.031476. Epub 2010 Jan 19. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- Curator comments
- Linagliptin is a p-gp inhibitor at higher doses.
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Graefe-Mody U, Retlich S, Friedrich C: Clinical pharmacokinetics and pharmacodynamics of linagliptin. Clin Pharmacokinet. 2012 Jul 1;51(7):411-27. doi: 10.2165/11630900-000000000-00000. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Secondary active organic cation transmembrane transporter activity
- Specific Function
- Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- Graefe-Mody U, Retlich S, Friedrich C: Clinical pharmacokinetics and pharmacodynamics of linagliptin. Clin Pharmacokinet. 2012 Jul 1;51(7):411-27. doi: 10.2165/11630900-000000000-00000. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Quaternary ammonium group transmembrane transporter activity
- Specific Function
- Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- Graefe-Mody U, Retlich S, Friedrich C: Clinical pharmacokinetics and pharmacodynamics of linagliptin. Clin Pharmacokinet. 2012 Jul 1;51(7):411-27. doi: 10.2165/11630900-000000000-00000. [Article]
- Ishiguro N, Shimizu H, Kishimoto W, Ebner T, Schaefer O: Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. Drug Metab Dispos. 2013 Jan;41(1):149-58. doi: 10.1124/dmd.112.048470. Epub 2012 Oct 16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Toxin transporter activity
- Specific Function
- Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
- Gene Name
- SLC22A3
- Uniprot ID
- O75751
- Uniprot Name
- Solute carrier family 22 member 3
- Molecular Weight
- 61279.485 Da
References
- Graefe-Mody U, Retlich S, Friedrich C: Clinical pharmacokinetics and pharmacodynamics of linagliptin. Clin Pharmacokinet. 2012 Jul 1;51(7):411-27. doi: 10.2165/11630900-000000000-00000. [Article]
Drug created at May 21, 2013 22:46 / Updated at February 20, 2024 23:55