Heads up!
We’ve moved some things around. Take a quick tour to learn what has changed.
Take the tour
No thanks!
Dabigatran etexilate
Identification
- Name
- Dabigatran etexilate
- Accession Number
- DB06695
- Description
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
Structure for Dabigatran etexilate (DB06695)
- 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.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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.
Target Actions Organism AProthrombin inhibitorHumans - 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
- Clearance
- Not Available
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- 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.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAbacavir Abacavir may decrease the excretion rate of Dabigatran etexilate which could result in a higher serum level. Abciximab Dabigatran etexilate may increase the anticoagulant activities of Abciximab. Acarbose Acarbose may decrease the excretion rate of Dabigatran etexilate which could result in a higher serum level. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Dabigatran etexilate. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Dabigatran etexilate. Acenocoumarol Dabigatran etexilate may increase the anticoagulant activities of Acenocoumarol. Acetaminophen Acetaminophen may decrease the excretion rate of Dabigatran etexilate which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Dabigatran etexilate which could result in a lower serum level and potentially a reduction in efficacy. Acetylsalicylic acid Dabigatran etexilate may increase the anticoagulant activities of Acetylsalicylic acid. Aclidinium Dabigatran etexilate may decrease the excretion rate of Aclidinium which could result in a higher serum level. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- 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
- Product Ingredients
Ingredient UNII CAS InChI Key Dabigatran etexilate mesilate SC7NUW5IIT 872728-81-9 XETBXHPXHHOLOE-UHFFFAOYSA-N - Active Moieties
Name Kind UNII CAS InChI Key Dabigatran prodrug I0VM4M70GC 211914-51-1 YBSJFWOBGCMAKL-UHFFFAOYSA-N - International/Other Brands
- Pradax (Boehringer Ingelheim) / Rendix
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataPradaxa Capsule 150 mg Oral Boehringer Ingelheim 2008-03-18 Not applicable EU 
Pradaxa Capsule 75 mg/1 Oral Boehringer Ingelheim Pharmaceuticals Inc. 2010-11-08 2010-10-25 US 
Pradaxa Capsule 110 mg/1 Oral Boehringer Ingelheim Pharmaceuticals Inc. 2015-11-23 Not applicable US Pradaxa Capsule 75 mg/1 Oral Boehringer Ingelheim Pharmaceuticals Inc. 2011-08-08 2019-09-30 US Pradaxa Capsule Oral Boehringer Ingelheim (Canada) Ltd Ltee 2008-07-03 Not applicable Canada 
Pradaxa Capsule 110 mg Oral Boehringer Ingelheim 2008-03-18 Not applicable EU Pradaxa Capsule 150 mg Oral Boehringer Ingelheim 2008-03-18 Not applicable EU Pradaxa Capsule 150 mg Oral Boehringer Ingelheim 2008-03-18 Not applicable EU Pradaxa Capsule 150 mg Oral Boehringer Ingelheim 2008-03-18 Not applicable EU Pradaxa Capsule 75 mg Oral Boehringer Ingelheim 2008-03-18 Not applicable EU Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataApo-dabigatran Capsule Oral Apotex Corporation 2019-02-04 Not applicable Canada Apo-dabigatran Capsule Oral Apotex Corporation 2019-02-04 Not applicable Canada Apo-dabigatran Capsule Oral Apotex Corporation 2019-08-14 Not applicable Canada Dabigatran Etexilate Capsule, coated pellets 75 mg/1 Oral Ascend Laboratories, LLC 2020-03-13 2020-03-13 US Dabigatran Etexilate Capsule, coated pellets 150 mg/1 Oral Ascend Laboratories, LLC 2020-03-13 2020-03-13 US Teva-dabigatran Capsule Oral TEVA Canada Limited Not applicable Not applicable Canada Teva-dabigatran Capsule Oral TEVA Canada Limited Not applicable Not applicable Canada Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
Categories
- ATC Codes
- B01AE07 — Dabigatran etexilate
- Drug Categories
- Anticoagulants
- Antithrombins
- Benzimidazoles
- Blood and Blood Forming Organs
- Drugs that are Mainly Renally Excreted
- Enzyme Inhibitors
- Hematologic Agents
- Heterocyclic Compounds, Fused-Ring
- P-glycoprotein substrates
- Protease Inhibitors
- Pyridines
- Serine Protease Inhibitors
- UGT1A9 Substrates
- UGT2B7 substrates
- 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)
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
- 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. [PubMed:17764540]
- 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. [PubMed:17869635]
- 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. [PubMed:23292752]
- 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. [PubMed:20551237]
- 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. [PubMed:23408233]
- FDA Drug Approval Package for Dabigatran Etexilate [Link]
- Apotex Inc. Product Monograph: Dabigatran Etexilate [File]
- External Links
- Human Metabolome Database
- HMDB0015641
- KEGG Drug
- D07144
- PubChem Compound
- 6445226
- PubChem Substance
- 99443249
- ChemSpider
- 4948999
- BindingDB
- 50432209
- 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
Phase Status Purpose Conditions Count 4 Active Not Recruiting Prevention Atrial Fibrillation (AF) / Device Related Thrombus / Left Atrial Appendage Thrombosis / Watchman LAA Closure Device 1 4 Active Not Recruiting Supportive Care Atrial Fibrillation (AF) / Flutter, Atrial 1 4 Active Not Recruiting Treatment Atrial Fibrillation (AF) / Valve Heart Disease 1 4 Completed Basic Science Venous Thromboembolism 1 4 Completed Prevention Arthroplasty, Replacement / Moderate Renal Impairment (CrCl 30-50 mL/Min) / Prevention of Venous Thromboembolism 1 4 Completed Prevention Atrial Fibrillation (AF) 2 4 Completed Treatment Atrial Fibrillation (AF) 3 4 Completed Treatment Coronary Heart Disease (CHD) 1 4 Enrolling by Invitation Treatment Atrial Fibrillation (AF) 1 4 Not Yet Recruiting Prevention Atrial Fibrillation (AF) / Mitral Valve Stenosis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule, coated pellets Oral 150 mg/1 Capsule, coated pellets Oral 75 mg/1 Capsule Oral 110 mg Capsule Oral 110 mg/1 Capsule Oral 150 mg/1 Capsule Oral 150 mg Capsule Oral 75 mg Capsule Oral 75 mg/1 Capsule Oral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataUS9034822 No 2015-05-19 2031-01-20 US US6087380 No 2000-07-11 2018-02-18 US US7932273 No 2011-04-26 2025-09-07 US US7866474 No 2011-01-11 2027-08-31 US US9925174 No 2018-03-27 2023-06-14 US Additional Data Available- Filed On
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 132 http://www.chemspider.com/Chemical-Structure.8615298.html water solubility 1.8mg/ml, partly soluble MSDS logP 3.8 Apotex Inc. Product Monograph: Dabigatran Etexilate - Predicted Properties
Property Value Source Water Solubility 0.00466 mg/mL ALOGPS logP 5.17 ALOGPS logP 4.59 ChemAxon logS -5.1 ALOGPS pKa (Strongest Acidic) 17.89 ChemAxon pKa (Strongest Basic) 4.48 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 8 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 154.03 Å2 ChemAxon Rotatable Bond Count 17 ChemAxon Refractivity 176.43 m3·mol-1 ChemAxon Polarizability 70.65 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 0 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.942 Blood Brain Barrier + 0.8673 Caco-2 permeable - 0.7014 P-glycoprotein substrate Substrate 0.7412 P-glycoprotein inhibitor I Inhibitor 0.7539 P-glycoprotein inhibitor II Inhibitor 0.8443 Renal organic cation transporter Non-inhibitor 0.701 CYP450 2C9 substrate Non-substrate 0.858 CYP450 2D6 substrate Non-substrate 0.837 CYP450 3A4 substrate Substrate 0.6154 CYP450 1A2 substrate Non-inhibitor 0.6906 CYP450 2C9 inhibitor Non-inhibitor 0.5102 CYP450 2D6 inhibitor Non-inhibitor 0.8417 CYP450 2C19 inhibitor Inhibitor 0.5157 CYP450 3A4 inhibitor Inhibitor 0.781 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.5789 Ames test Non AMES toxic 0.6292 Carcinogenicity Non-carcinogens 0.8065 Biodegradation Not ready biodegradable 0.9931 Rat acute toxicity 2.7093 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9047 hERG inhibition (predictor II) Inhibitor 0.6181
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-00kk-0981100000-78856b63936cf67ebce2 MS/MS Spectrum - , positive LC-MS/MS splash10-004r-0292116000-55b368cbe92da888e681
Targets
- 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
- 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. [PubMed:19756950]
- 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. [PubMed:17061960]
- Karthikeyan G, Eikelboom JW, Hirsh J: Dabigatran: ready for prime time? Pol Arch Med Wewn. 2010 Apr;120(4):137-42. [PubMed:20424539]
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
- 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. [PubMed:23239178]
- 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
- 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. [PubMed:23239178]
- 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
- 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. [PubMed:20551237]
- 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
- 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. [PubMed:20551237]
- 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
- 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. [PubMed:20551237]
- 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
- 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. [PubMed:22494098]
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
- 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. [PubMed:21327511]
- 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. [PubMed:23292752]
Drug created on May 03, 2010 12:25 / Updated on August 05, 2020 23:35
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
![]({"CS-Molecular-Health-1.jpg":"/assets/ads/CS-Molecular-Health-1-19e76f023997d5ac198da2cb9976457f7b9ba733f0ea8a780fe21191c759e8fa.jpg","Drug-Dev-2.jpg":"/assets/ads/Drug-Dev-2-7c3039d93245f493c23278efbf759e4f933848a676262d579087d5cc516af179.jpg","Drug-Search-3.jpg":"/assets/ads/Drug-Search-3-7346c33d2133f62b46cbfbbe2b666e78f955c6847e242692c6081fec37c4d10d.jpg","PM-3.jpg":"/assets/ads/PM-3-13494ac4c996d71619127a11f685681418d4280832dec162c0b2c9c8bc2eda50.jpg","OD-Webinar-1.jpg":"/assets/ads/OD-Webinar-1-f9357f6d57fef5e411aa1c0439ef46c86d9151214434659d096eeed6407b799b.jpg","DDI-3.jpg":"/assets/ads/DDI-3-12808cf864d540ad43757b10b08fc52ae93e793b0c6e81345555187b2840ad09.jpg","EMR-2.jpg":"/assets/ads/EMR-2-adacf8de3f42cb06d6676d06fce611c29781db6ad30776cd18b72a7d8e69f0c8.jpg","Covid.jpg":"/assets/ads/Covid-eed8f17668b0308db62ce3c656f5e2f562376e9185ae08dda5ce6ed9ab0bbd1f.jpg","CS-Molecular-Health-2.jpg":"/assets/ads/CS-Molecular-Health-2-22f41f94b3f87e44a1dcaa8f6c03dc411ab69558efd4f3148ff9bb6adaa956dc.jpg","OD-Webinar-2.jpg":"/assets/ads/OD-Webinar-2-ce7fd7bb39a487a49cbba56253322d2f5f19274f73394eb7f228e22d03ff5211.jpg","PM-5.jpg":"/assets/ads/PM-5-d0dc031e0fa0d0097d912eff07b7e80b27b867264dd5b055e379a57bfa2a8723.jpg","DDI-4.jpg":"/assets/ads/DDI-4-313b9c374b937fd78bb2ade652b9b030abb9e6cb90efd35833f793e384e8185b.jpg","EMR-3.jpg":"/assets/ads/EMR-3-a42ad923ae639012d6798326aa12cde3a950f13c84333b88ee28467db4ad1eaa.jpg","twoXAR-1.jpg":"/assets/ads/twoXAR-1-e2061afa34dd185640cb74a3a0efc3b15e0acbf12e2d1567ce077fedf19fdcfa.jpg","twoXAR-2.jpg":"/assets/ads/twoXAR-2-553e26bc0248fd52f9bf0422512e0374a03cc1c7d218552bb1640f30fd27df7a.jpg","twoXAR-3.jpg":"/assets/ads/twoXAR-3-af4296dd5d3298c2de0957a3f3ca400cf52a6921b50e7f0567a65efea0c5e27f.jpg","twoXAR-4.jpg":"/assets/ads/twoXAR-4-e52d48f8ffa5b12e1555a4d694bffc5702614d51925f9757ea67981da5d83ef4.jpg","twoXAR-5.jpg":"/assets/ads/twoXAR-5-dadf0af8d54f7c3f9bf3d3b4383fd80fa9a51acad26f5793b4395a5d311cc3f1.jpg"})
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates