Dabigatran etexilate

Identification

Summary

Dabigatran etexilate is an anticoagulant used for the prevention of venous thromboembolic events or stroke in patients with recent elective hip or knee replacement surgery and atrial fibrillation.

Brand Names
Pradaxa
Generic Name
Dabigatran etexilate
DrugBank Accession Number
DB06695
Background

Dabigatran etexilate is an oral prodrug that is hydrolyzed to the competitive and reversible direct thrombin inhibitor dabigatranLabel,5. Dabigatran etexilate may be used to decrease the risk of venous thromboembolic events in patients in whom anticoagulation therapy is indicated5. In contrast to warfarin, because its anticoagulant effects are predictable, lab monitoring is not necessary5. Dabigatran etexilate was approved by the FDA in 20106.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 627.7332
Monoisotopic: 627.316917457
Chemical Formula
C34H41N7O5
Synonyms
  • Dabigatran etexilate
External IDs
  • BIBR 1048
  • BIBR 1048 BS RS1
  • BIBR-1048
  • BIBR-1048-BS-RS1

Pharmacology

Indication

Dabigatran is indicated for the prevention of venous thromboembolic events in patients who have undergone elective hip or knee replacement surgery (based on RE-NOVATE, RE-MODEL, and RE-MOBILIZE trials)5,2,1. In 2010, it was approved in the US and Canada for prevention of stroke and systemic embolism in patients with atrial fibrillation (approval based on the RE-LY trial)Label,5.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Dabigatran directly inhibits thrombin in a concentration-dependent, reversible, specific, and competitive manner which results in a prolongation of aPTT (partial thromboplastin time), ECT (Ecarin clotting time), and TT (thrombin time)Label,5.

Mechanism of action

Dabigatran is hydrolysed to the active dabigatran by an esterase which induces hydrolysisLabel,4. Dabigatran and it's glucuronidated metabolites all share equal pharmacological activityLabel,4. Dabigatran and its metabolites inhibit thrombin, a serine proteaseLabel,4. This inhibition prevents the thrombin mediated conversion of fibrinogen to fibrin, an early step in the coagulation cascadeLabel,4. With reduced conversion of fibrinogen to fibrin, clotting time increases.

TargetActionsOrganism
AProthrombin
inhibitor
Humans
Absorption

Oral dabigatran is 3-7% bioavailable, reaching a maximum concentration 1 hour after administration in fasted subjectsLabel. When taken with a meal that is high in fat, the time to maximum concentration increases to 2 hours, though this does not affect dosingLabel,5. Dabigatran etexilate's bioavailability increases to 75% when taken without the capsule shell and so patients should not chew or crush the capsulesLabel.

Volume of distribution

50-70LLabel.

Protein binding

Dabigatran is approximately 35% protein plasma boundLabel,5.

Metabolism

Dabigatran etexilate is metabolised by esterases, microsomal carboxylesterases, and uridine 5'-diphospho-glucuronosyltransferases(UGTs)Label,4. Dabigatran etexilate undergoes hydrolysis to create the active dabigatran which is then glucuronidated by UGTs to 1-O, 2-O, 3-O, or 4-O-acylglucuronideLabel,4.

Hover over products below to view reaction partners

Route of elimination

7% of the dose is recovered in urine and 86% is recovered in the fecesLabel.

Half-life

12 to 17 hoursLabel,5.

Clearance

Not Available

Adverse Effects
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Toxicity

No human studies involving pregnancy, labor and delivery, nursing, or pediatricsLabel. Geriatric patients are at higher risk of adverse effects than younger patients but the risk to benefit ratio is generally still favourable for older patientsLabel. Patients with a creatinine clearance of 15-30mL/min should have their doses of dabigatran etexilate reduced, and no data is available for patients with a creatinine clearance below 15mL/minLabel.

In animal studies, dabigatran increases the rates of dead offspring and causes uterine and vaginal bleeding close to birthLabel. Dabigatran may or may not be excreted in breast milk so the risk and benefit of stopping the drug or stopping breast feeding must be consideredLabel.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Dabigatran etexilate which could result in a higher serum level.
AbciximabDabigatran etexilate may increase the anticoagulant activities of Abciximab.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Dabigatran etexilate.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Dabigatran etexilate.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Dabigatran etexilate.
AcenocoumarolDabigatran etexilate may increase the anticoagulant activities of Acenocoumarol.
AcetaminophenAcetaminophen may decrease the excretion rate of Dabigatran etexilate which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Dabigatran etexilate which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Dabigatran etexilate.
AclidiniumDabigatran etexilate may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Interactions
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Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • Avoid St. John's Wort. This herb induces PGP which may reduce the serum levels of dabigatran.
  • Take with a full glass of water.
  • Take with or without food.

Products

Products
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Product Ingredients
IngredientUNIICASInChI Key
Dabigatran etexilate mesilateSC7NUW5IIT872728-81-9XETBXHPXHHOLOE-UHFFFAOYSA-N
Active Moieties
NameKindUNIICASInChI Key
DabigatranprodrugI0VM4M70GC211914-51-1YBSJFWOBGCMAKL-UHFFFAOYSA-N
International/Other Brands
Pradax (Boehringer Ingelheim) / Rendix
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PradaxaCapsule150 mg/1OralBoehringer Ingelheim Pharmaceuticals Inc.2010-10-262020-05-31US flag
PradaxaCapsule30 mgOralBoehringer Ingelheim2021-02-10Not applicableEU flag
PradaxaCapsule150 mgOralBoehringer Ingelheim2016-09-08Not applicableEU flag
PradaxaCapsule110 mgOralBoehringer Ingelheim2016-09-08Not applicableEU flag
PradaxaCapsule150 mg/1Oralbryant ranch prepack2017-07-28Not applicableUS flag
PradaxaCapsule75 mgOralBoehringer Ingelheim2016-09-08Not applicableEU flag
PradaxaCapsule150 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2010-11-03Not applicableCanada flag
PradaxaCapsule110 mgOralBoehringer Ingelheim2016-09-08Not applicableEU flag
PradaxaCapsule110 mgOralBoehringer Ingelheim2016-09-08Not applicableEU flag
PradaxaCapsule75 mgOralBoehringer Ingelheim2016-09-08Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-dabigatranCapsule150 mgOralApotex Corporation2019-02-04Not applicableCanada flag
Apo-dabigatranCapsule110 mgOralApotex Corporation2019-02-04Not applicableCanada flag
Apo-dabigatranCapsule75 mgOralApotex Corporation2019-08-14Not applicableCanada flag
Dabigatran EtexilateCapsule, coated pellets150 mg/1OralAscend Laboratories, LLC2020-03-132020-03-13US flag
Dabigatran EtexilateCapsule, coated pellets75 mg/1OralAscend Laboratories, LLC2020-03-132020-03-13US flag
Teva-dabigatranCapsule150 mgOralTEVA Canada LimitedNot applicableNot applicableCanada flag
Teva-dabigatranCapsule75 mgOralTEVA Canada LimitedNot applicableNot applicableCanada flag

Categories

ATC Codes
B01AE07 — Dabigatran etexilate
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as benzimidazoles. These are organic compounds containing a benzene ring fused to an imidazole ring (five member ring containing a nitrogen atom, 4 carbon atoms, and two double bonds).
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzimidazoles
Sub Class
Not Available
Direct Parent
Benzimidazoles
Alternative Parents
Phenylalkylamines / Aniline and substituted anilines / Secondary alkylarylamines / Pyridines and derivatives / N-substituted imidazoles / Imidolactams / Tertiary carboxylic acid amides / Heteroaromatic compounds / Amino acids and derivatives / Carboxylic acid esters
show 10 more
Substituents
Amidine / Amine / Amino acid or derivatives / Aniline or substituted anilines / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Benzimidazole
show 27 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
carboxylic ester, carboxamidine, beta-alanine derivative, pyridines, aromatic amide, benzimidazoles (CHEBI:70746)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
2E18WX195X
CAS number
211915-06-9
InChI Key
KSGXQBZTULBEEQ-UHFFFAOYSA-N
InChI
InChI=1S/C34H41N7O5/c1-4-6-7-10-21-46-34(44)39-32(35)24-12-15-26(16-13-24)37-23-30-38-27-22-25(14-17-28(27)40(30)3)33(43)41(20-18-31(42)45-5-2)29-11-8-9-19-36-29/h8-9,11-17,19,22,37H,4-7,10,18,20-21,23H2,1-3H3,(H2,35,39,44)
IUPAC Name
ethyl 3-(1-{2-[({4-[(1E)-amino({[(hexyloxy)carbonyl]imino})methyl]phenyl}amino)methyl]-1-methyl-1H-1,3-benzodiazol-5-yl}-N-(pyridin-2-yl)formamido)propanoate
SMILES
CCCCCCOC(=O)\N=C(\N)C1=CC=C(NCC2=NC3=C(C=CC(=C3)C(=O)N(CCC(=O)OCC)C3=NC=CC=C3)N2C)C=C1

References

Synthesis Reference

Christian Filser, Wolfgang Dersch, Rainer Hamm, Arndt Hausherr, Gunter Koch, Ulrich Scholz, Georg Zerban, "METHOD FOR PRODUCING AN INTERMEDIATE PRODUCT OF DABIGATRAN ETEXILATE." U.S. Patent US20110118471, issued May 19, 2011.

US20110118471
General References
  1. Eriksson BI, Dahl OE, Rosencher N, Kurth AA, van Dijk CN, Frostick SP, Kalebo P, Christiansen AV, Hantel S, Hettiarachchi R, Schnee J, Buller HR: Oral dabigatran etexilate vs. subcutaneous enoxaparin for the prevention of venous thromboembolism after total knee replacement: the RE-MODEL randomized trial. J Thromb Haemost. 2007 Nov;5(11):2178-85. [Article]
  2. Eriksson BI, Dahl OE, Rosencher N, Kurth AA, van Dijk CN, Frostick SP, Prins MH, Hettiarachchi R, Hantel S, Schnee J, Buller HR: Dabigatran etexilate versus enoxaparin for prevention of venous thromboembolism after total hip replacement: a randomised, double-blind, non-inferiority trial. Lancet. 2007 Sep 15;370(9591):949-56. [Article]
  3. Scaglione F: New oral anticoagulants: comparative pharmacology with vitamin K antagonists. Clin Pharmacokinet. 2013 Feb;52(2):69-82. doi: 10.1007/s40262-012-0030-9. [Article]
  4. Ebner T, Wagner K, Wienen W: Dabigatran acylglucuronide, the major human metabolite of dabigatran: in vitro formation, stability, and pharmacological activity. Drug Metab Dispos. 2010 Sep;38(9):1567-75. doi: 10.1124/dmd.110.033696. Epub 2010 Jun 15. [Article]
  5. van Ryn J, Goss A, Hauel N, Wienen W, Priepke H, Nar H, Clemens A: The discovery of dabigatran etexilate. Front Pharmacol. 2013 Feb 12;4:12. doi: 10.3389/fphar.2013.00012. eCollection 2013. [Article]
  6. FDA Drug Approval Package for Dabigatran Etexilate [Link]
  7. Apotex Inc. Product Monograph: Dabigatran Etexilate [File]
Human Metabolome Database
HMDB0015641
KEGG Drug
D07144
PubChem Compound
6445226
PubChem Substance
99443249
ChemSpider
4948999
BindingDB
50432209
RxNav
1037042
ChEBI
70746
ChEMBL
CHEMBL539697
ZINC
ZINC000003943279
PharmGKB
PA165958369
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Dabigatran
AHFS Codes
  • 20:12.04.12 — Direct Thrombin Inhibitors
FDA label
Download (731 KB)
MSDS
Download (99.2 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingOtherCerebral Ischemic Events / Cognition Disorders / Dementia1
4Active Not RecruitingPreventionAtrial Fibrillation / Device Related Thrombus / Left Atrial Appendage Thrombosis / Watchman LAA Closure Device1
4CompletedBasic ScienceVenous Thromboembolism1
4CompletedPreventionArthroplasty, Replacement / Moderate Renal Impairment (CrCl 30-50 mL/Min) / Prevention of Venous Thromboembolism1
4CompletedPreventionAtrial Fibrillation2
4CompletedTreatmentAtrial Fibrillation3
4CompletedTreatmentAtrial Fibrillation / Flutter, Atrial1
4CompletedTreatmentAtrial Fibrillation / Valve Heart Disease1
4CompletedTreatmentCoronary Heart Disease (CHD)1
4Not Yet RecruitingTreatmentAcute Coronary Syndrome (ACS) / Antithrombotic Therapy / Atrial Fibrillation / Percutaneous Coronary Intervention (PCI)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Capsule, coatedOral
Capsule, coated pelletsOral150 mg/1
Capsule, coated pelletsOral75 mg/1
CapsuleOral
CapsuleOral110 mg/1
CapsuleOral150 mg/1
CapsuleOral20 mg
CapsuleOral30 mg
CapsuleOral40 mg
CapsuleOral50 mg
CapsuleOral6.25 mg/ml
CapsuleOral75 mg/1
CapsuleOral110 mg
CapsuleOral150 mg
CapsuleOral75 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9034822Yes2015-05-192031-07-20US flag
US6087380Yes2000-07-112022-06-28US flag
US7932273Yes2011-04-262026-03-07US flag
US7866474Yes2011-01-112028-03-02US flag
US9925174Yes2018-03-272023-12-14US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)132http://www.chemspider.com/Chemical-Structure.8615298.html
water solubility1.8mg/ml, partly soluble MSDS
logP3.8Apotex Inc. Product Monograph: Dabigatran Etexilate
Predicted Properties
PropertyValueSource
Water Solubility0.00466 mg/mLALOGPS
logP5.17ALOGPS
logP4.59ChemAxon
logS-5.1ALOGPS
pKa (Strongest Acidic)17.89ChemAxon
pKa (Strongest Basic)4.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area154.03 Å2ChemAxon
Rotatable Bond Count17ChemAxon
Refractivity176.43 m3·mol-1ChemAxon
Polarizability70.65 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.942
Blood Brain Barrier+0.8673
Caco-2 permeable-0.7014
P-glycoprotein substrateSubstrate0.7412
P-glycoprotein inhibitor IInhibitor0.7539
P-glycoprotein inhibitor IIInhibitor0.8443
Renal organic cation transporterNon-inhibitor0.701
CYP450 2C9 substrateNon-substrate0.858
CYP450 2D6 substrateNon-substrate0.837
CYP450 3A4 substrateSubstrate0.6154
CYP450 1A2 substrateNon-inhibitor0.6906
CYP450 2C9 inhibitorNon-inhibitor0.5102
CYP450 2D6 inhibitorNon-inhibitor0.8417
CYP450 2C19 inhibitorInhibitor0.5157
CYP450 3A4 inhibitorInhibitor0.781
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5789
Ames testNon AMES toxic0.6292
CarcinogenicityNon-carcinogens0.8065
BiodegradationNot ready biodegradable0.9931
Rat acute toxicity2.7093 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9047
hERG inhibition (predictor II)Inhibitor0.6181
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 GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
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/MSsplash10-00kk-0981100000-78856b63936cf67ebce2
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004r-0292116000-55b368cbe92da888e681

Targets

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Thrombospondin receptor activity
Specific Function
Thrombin, which cleaves bonds after Arg and Lys, converts fibrinogen to fibrin and activates factors V, VII, VIII, XIII, and, in complex with thrombomodulin, protein C. Functions in blood homeostas...
Gene Name
F2
Uniprot ID
P00734
Uniprot Name
Prothrombin
Molecular Weight
70036.295 Da
References
  1. Squizzato A, Dentali F, Steidl L, Ageno W: New direct thrombin inhibitors. Intern Emerg Med. 2009 Dec;4(6):479-84. doi: 10.1007/s11739-009-0314-8. Epub 2009 Sep 15. [Article]
  2. Liesenfeld KH, Schafer HG, Troconiz IF, Tillmann C, Eriksson BI, Stangier J: Effects of the direct thrombin inhibitor dabigatran on ex vivo coagulation time in orthopaedic surgery patients: a population model analysis. Br J Clin Pharmacol. 2006 Nov;62(5):527-37. [Article]
  3. Karthikeyan G, Eikelboom JW, Hirsh J: Dabigatran: ready for prime time? Pol Arch Med Wewn. 2010 Apr;120(4):137-42. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Triglyceride lipase activity
Specific Function
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acy...
Gene Name
CES1
Uniprot ID
P23141
Uniprot Name
Liver carboxylesterase 1
Molecular Weight
62520.62 Da
References
  1. Hu ZY, Parker RB, Herring VL, Laizure SC: Conventional liquid chromatography/triple quadrupole mass spectrometry based metabolite identification and semi-quantitative estimation approach in the investigation of in vitro dabigatran etexilate metabolism. Anal Bioanal Chem. 2013 Feb;405(5):1695-704. doi: 10.1007/s00216-012-6576-4. Epub 2012 Dec 14. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Methylumbelliferyl-acetate deacetylase activity
Specific Function
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Shows high catalytic efficiency for hydrolysis of cocaine, 4-methylumbelliferyl acetate, heroin and ...
Gene Name
CES2
Uniprot ID
O00748
Uniprot Name
Cocaine esterase
Molecular Weight
61806.41 Da
References
  1. Hu ZY, Parker RB, Herring VL, Laizure SC: Conventional liquid chromatography/triple quadrupole mass spectrometry based metabolite identification and semi-quantitative estimation approach in the investigation of in vitro dabigatran etexilate metabolism. Anal Bioanal Chem. 2013 Feb;405(5):1695-704. doi: 10.1007/s00216-012-6576-4. Epub 2012 Dec 14. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
Gene Name
UGT1A9
Uniprot ID
O60656
Uniprot Name
UDP-glucuronosyltransferase 1-9
Molecular Weight
59940.495 Da
References
  1. Ebner T, Wagner K, Wienen W: Dabigatran acylglucuronide, the major human metabolite of dabigatran: in vitro formation, stability, and pharmacological activity. Drug Metab Dispos. 2010 Sep;38(9):1567-75. doi: 10.1124/dmd.110.033696. Epub 2010 Jun 15. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
Gene Name
UGT2B7
Uniprot ID
P16662
Uniprot Name
UDP-glucuronosyltransferase 2B7
Molecular Weight
60694.12 Da
References
  1. Ebner T, Wagner K, Wienen W: Dabigatran acylglucuronide, the major human metabolite of dabigatran: in vitro formation, stability, and pharmacological activity. Drug Metab Dispos. 2010 Sep;38(9):1567-75. doi: 10.1124/dmd.110.033696. Epub 2010 Jun 15. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGTs are of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isozyme displays activity toward several classes of xeno...
Gene Name
UGT2B15
Uniprot ID
P54855
Uniprot Name
UDP-glucuronosyltransferase 2B15
Molecular Weight
61035.815 Da
References
  1. Ebner T, Wagner K, Wienen W: Dabigatran acylglucuronide, the major human metabolite of dabigatran: in vitro formation, stability, and pharmacological activity. Drug Metab Dispos. 2010 Sep;38(9):1567-75. doi: 10.1124/dmd.110.033696. Epub 2010 Jun 15. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Nadph dehydrogenase (quinone) activity
Specific Function
The enzyme apparently serves as a quinone reductase in connection with conjugation reactions of hydroquinones involved in detoxification pathways as well as in biosynthetic processes such as the vi...
Gene Name
NQO2
Uniprot ID
P16083
Uniprot Name
Ribosyldihydronicotinamide dehydrogenase [quinone]
Molecular Weight
25918.4 Da
References
  1. Michaelis S, Marais A, Schrey AK, Graebner OY, Schaudt C, Sefkow M, Kroll F, Dreger M, Glinski M, Koester H, Metternich R, Fischer JJ: Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). J Med Chem. 2012 Apr 26;55(8):3934-44. doi: 10.1021/jm3001339. Epub 2012 Apr 17. [Article]

Transporters

Kind
Protein
Organism
Humans
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
References
  1. Galanis T, Thomson L, Palladino M, Merli GJ: New oral anticoagulants. J Thromb Thrombolysis. 2011 Apr;31(3):310-20. doi: 10.1007/s11239-011-0559-8. [Article]
  2. Scaglione F: New oral anticoagulants: comparative pharmacology with vitamin K antagonists. Clin Pharmacokinet. 2013 Feb;52(2):69-82. doi: 10.1007/s40262-012-0030-9. [Article]

Drug created on May 03, 2010 18:25 / Updated on May 15, 2021 12:14