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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 CodesA10BD11A10BD19A10BH05
AHFS Codes
  • 68:20.05
PDB EntriesNot Available
FDA labelDownload (353 KB)
MSDSDownload (104 KB)
Interactions
Drug Interactions
Drug
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.
AtazanavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Atazanavir.
BendroflumethiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Bendroflumethiazide.
BetamethasoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Betamethasone.
BrexpiprazoleThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Brexpiprazole.
BumetanideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Bumetanide.
BuserelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Buserelin.
CarbamazepineThe serum concentration of Linagliptin can be decreased when it is combined with Carbamazepine.
CeritinibThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Ceritinib.
ChlorothiazideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Chlorothiazide.
ChlorpropamideLinagliptin may increase the hypoglycemic activities of Chlorpropamide.
ChlorthalidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Chlorthalidone.
ClozapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Clozapine.
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.
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.
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.
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.
DiazoxideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Diazoxide.
DienogestThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Dienogest.
DisopyramideLinagliptin may increase the hypoglycemic activities of Disopyramide.
DrospirenoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Drospirenone.
EnzalutamideThe serum concentration of Linagliptin can be decreased when it is combined with Enzalutamide.
EpinephrineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Epinephrine.
ErythromycinLinagliptin may increase the hypoglycemic activities of Erythromycin.
EstradiolThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Estradiol.
Estrone sulfateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Estropipate.
Etacrynic acidThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Ethacrynic 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.
EtonogestrelThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Etonogestrel.
EverolimusThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Everolimus.
FludrocortisoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Fludrocortisone.
FosamprenavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Fosamprenavir.
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.
GliclazideLinagliptin may increase the hypoglycemic activities of Gliclazide.
GlimepirideLinagliptin may increase the hypoglycemic activities of Glimepiride.
GlipizideLinagliptin may increase the hypoglycemic activities of Glipizide.
GlyburideLinagliptin may increase the hypoglycemic activities of Glyburide.
GoserelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Goserelin.
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.
Hydroxyprogesterone caproateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydroxyprogesterone caproate.
IloperidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Iloperidone.
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.
Insulin AspartLinagliptin may increase the hypoglycemic activities of Insulin Aspart.
Insulin DegludecLinagliptin may increase the hypoglycemic activities of Insulin degludec.
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 Regular.
Insulin LisproLinagliptin may increase the hypoglycemic activities of Insulin Lispro.
LanreotideLinagliptin may increase the hypoglycemic activities of Lanreotide.
LeuprolideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Leuprolide.
LevonorgestrelThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Levonorgestrel.
LopinavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Lopinavir.
LurasidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Lurasidone.
MecaserminLinagliptin may increase the hypoglycemic activities of Mecasermin.
Medroxyprogesterone acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Medroxyprogesterone Acetate.
Megestrol acetateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Megestrol acetate.
MestranolThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Mestranol.
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.
MifepristoneLinagliptin may increase the hypoglycemic activities of Mifepristone.
MitotaneThe serum concentration of Linagliptin can be decreased when it is combined with Mitotane.
NadololThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Nadolol.
NateglinideLinagliptin may increase the hypoglycemic activities of Nateglinide.
NelfinavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Nelfinavir.
NiacinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Niacin.
NilotinibThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Nilotinib.
NorethisteroneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Norethindrone.
NorgestimateThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Norgestimate.
OctreotideLinagliptin may increase the hypoglycemic activities of Octreotide.
OlanzapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Olanzapine.
PaliperidoneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Paliperidone.
PasireotideLinagliptin may increase the hypoglycemic activities of Pasireotide.
PentamidineLinagliptin may increase the hypoglycemic activities of Pentamidine.
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.
PipotiazineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Pipotiazine.
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.
ProgesteroneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Progesterone.
QuetiapineThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Quetiapine.
QuinineLinagliptin may increase the hypoglycemic activities of Quinine.
RepaglinideLinagliptin may increase the hypoglycemic activities of Repaglinide.
Repository corticotropinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Repository corticotropin.
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.
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.
SaquinavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Saquinavir.
SirolimusThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Sirolimus.
SulfadiazineLinagliptin may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleLinagliptin may increase the hypoglycemic activities of Sulfamethoxazole.
SulfisoxazoleLinagliptin may increase the hypoglycemic activities of Sulfisoxazole.
SunitinibLinagliptin may increase the hypoglycemic activities of Sunitinib.
TacrolimusThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Tacrolimus.
TemsirolimusThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Temsirolimus.
TipranavirThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Tipranavir.
TolazamideLinagliptin may increase the hypoglycemic activities of Tolazamide.
TolbutamideLinagliptin may increase the hypoglycemic activities of Tolbutamide.
TorasemideThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Torasemide.
TriamcinoloneThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Triamcinolone.
TrimethoprimLinagliptin may increase the hypoglycemic activities of Trimethoprim.
TriptorelinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Triptorelin.
VinblastineThe serum concentration of Linagliptin can be decreased when it is combined with Vinblastine.
VorinostatThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Vorinostat.
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 July 27, 2016 01:58