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Identification
NameLinagliptin
Accession NumberDB08882
TypeSmall Molecule
GroupsApproved
Description

Linagliptin is a DPP-4 inhibitor developed by Boehringer Ingelheim for the treatment of type II diabetes [Wikipedia]. Two pharmacological characteristics that sets linagliptin apart from other DPP-4 inhibitors is that it has a non-linear pharmacokinetic profile and is not primarily eliminated by the renal system. FDA approved on May 2, 2011.

Structure
Thumb
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
BI 1356
BI-1356
Tradjenta
Trajenta
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Tradjentatablet, film coated5 mg/1oralBoehringer Ingelheim Pharmaceuticals, Inc.2011-05-09Not applicableUs
Tradjentatablet, film coated5 mg/1oralCardinal Health2011-05-09Not applicableUs
Trajentatablet5 mgoralBoehringer Ingelheim (Canada) Ltd Ltee2011-09-13Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
GlyxambiBoehringer Ingelheim Pharmaceuticals, Inc.
JentaduetoBoehringer Ingelheim Pharmaceuticals, Inc.
SaltsNot Available
Categories
UNII3X29ZEJ4R2
CAS number668270-12-0
WeightAverage: 472.5422
Monoisotopic: 472.23352218
Chemical FormulaC25H28N8O2
InChI KeyInChIKey=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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alkaloids and derivatives. These are naturally occurring chemical compounds that contain mostly basic nitrogen atoms. This group also includes some related compounds with neutral and even weakly acidic properties. Also some synthetic compounds of similar structure are attributed to alkaloids. In addition to carbon, hydrogen and nitrogen, alkaloids may also contain oxygen, sulfur and more rarely other elements such as chlorine, bromine, and phosphorus.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassNot Available
Sub ClassNot Available
Direct ParentAlkaloids and derivatives
Alternative Parents
Substituents
  • Alkaloid or derivatives
  • Xanthine
  • Quinazoline
  • Purinone
  • 6-oxopurine
  • Purine
  • Imidazopyrimidine
  • Dialkylarylamine
  • Pyrimidone
  • 3-aminopiperidine
  • Benzenoid
  • Pyrimidine
  • Piperidine
  • N-substituted imidazole
  • Heteroaromatic compound
  • Vinylogous amide
  • Imidazole
  • Azole
  • Urea
  • Tertiary amine
  • Lactam
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationLinagliptin is used for the management of type 2 diabetes mellitus.
PharmacodynamicsLinagliptin is a more potent inhibitor of DPP-4 than other drugs that belong to the same class with an IC50 of 1 nM. In comparison, sitagliptin, saxagliptin, and vildagliptin have an IC50 of 19, 50, and 62 nM respectively. A dose of 2.5 and 5 mg reduces the activity of DPP-4 by 72.7% and 86.1% from baseline respectively in healthy male subjects. In diabetes patients, a dose of 5 and 10 mg inhibits >90% of DPP-4. Linagliptin is also selectively inhibits DPP-4 as indicated by the lack of DPP-8 or DPP-9 inhibition at therapeutic exposures in vitro.
Mechanism of actionLinagliptin is a competitive and reversible dipeptidyl peptidase (DPP)-4 enzyme inhibitor that slows the breakdown of insulinotropic hormone glucagon-like peptide (GLP)-1 for better glycemic control in diabetes patients. GLP and glucose-dependent insulinotropic polypeptide (GIP) are incretin hormones that increase the production and release of insulin from pancreatic beta cells and decrease the release of glucagon from pancreatic alpha cells. This results in a overall decrease in glucose production in the liver and increase an of insulin in a glucose-dependent manner.
Related Articles
AbsorptionCmax, 5 mg, healthy subjects = 8.32 nmol/L; Tmax, 5 mg, healthy subjects = 1.75 hours; AUC(0-24 hours), 5 mg, healthy subjects = 119 nmol · h/L; Bioavailability, healthy subjects = 30%. When a dose of 5 mg once daily is given, steady state is achieved by the third dose. Although a high fat meal reduces Cmax and increases AUC, this interaction with food is not clinically significant. Linagliptin may be administered with or without food.
Volume of distribution

Vd = 1110 L

Protein binding70-80% protein bound, the extent to which is concentration dependent. Because of the propensity of linagliptin to bind to plasma protein, it has a long terminal half-life and a non-linear pharmacokinetic profile. In contrast, other DPP-4 inhibitors have linear pharmacokinetic profiles which makes linagliptin unique.
Metabolism

Linagliptin is not extensively metabolized, 90% of dose is excreted unchanged. The small portion of drug that is metabolized, the main metabolite is CD 1790 and is pharmacologically inactive. Glucuronidation forms some of its other minor metabolites.

SubstrateEnzymesProduct
Linagliptin
Not Available
CD 1790Details
Route of eliminationLinagliptin is eliminated via the feces/enteroheptic system (80%) and urine (5%). This is unlike other DPP-4 inhibitors which are primarily eliminated by the renal system.
Half lifeTerminal half life = 131 hours. Because of this long half-life, inhibition of DPP-4 activity is sustained which indicates that once-daily dosing is appropriate. Effective half-life for accumulation of drug is 12 hours when multiple oral doses of 5 mg are given.
Clearance

Renal clearance, steady state = 70 mL/min

ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral
Tablet, film coatedoral
Tablet, film coatedoral5 mg/1
Tabletoral5 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2435730 No2011-03-292022-02-21Canada
CA2496249 No2012-01-242023-08-18Canada
US6303661 No1997-04-242017-04-24Us
US6890898 No1999-02-022019-02-02Us
US7078381 No1999-02-022019-02-02Us
US7407955 No2003-08-122023-08-12Us
US7459428 No1999-02-022019-02-02Us
US7579449 No2005-11-052025-11-05Us
US7713938 No2007-04-152027-04-15Us
US8119648 No2003-08-122023-08-12Us
US8178541 No2003-08-122023-08-12Us
US8551957 No2009-10-192029-10-19Us
US8673927 No2007-05-042027-05-04Us
US8846695 No2010-06-042030-06-04Us
US8853156 No2011-03-052031-03-05Us
US8883805 No2005-11-262025-11-26Us
US9155705 No2010-05-212030-05-21Us
US9173859 No2007-05-042027-05-04Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
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 FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
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 ]
External Links
ATC CodesA10BH05A10BD19A10BD11
AHFS Codes
  • 68:20.05
PDB EntriesNot Available
FDA labelDownload (353 KB)
MSDSDownload (104 KB)
Interactions
Drug Interactions
Drug
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Linagliptin.
AcetaminophenThe serum concentration of Linagliptin can be increased when it is combined with Acetaminophen.
AcetohexamideLinagliptin may increase the hypoglycemic activities of Acetohexamide.
AfatinibThe serum concentration of Linagliptin can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Linagliptin can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Linagliptin can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Linagliptin can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Linagliptin can be increased when it is combined with Alfentanil.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Linagliptin.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Linagliptin.
AmantadineThe serum concentration of Linagliptin can be increased when it is combined with Amantadine.
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Linagliptin.
Aminohippuric acidThe serum concentration of Linagliptin can be increased when it is combined with Aminohippuric acid.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Linagliptin.
AmiodaroneThe serum concentration of Linagliptin can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Linagliptin.
AmlodipineThe serum concentration of Linagliptin can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Linagliptin can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Linagliptin can be increased when it is combined with Amsacrine.
AripiprazoleThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Aripiprazole.
Arsenic trioxideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Arsenic trioxide.
ArticaineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Articaine.
AsenapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Asenapine.
AstemizoleThe serum concentration of Linagliptin can be increased when it is combined with Astemizole.
AtazanavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Atazanavir.
AtenololThe serum concentration of Linagliptin can be increased when it is combined with Atenolol.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Linagliptin.
AzelastineThe serum concentration of Linagliptin can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Linagliptin can be increased when it is combined with Azithromycin.
BenazeprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Benazepril.
BendroflumethiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Bendroflumethiazide.
BenzocaineThe serum concentration of Linagliptin can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Linagliptin can be increased when it is combined with Bepridil.
BetamethasoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Betamethasone.
BiperidenThe serum concentration of Linagliptin can be increased when it is combined with Biperiden.
BoceprevirThe serum concentration of Linagliptin can be decreased when it is combined with Boceprevir.
BosutinibThe serum concentration of Linagliptin can be increased when it is combined with Bosutinib.
BrexpiprazoleThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Brexpiprazole.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Linagliptin.
BumetanideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Bumetanide.
BuprenorphineThe serum concentration of Linagliptin can be increased when it is combined with Buprenorphine.
BuserelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Buserelin.
BuspironeThe serum concentration of Linagliptin can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Linagliptin can be increased when it is combined with Cabazitaxel.
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Linagliptin.
CaffeineThe serum concentration of Linagliptin can be increased when it is combined with Caffeine.
CanagliflozinThe serum concentration of Linagliptin can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Linagliptin can be increased when it is combined with Candesartan.
CandoxatrilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Candoxatril.
CaptoprilThe serum concentration of Linagliptin can be increased when it is combined with Captopril.
CaptoprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Captopril.
CarbamazepineThe serum concentration of Linagliptin can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Linagliptin can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Linagliptin can be increased when it is combined with Caspofungin.
CeritinibThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Ceritinib.
ChloroquineThe serum concentration of Linagliptin can be increased when it is combined with Chloroquine.
ChlorothiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Chlorothiazide.
ChlorpromazineThe serum concentration of Linagliptin can be increased when it is combined with Chlorpromazine.
ChlorpropamideLinagliptin may increase the hypoglycemic activities of Chlorpropamide.
ChlorpropamideThe serum concentration of Linagliptin can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Linagliptin can be increased when it is combined with Chlorprothixene.
ChlorthalidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Chlorthalidone.
CholesterolThe serum concentration of Linagliptin can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Linagliptin can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Linagliptin can be increased when it is combined with Cilazapril.
CilazaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Cilazapril.
CimetidineThe serum concentration of Linagliptin can be decreased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Linagliptin can be increased when it is combined with Ciprofloxacin.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Linagliptin.
CitalopramThe serum concentration of Linagliptin can be increased when it is combined with Citalopram.
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Linagliptin.
ClarithromycinThe serum concentration of Linagliptin can be increased when it is combined with Clarithromycin.
ClofazimineThe serum concentration of Linagliptin can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Linagliptin.
ClotrimazoleThe serum concentration of Linagliptin can be decreased when it is combined with Clotrimazole.
ClozapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Clozapine.
CobicistatThe serum concentration of Linagliptin can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Linagliptin can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Linagliptin can be increased when it is combined with Colforsin.
CorticotropinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Corticotropin.
Cortisone acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Cortisone acetate.
CrizotinibThe serum concentration of Linagliptin can be increased when it is combined with Crizotinib.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Linagliptin.
CyclophosphamideThe risk or severity of adverse effects can be increased when Linagliptin is combined with Cyclophosphamide.
CyclophosphamideThe serum concentration of Linagliptin can be increased when it is combined with Cyclophosphamide.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Linagliptin.
CyclosporineThe serum concentration of Linagliptin can be decreased when it is combined with Cyclosporine.
Cyproterone acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Cyproterone acetate.
DabrafenibThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Dabrafenib.
DaclatasvirThe serum concentration of Linagliptin can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Linagliptin can be increased when it is combined with Dactinomycin.
DanazolThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Danazol.
DarunavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Darunavir.
DasatinibThe serum concentration of Linagliptin can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Linagliptin can be decreased when it is combined with Daunorubicin.
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Linagliptin.
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Linagliptin.
DesloratadineThe serum concentration of Linagliptin can be increased when it is combined with Desloratadine.
DesogestrelThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Desogestrel.
DexamethasoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Dexamethasone.
DextromethorphanThe serum concentration of Linagliptin can be increased when it is combined with Dextromethorphan.
DiazoxideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Diazoxide.
DiclofenacThe serum concentration of Linagliptin can be increased when it is combined with Diclofenac.
DienogestThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Dienogest.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Linagliptin.
DigoxinThe serum concentration of Linagliptin can be decreased when it is combined with Digoxin.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Linagliptin.
DiltiazemThe serum concentration of Linagliptin can be increased when it is combined with Diltiazem.
DipyridamoleThe serum concentration of Linagliptin can be increased when it is combined with Dipyridamole.
DisopyramideLinagliptin may increase the hypoglycemic activities of Disopyramide.
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Linagliptin.
DoxazosinThe serum concentration of Linagliptin can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Linagliptin.
DoxorubicinThe serum concentration of Linagliptin can be decreased when it is combined with Doxorubicin.
DronabinolThe serum concentration of Linagliptin can be increased when it is combined with Dronabinol.
DronedaroneThe serum concentration of Linagliptin can be increased when it is combined with Dronedarone.
DrospirenoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Drospirenone.
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Linagliptin.
ElbasvirThe serum concentration of Linagliptin can be increased when it is combined with Elbasvir.
EnalaprilThe serum concentration of Linagliptin can be increased when it is combined with Enalapril.
EnalaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Enalapril.
EnalaprilatThe risk or severity of adverse effects can be increased when Linagliptin is combined with Enalaprilat.
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Linagliptin.
EnzalutamideThe serum concentration of Linagliptin can be increased when it is combined with Enzalutamide.
EpinephrineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Epinephrine.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Linagliptin.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Linagliptin.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Linagliptin.
ErythromycinThe serum concentration of Linagliptin can be decreased when it is combined with Erythromycin.
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Linagliptin.
EstradiolThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Estradiol.
EstramustineThe serum concentration of Linagliptin can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Linagliptin can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Linagliptin can be decreased when it is combined with Estrone.
Estrone sulfateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Estrone sulfate.
Etacrynic acidThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Etacrynic acid.
Ethinyl EstradiolThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Ethinyl Estradiol.
Ethynodiol diacetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Ethynodiol diacetate.
EtonogestrelThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Etonogestrel.
EtoposideThe serum concentration of Linagliptin can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Linagliptin.
EtravirineThe serum concentration of Linagliptin can be increased when it is combined with Etravirine.
EverolimusThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Everolimus.
FelodipineThe serum concentration of Linagliptin can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Linagliptin can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Linagliptin can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Linagliptin can be increased when it is combined with Fidaxomicin.
FluconazoleThe serum concentration of Linagliptin can be increased when it is combined with Fluconazole.
FludrocortisoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Fludrocortisone.
FluoxetineThe serum concentration of Linagliptin can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Linagliptin can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Linagliptin can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Linagliptin can be increased when it is combined with Flurazepam.
FluvoxamineThe serum concentration of Linagliptin can be increased when it is combined with Fluvoxamine.
FosamprenavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Fosamprenavir.
FosinoprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Fosinopril.
FosphenytoinThe serum concentration of Linagliptin can be decreased when it is combined with Fosphenytoin.
FurosemideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Furosemide.
GarlicThe serum concentration of Linagliptin can be decreased when it is combined with Garlic.
GefitinibThe serum concentration of Linagliptin can be increased when it is combined with Gefitinib.
GenisteinThe serum concentration of Linagliptin can be increased when it is combined with Genistein.
GlibornurideLinagliptin may increase the hypoglycemic activities of Glibornuride.
GliclazideLinagliptin may increase the hypoglycemic activities of Gliclazide.
GlimepirideLinagliptin may increase the hypoglycemic activities of Glimepiride.
GlipizideLinagliptin may increase the hypoglycemic activities of Glipizide.
GliquidoneLinagliptin may increase the hypoglycemic activities of Gliquidone.
GlisoxepideLinagliptin may increase the hypoglycemic activities of Glisoxepide.
GlyburideLinagliptin may increase the hypoglycemic activities of Glyburide.
GlyburideThe serum concentration of Linagliptin can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Linagliptin can be increased when it is combined with Glycerol.
GoserelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Goserelin.
Gramicidin DThe serum concentration of Linagliptin can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Linagliptin can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Linagliptin can be increased when it is combined with Haloperidol.
HistrelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Histrelin.
HydrochlorothiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydrochlorothiazide.
HydrocortisoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydrocortisone.
HydroflumethiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydroflumethiazide.
Hydroxyprogesterone caproateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydroxyprogesterone caproate.
IdelalisibThe serum concentration of Linagliptin can be increased when it is combined with Idelalisib.
IloperidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Iloperidone.
ImatinibThe serum concentration of Linagliptin can be increased when it is combined with Imatinib.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Linagliptin.
IndapamideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Indapamide.
IndinavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Indinavir.
IndomethacinThe serum concentration of Linagliptin can be increased when it is combined with Indomethacin.
Insulin AspartLinagliptin may increase the hypoglycemic activities of Insulin Aspart.
Insulin DetemirLinagliptin may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlargineLinagliptin may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineLinagliptin may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanLinagliptin may increase the hypoglycemic activities of Insulin Human.
Insulin LisproLinagliptin may increase the hypoglycemic activities of Insulin Lispro.
Insulin PorkLinagliptin may increase the hypoglycemic activities of Insulin Pork.
IsavuconazoniumThe serum concentration of Linagliptin can be increased when it is combined with Isavuconazonium.
ItraconazoleThe serum concentration of Linagliptin can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Linagliptin can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Linagliptin can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Linagliptin can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of Linagliptin can be increased when it is combined with Ketoconazole.
LanreotideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Lanreotide.
LanreotideLinagliptin may increase the hypoglycemic activities of Lanreotide.
LansoprazoleThe serum concentration of Linagliptin can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Linagliptin can be increased when it is combined with Lapatinib.
LeuprolideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Leuprolide.
LevofloxacinThe serum concentration of Linagliptin can be increased when it is combined with Levofloxacin.
LevonorgestrelThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Levonorgestrel.
LevothyroxineThe serum concentration of Linagliptin can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Linagliptin can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Linagliptin can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Linagliptin can be decreased when it is combined with Liotrix.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Linagliptin.
LisinoprilThe serum concentration of Linagliptin can be increased when it is combined with Lisinopril.
LisinoprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Lisinopril.
LomitapideThe serum concentration of Linagliptin can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Linagliptin can be increased when it is combined with Loperamide.
LopinavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Lopinavir.
LoratadineThe serum concentration of Linagliptin can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Linagliptin can be increased when it is combined with Losartan.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Linagliptin.
LumacaftorThe serum concentration of Linagliptin can be decreased when it is combined with Lumacaftor.
LurasidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Lurasidone.
MaprotilineThe serum concentration of Linagliptin can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Linagliptin can be increased when it is combined with Mebendazole.
MecaserminLinagliptin may increase the hypoglycemic activities of Mecasermin.
Medroxyprogesterone acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Medroxyprogesterone acetate.
MefloquineThe serum concentration of Linagliptin can be increased when it is combined with Mefloquine.
Megestrol acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Megestrol acetate.
MeprobamateThe serum concentration of Linagliptin can be increased when it is combined with Meprobamate.
MestranolThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Mestranol.
MethadoneThe serum concentration of Linagliptin can be increased when it is combined with Methadone.
MethotrimeprazineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Methotrimeprazine.
MethyclothiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Methyclothiazide.
MethylprednisoloneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Methylprednisolone.
MetolazoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Metolazone.
MetoprololThe serum concentration of Linagliptin can be increased when it is combined with Metoprolol.
MibefradilThe serum concentration of Linagliptin can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Linagliptin can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Linagliptin.
MidazolamThe serum concentration of Linagliptin can be decreased when it is combined with Midazolam.
MifepristoneLinagliptin may increase the hypoglycemic activities of Mifepristone.
MifepristoneThe serum concentration of Linagliptin can be decreased when it is combined with Mifepristone.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Linagliptin.
MitomycinThe serum concentration of Linagliptin can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Linagliptin can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Linagliptin can be decreased when it is combined with Mitoxantrone.
MoexiprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Moexipril.
MorphineThe serum concentration of Linagliptin can be increased when it is combined with Morphine.
NaltrexoneThe serum concentration of Linagliptin can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Linagliptin can be increased when it is combined with Naringenin.
NateglinideLinagliptin may increase the hypoglycemic activities of Nateglinide.
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Linagliptin.
NefazodoneThe serum concentration of Linagliptin can be decreased when it is combined with Nefazodone.
NelfinavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Nelfinavir.
NeostigmineThe serum concentration of Linagliptin can be increased when it is combined with Neostigmine.
NevirapineThe serum concentration of Linagliptin can be decreased when it is combined with Nevirapine.
NiacinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Niacin.
NicardipineThe serum concentration of Linagliptin can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Linagliptin can be decreased when it is combined with Nifedipine.
NilotinibThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Nilotinib.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Linagliptin.
NisoldipineThe serum concentration of Linagliptin can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Linagliptin can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Linagliptin can be increased when it is combined with Nitrendipine.
NorethisteroneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Norethisterone.
NorgestimateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Norgestimate.
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Linagliptin.
OctreotideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Octreotide.
OctreotideLinagliptin may increase the hypoglycemic activities of Octreotide.
OlanzapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Olanzapine.
OmapatrilatThe risk or severity of adverse effects can be increased when Linagliptin is combined with Omapatrilat.
OmeprazoleThe serum concentration of Linagliptin can be increased when it is combined with Omeprazole.
P-NitrophenolThe serum concentration of Linagliptin can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Linagliptin can be increased when it is combined with Paclitaxel.
PaliperidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Paliperidone.
Palmitic AcidThe serum concentration of Linagliptin can be increased when it is combined with Palmitic Acid.
PantoprazoleThe serum concentration of Linagliptin can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Linagliptin can be increased when it is combined with Paroxetine.
PasireotideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Pasireotide.
PasireotideLinagliptin may increase the hypoglycemic activities of Pasireotide.
PentamidineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Pentamidine.
PentamidineLinagliptin may increase the hypoglycemic activities of Pentamidine.
PentobarbitalThe serum concentration of Linagliptin can be decreased when it is combined with Pentobarbital.
PerindoprilThe serum concentration of Linagliptin can be increased when it is combined with Perindopril.
PerindoprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Perindopril.
PethidineThe risk or severity of adverse effects can be increased when Linagliptin is combined with Pethidine.
PhenobarbitalThe serum concentration of Linagliptin can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Linagliptin can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Linagliptin.
PiperazineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Piperazine.
PipotiazineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Pipotiazine.
Platelet Activating FactorThe serum concentration of Linagliptin can be decreased when it is combined with Platelet Activating Factor.
PolythiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Polythiazide.
PonatinibThe serum concentration of Linagliptin can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Linagliptin can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Linagliptin can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Linagliptin can be increased when it is combined with Prazosin.
PrednisoloneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Prednisolone.
PrednisoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Prednisone.
PrimidoneThe serum concentration of Linagliptin can be decreased when it is combined with Primidone.
ProbenecidThe serum concentration of Linagliptin can be increased when it is combined with Probenecid.
ProgesteroneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Progesterone.
PromethazineThe serum concentration of Linagliptin can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Linagliptin can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Linagliptin can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Linagliptin.
QuercetinThe serum concentration of Linagliptin can be increased when it is combined with Quercetin.
QuetiapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Quetiapine.
QuinacrineThe serum concentration of Linagliptin can be increased when it is combined with Quinacrine.
QuinaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Quinapril.
QuinethazoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Quinethazone.
QuinidineThe serum concentration of Linagliptin can be increased when it is combined with Quinidine.
QuinineLinagliptin may increase the hypoglycemic activities of Quinine.
QuinineThe serum concentration of Linagliptin can be increased when it is combined with Quinine.
RamiprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Ramipril.
RanitidineThe serum concentration of Linagliptin can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Linagliptin can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Linagliptin can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Linagliptin can be increased when it is combined with Regorafenib.
RepaglinideLinagliptin may increase the hypoglycemic activities of Repaglinide.
RescinnamineThe risk or severity of adverse effects can be increased when Linagliptin is combined with Rescinnamine.
ReserpineThe serum concentration of Linagliptin can be decreased when it is combined with Reserpine.
RifabutinThe serum concentration of Linagliptin can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Linagliptin can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Linagliptin can be decreased when it is combined with Rifapentine.
RilpivirineThe serum concentration of Linagliptin can be increased when it is combined with Rilpivirine.
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Linagliptin.
RisperidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Risperidone.
RitonavirThe serum concentration of Linagliptin can be increased when it is combined with Ritonavir.
RolapitantThe serum concentration of Linagliptin can be increased when it is combined with Rolapitant.
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Linagliptin.
SaquinavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Saquinavir.
ScopolamineThe serum concentration of Linagliptin can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Linagliptin can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Linagliptin can be increased when it is combined with Sertraline.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Linagliptin.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Linagliptin.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Linagliptin.
SirolimusThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Sirolimus.
SorafenibThe serum concentration of Linagliptin can be increased when it is combined with Sorafenib.
SpiraprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Spirapril.
SpironolactoneThe serum concentration of Linagliptin can be increased when it is combined with Spironolactone.
St. John's WortThe metabolism of Linagliptin can be increased when combined with St. John&#39;s Wort.
StaurosporineThe serum concentration of Linagliptin can be increased when it is combined with Staurosporine.
StreptozocinThe serum concentration of Linagliptin can be decreased when it is combined with Streptozocin.
SulfadiazineLinagliptin may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleLinagliptin may increase the hypoglycemic activities of Sulfamethoxazole.
SulfinpyrazoneThe serum concentration of Linagliptin can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleLinagliptin may increase the hypoglycemic activities of Sulfisoxazole.
SumatriptanThe serum concentration of Linagliptin can be increased when it is combined with Sumatriptan.
SunitinibLinagliptin may increase the hypoglycemic activities of Sunitinib.
SunitinibThe serum concentration of Linagliptin can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Linagliptin can be increased when it is combined with Tacrine.
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Linagliptin.
TacrolimusThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Tacrolimus.
TamoxifenThe serum concentration of Linagliptin can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Linagliptin can be increased when it is combined with Taurocholic Acid.
TelmisartanThe serum concentration of Linagliptin can be increased when it is combined with Telmisartan.
TemocaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Temocapril.
TemsirolimusThe risk or severity of adverse effects can be increased when Linagliptin is combined with Temsirolimus.
TemsirolimusThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Temsirolimus.
TerazosinThe serum concentration of Linagliptin can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Linagliptin can be increased when it is combined with Terfenadine.
TesmilifeneThe serum concentration of Linagliptin can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Linagliptin can be increased when it is combined with Testosterone.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Linagliptin.
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Linagliptin.
TicagrelorThe serum concentration of Linagliptin can be increased when it is combined with Ticagrelor.
TipranavirThe serum concentration of Linagliptin can be decreased when it is combined with Tipranavir.
TolazamideLinagliptin may increase the hypoglycemic activities of Tolazamide.
TolbutamideLinagliptin may increase the hypoglycemic activities of Tolbutamide.
TolvaptanThe serum concentration of Linagliptin can be increased when it is combined with Tolvaptan.
TorasemideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Torasemide.
TrandolaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Trandolapril.
TrazodoneThe serum concentration of Linagliptin can be decreased when it is combined with Trazodone.
TriamcinoloneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Triamcinolone.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Linagliptin.
TrichlormethiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Trichlormethiazide.
TrifluoperazineThe serum concentration of Linagliptin can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Linagliptin can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Linagliptin can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Linagliptin.
TriptorelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Triptorelin.
TroleandomycinThe serum concentration of Linagliptin can be increased when it is combined with Troleandomycin.
VenlafaxineThe serum concentration of Linagliptin can be increased when it is combined with Venlafaxine.
VerapamilThe serum concentration of Linagliptin can be decreased when it is combined with Verapamil.
VinblastineThe serum concentration of Linagliptin can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Linagliptin can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Linagliptin can be increased when it is combined with Vinorelbine.
VorinostatThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Vorinostat.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Linagliptin.
ZimelidineThe serum concentration of Linagliptin can be increased when it is combined with Zimelidine.
ZiprasidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Ziprasidone.
Food Interactions
  • Although a high fat meal reduces Cmax and increases AUC, this interaction with food is not clinically significant

Targets

Kind
Protein
Organism
Human
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 binding at least ADA, CAV1, IGF2R, and PTPRC. Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor/CD3-dependent manner. Its interaction with ADA also ...
Gene Name:
DPP4
Uniprot ID:
P27487
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
Human
Pharmacological action
unknown
Actions
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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
Molecular Weight:
141477.255 Da
Comments
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Drug created on May 21, 2013 16:46 / Updated on August 31, 2016 02:15