Identification

Name
Linagliptin
Accession Number
DB08882
Description

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
Thumb
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

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
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.

TargetActionsOrganism
ADipeptidyl peptidase 4
inhibitor
Humans
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
Learn about our commercial Adverse Effects data.
Learn More
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.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
AbametapirThe serum concentration of Linagliptin can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Linagliptin can be increased when combined with Abatacept.
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Linagliptin.
AcalabrutinibThe metabolism of Linagliptin can be decreased when combined with Acalabrutinib.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Linagliptin.
AcebutololThe therapeutic efficacy of Acebutolol can be increased when used in combination with Linagliptin.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Linagliptin.
AcetaminophenThe metabolism of Linagliptin can be increased when combined with Acetaminophen.
AcetazolamideThe therapeutic efficacy of Linagliptin can be increased when used in combination with Acetazolamide.
AcetohexamideLinagliptin may increase the hypoglycemic activities of Acetohexamide.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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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

Product Images
International/Other Brands
Tradjenta
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
TradjentaTablet, film coated5 mg/1OralA-S Medication Solutions2011-05-09Not applicableUS flag
TradjentaTablet, film coated5 mg/1OralCardinal Health2011-05-09Not applicableUS flag00597 0140 30 nlmimage10 ed3d76cb
TradjentaTablet, film coated5 mg/1OralBoehringer Ingelheim Pharmaceuticals, Inc.2011-05-09Not applicableUS flag0597 014020180907 15195 v9gh0y
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEU flag
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEU flag
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEU flag
TrajentaTabletOralBoehringer Ingelheim (Canada) Ltd Ltee2011-09-13Not applicableCanada flag
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEU flag
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEU flag
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEU flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
GlyxambiLinagliptin (5 mg/1) + Empagliflozin (10 mg/1)Tablet, film coatedOralBoehringer Ingelheim Pharmaceuticals, Inc.2015-01-30Not applicableUS flag0597 018220180913 8702 q7fevz
GlyxambiLinagliptin (5 mg) + Empagliflozin (25 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-12-21Not applicableCanada flag
GlyxambiLinagliptin (5 mg/1) + Empagliflozin (10 mg/1)Tablet, film coatedOralREMEDYREPACK INC.2019-04-29Not applicableUS flag
GlyxambiLinagliptin (5 mg) + Empagliflozin (10 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-12-21Not applicableCanada flag
GlyxambiLinagliptin (5 mg/1) + Empagliflozin (25 mg/1)Tablet, film coatedOralBoehringer Ingelheim Pharmaceuticals, Inc.2015-01-30Not applicableUS flag
JentaduetoLinagliptin (2.5 mg) + Metformin hydrochloride (850 mg)Tablet, film coatedOralBoehringer Ingelheim2012-07-20Not applicableEU flag
JentaduetoLinagliptin (2.5 mg) + Metformin hydrochloride (1000 mg)Tablet, film coatedOralBoehringer Ingelheim2012-07-20Not applicableEU flag
JentaduetoLinagliptin (2.5 mg) + Metformin hydrochloride (850 mg)Tablet, film coatedOralBoehringer Ingelheim2012-07-20Not applicableEU flag
JentaduetoLinagliptin (2.5 mg) + Metformin hydrochloride (500 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2013-04-17Not applicableCanada flag
JentaduetoLinagliptin (2.5 mg/1) + Metformin hydrochloride (1000 mg/1)Tablet, film coatedOralbryant ranch prepack2012-02-13Not applicableUS flag

Categories

ATC Codes
A10BH05 — LinagliptinA10BD19 — Linagliptin and empagliflozinA10BD11 — Metformin and linagliptin
Drug Categories
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)

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[[email protected]@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
  1. 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. [PubMed:22149370]
  2. 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. [PubMed:20086031]
  3. 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. [PubMed:22568694]
  4. 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. [PubMed:29171139]
  5. FDA Approved Drug Products: Linagliptin Oral Tablets [Link]
  6. FDA Approved Drug Products: Trijardy XR (empagliflozin/linagliptin/metformin) extended-release tablets [Link]
KEGG Drug
D09566
PubChem Compound
10096344
PubChem Substance
175427132
ChemSpider
8271879
BindingDB
50228403
RxNav
1100699
ChEBI
68610
ChEMBL
CHEMBL237500
ZINC
ZINC000003820029
PDBe Ligand
356
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Linagliptin
AHFS Codes
  • 68:20.05 — Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
PDB Entries
2rgu
FDA label
Download (353 KB)
MSDS
Download (104 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentType II Diabetes in Subjects BMI 27 to 321
4CompletedBasic ScienceType 2 Diabetes Mellitus2
4CompletedPreventionChronic Renal Failure (CRF) / Type 2 Diabetes Mellitus1
4CompletedPreventionImpaired Glucose Tolerance / Insulin Resistance / Prediabetic State1
4CompletedPreventionInsulin Resistance / Prediabetic State1
4CompletedTreatmentCoronary Artery Disease (CAD) / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes1
4CompletedTreatmentDiabetes Mellitus1
4CompletedTreatmentImpaired kidney function / Type 2 Diabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus8

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral10 MG
Tablet, film coatedOral25 MG
Tablet, coatedOral10 mg
Tablet, coatedOral25 mg
TabletOral
Tablet, film coatedOral
Tablet, film coatedOral2.5 MG
Tablet, film coated, extended releaseOral
Tablet, film coatedOral5 mg/1
TabletOral
Tablet, film coatedOral
Tablet, film coatedOral5 mg
Tablet, coated5 mg
Tablet
Tablet, coatedOral2.5 mg
Tablet, coated2.5 mg/1000mg
Tablet, coated2.5 mg/850mg
Tablet, coatedOral5 mg
Tablet, extended releaseOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2435730No2011-03-292022-02-21Canada flag
CA2496249No2012-01-242023-08-18Canada flag
US7407955No2008-08-052023-08-12US flag
US6340475No2002-01-222016-09-19US flag
US6635280No2003-10-212016-09-19US flag
US6488962No2002-12-032020-06-20US flag
US6303661No2001-10-162017-04-24US flag
US6890898No2005-05-102019-02-02US flag
US7078381No2006-07-182019-02-02US flag
US7459428No2008-12-022019-02-02US flag
US8119648No2012-02-212023-08-12US flag
US8178541No2012-05-152023-08-12US flag
US8846695No2014-09-302030-06-04US flag
US9173859No2015-11-032027-05-04US flag
US8853156No2014-10-072031-03-05US flag
US8673927No2014-03-182027-05-04US flag
US8883805No2014-11-112025-11-26US flag
US9155705No2015-10-132030-05-21US flag
US8551957No2013-10-082029-10-19US flag
US7713938No2010-05-112027-04-15US flag
US7579449No2009-08-252025-11-05US flag
US9486526No2016-11-082029-08-05US flag
US9415016No2016-08-162029-04-02US flag
US9555001No2017-01-312033-03-06US flag
US9949998No2018-04-242034-06-11US flag
US10034877No2018-07-312029-08-05US flag
US10022379No2018-07-172029-04-02US flag
US10258637No2019-04-162034-04-03US flag
US10406172No2019-09-102030-06-15US flag
US10596120No2012-03-072032-03-07US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)190-196http://www.chemspider.com/Chemical-Structure.8271879.html?rid=e059df1a-34ab-48c0-9c24-9d6c4d699c47&page_num=0
water solubility<1 mg/mL MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.0502 mg/mLALOGPS
logP2.62ALOGPS
logP2.8ChemAxon
logS-4ALOGPS
pKa (Strongest Basic)9.86ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area113.48 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity133.43 m3·mol-1ChemAxon
Polarizability51.24 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9513
Caco-2 permeable-0.5842
P-glycoprotein substrateSubstrate0.774
P-glycoprotein inhibitor IInhibitor0.5185
P-glycoprotein inhibitor IINon-inhibitor0.7716
Renal organic cation transporterNon-inhibitor0.6658
CYP450 2C9 substrateNon-substrate0.803
CYP450 2D6 substrateNon-substrate0.7335
CYP450 3A4 substrateSubstrate0.7013
CYP450 1A2 substrateNon-inhibitor0.9273
CYP450 2C9 inhibitorNon-inhibitor0.8474
CYP450 2D6 inhibitorNon-inhibitor0.9176
CYP450 2C19 inhibitorNon-inhibitor0.8163
CYP450 3A4 inhibitorNon-inhibitor0.5548
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8562
Ames testNon AMES toxic0.5444
CarcinogenicityNon-carcinogens0.8587
BiodegradationNot ready biodegradable0.9966
Rat acute toxicity2.7553 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6109
hERG inhibition (predictor II)Inhibitor0.8116
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00di-0113900000-1cf1f79967a4761f3983
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0ufr-0391100000-8df1ebbcbdc456f86470
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00di-0114900000-928cf1c76b7fa52190f2

Targets

Details
1. Dipeptidyl peptidase 4
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
  1. 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. [PubMed:22149370]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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
  1. 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. [PubMed:20086031]

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
  1. 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. [PubMed:22568694]
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
  1. 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. [PubMed:22568694]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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
  1. 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. [PubMed:22568694]
  2. 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. [PubMed:23073734]
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
  1. 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. [PubMed:22568694]

Drug created on May 21, 2013 16:46 / Updated on October 21, 2020 01:55

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