Identification

Name
Linagliptin
Accession Number
DB08882
Type
Small Molecule
Groups
Approved
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
  • Trajenta
External IDs
BI 1356 / BI 1356 BS / BI-1356 / BI-1356-BS
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
TradjentaTablet, film coated5 mg/1OralCardinal Health2011-05-09Not applicableUs00597 0140 30 nlmimage10 ed3d76cb
TradjentaTablet, film coated5 mg/1OralBoehringer Ingelheim2011-05-09Not applicableUs
TrajentaTablet5 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2011-09-13Not applicableCanada
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEu
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEu
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEu
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEu
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEu
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEu
TrajentaTablet, film coated5 mgOralBoehringer Ingelheim2011-08-24Not applicableEu
International/Other Brands
Tradjenta
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
GlyxambiLinagliptin (5 mg/1) + Empagliflozin (10 mg/1)Tablet, film coatedOralBoehringer Ingelheim2015-01-30Not applicableUs
GlyxambiLinagliptin (5 mg) + Empagliflozin (25 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-12-21Not applicableCanada
GlyxambiLinagliptin (5 mg/1) + Empagliflozin (25 mg/1)Tablet, film coatedOralBoehringer Ingelheim2015-01-30Not applicableUs
GlyxambiLinagliptin (5 mg) + Empagliflozin (10 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2016-12-21Not applicableCanada
JentaduetoLinagliptin (2.5 mg/1) + Metformin Hydrochloride (1000 mg/1)Tablet, film coatedOralPhysicians Total Care, Inc.2012-02-13Not applicableUs
JentaduetoLinagliptin (2.5 mg/1) + Metformin Hydrochloride (850 mg/1)Tablet, film coatedOralBoehringer Ingelheim2012-02-13Not applicableUs
JentaduetoLinagliptin (2.5 mg) + Metformin Hydrochloride (1000 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2013-04-17Not applicableCanada
JentaduetoLinagliptin (2.5 mg/1) + Metformin Hydrochloride (1000 mg/1)Tablet, film coatedOralBoehringer Ingelheim2012-02-13Not applicableUs
JentaduetoLinagliptin (2.5 mg) + Metformin Hydrochloride (500 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee2013-04-17Not applicableCanada
JentaduetoLinagliptin (2.5 mg/1) + Metformin Hydrochloride (1000 mg/1)Tablet, film coatedOralbryant ranch prepack2012-02-13Not applicableUs
Categories
UNII
3X29ZEJ4R2
CAS number
668270-12-0
Weight
Average: 472.5422
Monoisotopic: 472.23352218
Chemical Formula
C25H28N8O2
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

Pharmacology

Indication

Linagliptin is used for the management of type 2 diabetes mellitus.

Structured Indications
Pharmacodynamics

Linagliptin 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 action

Linagliptin 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.

TargetActionsOrganism
ADipeptidyl peptidase 4
inhibitor
Human
Absorption

Cmax, 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 binding

70-80% 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.

Route of elimination

Linagliptin 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 life

Terminal 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

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

Interactions

Drug Interactions
DrugInteractionDrug group
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Linagliptin.Approved, Investigational
AcetohexamideLinagliptin may increase the hypoglycemic activities of Acetohexamide.Investigational, Withdrawn
AldosteroneThe serum concentration of Linagliptin can be decreased when it is combined with Aldosterone.Experimental, Investigational
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Linagliptin.Approved, Investigational
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Linagliptin.Approved, Illicit, Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Linagliptin.Experimental, Investigational
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Linagliptin.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Linagliptin.Approved
AmiodaroneThe serum concentration of Linagliptin can be decreased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Linagliptin.Approved
AmoxapineThe serum concentration of Amoxapine can be increased when it is combined with Linagliptin.Approved
AmprenavirThe serum concentration of Linagliptin can be decreased when it is combined with Amprenavir.Approved
AripiprazoleThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Asenapine.Approved
AtazanavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Atazanavir.Approved, Investigational
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Linagliptin.Approved
BenazeprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Benazepril.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Bendroflumethiazide.Approved
BetamethasoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BoceprevirThe serum concentration of Linagliptin can be decreased when it is combined with Boceprevir.Approved, Withdrawn
BrexpiprazoleThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Brexpiprazole.Approved
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Linagliptin.Approved, Investigational
BumetanideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Bumetanide.Approved
BuserelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Buserelin.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Linagliptin.Approved
CandoxatrilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Candoxatril.Experimental
CaptoprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Captopril.Approved
CarbamazepineThe metabolism of Linagliptin can be increased when combined with Carbamazepine.Approved, Investigational
CarbutamideLinagliptin may increase the hypoglycemic activities of Carbutamide.Experimental
CeritinibThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Linagliptin.Withdrawn
ChlorothiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Linagliptin.Investigational, Withdrawn
ChlorpropamideLinagliptin may increase the hypoglycemic activities of Chlorpropamide.Approved
ChlorthalidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Chlorthalidone.Approved
Cholic AcidThe serum concentration of Linagliptin can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Cilazapril.Approved
CimetidineThe serum concentration of Linagliptin can be decreased when it is combined with Cimetidine.Approved
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Linagliptin.Approved, Investigational, Withdrawn
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Linagliptin.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Linagliptin.Approved, Vet Approved
ClotrimazoleThe serum concentration of Linagliptin can be decreased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Clozapine.Approved
Conjugated estrogensThe serum concentration of Conjugated estrogens can be decreased when it is combined with Linagliptin.Approved
CorticotropinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Cortisone acetate.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Linagliptin.Approved
CyclopenthiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Cyclopenthiazide.Experimental
CyclophosphamideThe risk or severity of adverse effects can be increased when Linagliptin is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Linagliptin can be decreased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Danazol.Approved
DarunavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Darunavir.Approved
DaunorubicinThe serum concentration of Linagliptin can be decreased when it is combined with Daunorubicin.Approved
DelaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Delapril.Experimental
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Linagliptin.Approved
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Linagliptin.Approved
DesogestrelThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Desogestrel.Approved
DexamethasoneThe serum concentration of Linagliptin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Diazoxide.Approved
DibenzepinThe serum concentration of Dibenzepin can be increased when it is combined with Linagliptin.Experimental
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Linagliptin.Approved, Investigational
DienogestThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Dienogest.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Linagliptin.Approved, Investigational
DigoxinThe serum concentration of Linagliptin can be decreased when it is combined with Digoxin.Approved
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Linagliptin.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Linagliptin.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Linagliptin.Experimental
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Linagliptin.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Linagliptin.Approved
DisopyramideLinagliptin may increase the hypoglycemic activities of Disopyramide.Approved
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Linagliptin.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Linagliptin.Approved
DoxorubicinThe serum concentration of Linagliptin can be decreased when it is combined with Doxorubicin.Approved, Investigational
DrospirenoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Drospirenone.Approved
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Linagliptin.Approved
EnalaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Linagliptin is combined with Enalaprilat.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Linagliptin.Approved, Investigational
EnzalutamideThe serum concentration of Linagliptin can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Epinephrine.Approved, Vet Approved
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Linagliptin.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Linagliptin.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Linagliptin.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Linagliptin.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Linagliptin.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Linagliptin.Approved
EstriolThe serum concentration of Linagliptin can be decreased when it is combined with Estriol.Approved, Investigational, Vet Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Linagliptin.Approved
EstroneThe serum concentration of Linagliptin can be decreased when it is combined with Estrone.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Linagliptin.Approved
Etacrynic acidThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Linagliptin.Approved
Ethynodiol diacetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Linagliptin.Approved
EverolimusThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Everolimus.Approved
FludrocortisoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Fludrocortisone.Approved
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Linagliptin.Approved
FosamprenavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Fosamprenavir.Approved
FosinoprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Fosinopril.Approved
FosphenytoinThe serum concentration of Linagliptin can be decreased when it is combined with Fosphenytoin.Approved
FurosemideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Furosemide.Approved, Vet Approved
GarlicThe serum concentration of Linagliptin can be decreased when it is combined with Garlic.Approved
GlibornurideLinagliptin may increase the hypoglycemic activities of Glibornuride.Investigational, Withdrawn
GliclazideLinagliptin may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideLinagliptin may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideLinagliptin may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneLinagliptin may increase the hypoglycemic activities of Gliquidone.Approved, Investigational
GlisoxepideLinagliptin may increase the hypoglycemic activities of Glisoxepide.Approved, Investigational
GlyburideLinagliptin may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Goserelin.Approved
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Linagliptin.Withdrawn
HistrelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Histrelin.Approved
HydrochlorothiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydroflumethiazide.Approved, Investigational
Hydroxyprogesterone caproateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IloperidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Iloperidone.Approved
ImidaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Imidapril.Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Linagliptin.Approved
IndapamideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Indapamide.Approved
IndinavirThe serum concentration of Linagliptin can be decreased when it is combined with Indinavir.Approved
Insulin AspartLinagliptin may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirLinagliptin may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineLinagliptin may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineLinagliptin may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanLinagliptin may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproLinagliptin may increase the hypoglycemic activities of Insulin Lispro.Approved
Insulin PorkLinagliptin may increase the hypoglycemic activities of Insulin Pork.Approved
IprindoleThe serum concentration of Iprindole can be increased when it is combined with Linagliptin.Experimental
LanreotideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Lanreotide.Approved
LeuprolideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Leuprolide.Approved, Investigational
LevonorgestrelThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LevothyroxineThe serum concentration of Linagliptin can be decreased when it is combined with Levothyroxine.Approved
LiothyronineThe serum concentration of Linagliptin can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Linagliptin can be decreased when it is combined with Liotrix.Approved
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Linagliptin.Approved, Nutraceutical
LisinoprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Lisinopril.Approved, Investigational
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Linagliptin.Approved, Investigational
LofepramineThe serum concentration of Lofepramine can be increased when it is combined with Linagliptin.Experimental
LopinavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Lopinavir.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Linagliptin.Approved, Investigational
LumacaftorThe serum concentration of Linagliptin can be decreased when it is combined with Lumacaftor.Approved
LurasidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Lurasidone.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Linagliptin.Illicit, Investigational, Withdrawn
MecaserminLinagliptin may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Linagliptin.Approved
MetahexamideLinagliptin may increase the hypoglycemic activities of Metahexamide.Experimental
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Linagliptin.Experimental
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Linagliptin.Experimental
MethotrimeprazineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Methyclothiazide.Approved
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Linagliptin.Approved
MethylprednisoloneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Linagliptin.Approved
MetolazoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Metolazone.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Linagliptin.Experimental
MidazolamThe serum concentration of Linagliptin can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Linagliptin can be decreased when it is combined with Mifepristone.Approved, Investigational
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Linagliptin.Approved
MitotaneThe serum concentration of Linagliptin can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Linagliptin can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MoexiprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Moexipril.Approved
NateglinideLinagliptin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Linagliptin.Approved, Withdrawn
NelfinavirThe serum concentration of Linagliptin can be decreased when it is combined with Nelfinavir.Approved
NevirapineThe serum concentration of Linagliptin can be decreased when it is combined with Nevirapine.Approved
NiacinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Linagliptin.Approved, Investigational
NifedipineThe serum concentration of Linagliptin can be decreased when it is combined with Nifedipine.Approved
NilotinibThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Nilotinib.Approved, Investigational
NorethisteroneThe serum concentration of Linagliptin can be decreased when it is combined with Norethisterone.Approved
NorgestimateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Norgestimate.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Linagliptin.Approved
OctreotideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Octreotide.Approved, Investigational
OlanzapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Olanzapine.Approved, Investigational
OmapatrilatThe risk or severity of adverse effects can be increased when Linagliptin is combined with Omapatrilat.Investigational
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Linagliptin.Investigational
PaliperidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Paliperidone.Approved
PasireotideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Pasireotide.Approved
PentamidineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Pentamidine.Approved
PentobarbitalThe serum concentration of Linagliptin can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Linagliptin.Approved, Investigational, Vet Approved, Withdrawn
PerindoprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Perindopril.Approved
PethidineThe risk or severity of adverse effects can be increased when Linagliptin is combined with Pethidine.Approved
PhenobarbitalThe serum concentration of Linagliptin can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Linagliptin can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Linagliptin.Approved
PiperazineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Pipotiazine.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Linagliptin.Approved
Platelet Activating FactorThe serum concentration of Linagliptin can be decreased when it is combined with Platelet Activating Factor.Experimental
PolythiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Polythiazide.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Linagliptin.Approved
PrednisoloneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Prednisone.Approved, Vet Approved
PrimidoneThe serum concentration of Linagliptin can be decreased when it is combined with Primidone.Approved, Vet Approved
ProgesteroneThe serum concentration of Linagliptin can be decreased when it is combined with Progesterone.Approved, Vet Approved
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Linagliptin.Approved
QuetiapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Quetiapine.Approved
QuinaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Quinapril.Approved, Investigational
QuinethazoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Quinethazone.Approved
QuinineLinagliptin may increase the hypoglycemic activities of Quinine.Approved
RamiprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Ramipril.Approved
RanolazineThe serum concentration of Linagliptin can be increased when it is combined with Ranolazine.Approved, Investigational
RepaglinideLinagliptin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RescinnamineThe risk or severity of adverse effects can be increased when Linagliptin is combined with Rescinnamine.Approved
ReserpineThe serum concentration of Linagliptin can be decreased when it is combined with Reserpine.Approved, Investigational
RifabutinThe serum concentration of Linagliptin can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Linagliptin can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Linagliptin can be decreased when it is combined with Rifapentine.Approved
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Linagliptin.Approved
RisperidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe serum concentration of Linagliptin can be increased when it is combined with Ritonavir.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Linagliptin.Approved
SaquinavirThe serum concentration of Linagliptin can be decreased when it is combined with Saquinavir.Approved, Investigational
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Linagliptin.Approved, Investigational
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Linagliptin.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Linagliptin.Approved
SirolimusThe serum concentration of Linagliptin can be decreased when it is combined with Sirolimus.Approved, Investigational
SpiraprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Spirapril.Approved
St. John's WortThe serum concentration of Linagliptin can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StreptozocinThe serum concentration of Linagliptin can be decreased when it is combined with Streptozocin.Approved
SulfadiazineLinagliptin may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleLinagliptin may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazoleLinagliptin may increase the hypoglycemic activities of Sulfisoxazole.Approved, Vet Approved
SunitinibLinagliptin may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Linagliptin.Approved
TacrolimusThe serum concentration of Linagliptin can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Linagliptin can be decreased when it is combined with Tamoxifen.Approved
TemocaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Temocapril.Experimental, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Linagliptin is combined with Temsirolimus.Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Linagliptin.Experimental
TesmilifeneThe serum concentration of Linagliptin can be decreased when it is combined with Tesmilifene.Investigational
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Linagliptin.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Linagliptin.Approved, Investigational
TipranavirThe serum concentration of Linagliptin can be decreased when it is combined with Tipranavir.Approved, Investigational
TolazamideLinagliptin may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideLinagliptin may increase the hypoglycemic activities of Tolbutamide.Approved
TorasemideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Torasemide.Approved
TrandolaprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Trandolapril.Approved
TrazodoneThe serum concentration of Linagliptin can be decreased when it is combined with Trazodone.Approved, Investigational
TriamcinoloneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Linagliptin.Approved
TrichlormethiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrimethoprimThe serum concentration of Linagliptin can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Linagliptin.Approved
TriptorelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Triptorelin.Approved, Vet Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Linagliptin.Approved, Experimental
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Linagliptin.Approved, Investigational
VerapamilThe serum concentration of Linagliptin can be decreased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Linagliptin can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Linagliptin can be decreased when it is combined with Vincristine.Approved, Investigational
VorinostatThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Vorinostat.Approved, Investigational
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Linagliptin.Approved
ZiprasidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Ziprasidone.Approved
ZofenoprilThe risk or severity of adverse effects can be increased when Linagliptin is combined with Zofenopril.Experimental
Food Interactions
  • Although a high fat meal reduces Cmax and increases AUC, this interaction with food is not clinically significant

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
KEGG Drug
D09566
PubChem Compound
10096344
PubChem Substance
175427132
ChemSpider
8271879
BindingDB
50228403
ChEBI
68610
ChEMBL
CHEMBL237500
HET
356
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Linagliptin
ATC Codes
A10BH05 — LinagliptinA10BD19 — Linagliptin and empagliflozinA10BD11 — Metformin and 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
1CompletedNot AvailableHealthy Volunteers1
1CompletedHealth Services ResearchHealthy Volunteers1
1CompletedTreatmentHealthy Volunteers31
1CompletedTreatmentHepatic Insufficiency1
1CompletedTreatmentType 2 Diabetes Mellitus3
1SuspendedTreatmentSchizophrenic Disorders1
1, 2RecruitingTreatmentGastric Adenocarcinoma or Gastroesophageal Junction Adenocarcinoma1
2CompletedTreatmentType 2 Diabetes Mellitus5
3Active Not RecruitingTreatmentType 2 Diabetes Mellitus1
3CompletedNot AvailableAlbuminuria / Arterial Hypertension1
3CompletedTreatmentType 2 DM Patients With Moderate or Severe Renal Impairment1
3CompletedTreatmentType 2 Diabetes Mellitus28
3Not Yet RecruitingTreatmentDM21
3RecruitingTreatmentLeft Ventricular Systolic Dysfunction / Type 2 Diabetes Mellitus1
3RecruitingTreatmentType 2 Diabetes Mellitus2
3TerminatedTreatmentLeft Ventricular Diastolic Dysfunction / Type 2 Diabetes Mellitus1
3TerminatedTreatmentPlaque Morphology / Type 2 Diabetes Mellitus / Vascular Inflammation1
4Active Not RecruitingPreventionInsulin Resistance / Prediabetic State1
4Active Not RecruitingTreatmentType 2 Diabetes Mellitus3
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedPreventionChronic Renal Failure (CRF) / Type 2 Diabetes Mellitus1
4CompletedTreatmentCoronary Artery Disease / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes1
4CompletedTreatmentDiabetes Mellitus (DM)1
4CompletedTreatmentType 2 Diabetes Mellitus5
4Not Yet RecruitingTreatmentAdvanced Glycation End Products / Diabetes / SGLT-2 Inhibitors1
4Not Yet RecruitingTreatmentBone destruction / Diabetes Mellitus (DM)1
4Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
4Not Yet RecruitingTreatmentType2 Diabetes Mellitus1
4RecruitingBasic ScienceSchizophrenic Disorders1
4RecruitingTreatmentImpaired Renal Function / Type 2 Diabetes Mellitus1
4RecruitingTreatmentPeritoneal dialysis therapy / Type 2 Diabetes Mellitus1
4RecruitingTreatmentType 2 Diabetes Mellitus1
4RecruitingTreatmentType II Diabetes in Subjects BMI 27 to 32 / Type II Diabetes in the Not so Obese1
4RecruitingTreatmentType2 Diabetes1
4TerminatedTreatmentType 2 Diabetes Mellitus1
4Unknown StatusBasic ScienceType 2 Diabetes Mellitus2
4Unknown StatusTreatmentInsulin Sensitivity/Resistance / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentType 2 Diabetes Mellitus1
Not AvailableActive Not RecruitingBasic ScienceType 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableType 2 Diabetes Mellitus2
Not AvailableNot Yet RecruitingNot AvailableType 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentChronic Kidney Disease (CKD) / Type 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableTerminatedNot AvailableType 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral
Tablet, film coatedOral
Tablet, film coated, extended releaseOral
Tablet, film coatedOral5 mg/1
TabletOral5 mg
Tablet, film coatedOral5 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2435730No2011-03-292022-02-21Canada
CA2496249No2012-01-242023-08-18Canada
US7407955No2003-08-122023-08-12Us
US6340475No1996-09-192016-09-19Us
US6635280No1996-09-192016-09-19Us
US6488962No2000-06-202020-06-20Us
US6303661No1997-04-242017-04-24Us
US6890898No1999-02-022019-02-02Us
US7078381No1999-02-022019-02-02Us
US7459428No1999-02-022019-02-02Us
US8119648No2003-08-122023-08-12Us
US8178541No2003-08-122023-08-12Us
US8846695No2010-06-042030-06-04Us
US9173859No2007-05-042027-05-04Us
US8853156No2011-03-052031-03-05Us
US8673927No2007-05-042027-05-04Us
US8883805No2005-11-262025-11-26Us
US9155705No2010-05-212030-05-21Us
US8551957No2009-10-192029-10-19Us
US7713938No2007-04-152027-04-15Us
US7579449No2005-11-052025-11-05Us
US9486526No2009-08-052029-08-05Us
US9415016No2009-04-022029-04-02Us
US9555001No2013-03-062033-03-06Us

Properties

State
Solid
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 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

Taxonomy

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
Xanthine / Diazanaphthalene / 6-oxopurine / Purinone / Quinazoline / Alkaloid or derivatives / Dialkylarylamine / 3-aminopiperidine / Pyrimidone / Piperidine
show 22 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
aminopiperidine, quinazolines (CHEBI:68610)

Targets

Details
1. Dipeptidyl peptidase 4
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 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
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da

Drug created on May 21, 2013 16:46 / Updated on November 19, 2017 20:34