Identification
- Summary
Rivaroxaban is a factor Xa inhibitor used to treat deep vein thrombosis (DVT) and pulmonary embolism (PE). May also be used as thrombosis prophylaxis in specific situations.
- Brand Names
- Xarelto
- Generic Name
- Rivaroxaban
- DrugBank Accession Number
- DB06228
- Background
Rivaroxaban is an anticoagulant and the first orally active direct factor Xa inhibitor. Unlike warfarin, routine lab monitoring of INR is not necessary. However there is no antidote available in the event of a major bleed. Only the 10 mg tablet can be taken without regard to food. The 15 mg and 20 mg tablet should be taken with food. FDA approved on July 1, 2011.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Rivaroxaban (DB06228)
- Weight
- Average: 435.881
Monoisotopic: 435.065569098 - Chemical Formula
- C19H18ClN3O5S
- Synonyms
- Rivaroxaban
- External IDs
- BAY 59-7939
- BAY-59-7939
- JNJ-39039039
- JNJ39039039
Pharmacology
- Indication
Rivaroxaban is indicated for the prevention of venous thromboembolic events (VTE) in patients who have undergone total hips replacements and total knee replacement surgery; prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation; treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE); to reduce risk of recurrent DVT and/or PE. Rivaroxaban is also indicated, in combination with aspirin, for reducing the risk of major cardiovascular events in patients with chronic coronary artery disease or peripheral artery disease. Its use is also not recommended in those with severe renal impairment (<30mL/min).7
Rivaroxaban is also indicated for the treatment and prevention of VTE in pediatric patients (from birth to 18 years of age) and for thromboprophylaxis in pediatric patients ≥2 years old with congenital heart disease following the Fontan procedure.7
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to prevent Cardiovascular death Regimen in combination with: Acetylsalicylic acid (DB00945) •••••••••••• ••••••• •••• •••••• Prophylaxis of Deep vein thrombosis •••••••••••• ••••••• •••• •••••• Treatment of Deep vein thrombosis •••••••••••• ••••••• •••• •••••• Prophylaxis of Deep vein thrombosis •••••••••••• ••••••• •••• •••••• Prevention of Major adverse cardiovascular events •••••••••••• •••••••• •••••• ••••••• ••••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Rivaroxaban is an anticoagulant which binds directly to factor Xa. Thereafter, it effectively blocks the amplification of the coagulation cascade, preventing the formation of thrombus. Rivaroxaban is a unqiue anticoagulant for two reasons. First of all, it is does not involve antithrombin III (ATIII) to exert its anticoagulant effects. Secondly, it is an oral agent whereas the widely used unfractionated heparin and low molecular weight heparins are for parenteral use only. Although the activated partial thromboplastin time (aPTT) and HepTest (a test developed to assay low molecular weight heparins) are prolonged in a dose-dependant manner, neither test is recommended for the assessment of the pharmacodynamic effects of rivaroxaban. Anti-Xa activity and inhibition of anti-Xa activity monitoring is also not recommended despite being influenced by rivaroxaban.
- Mechanism of action
Rivaroxaban competitively inhibits free and clot bound factor Xa. Factor Xa is needed to activate prothrombin (factor II) to thrombin (factor IIa). Thrombin is a serine protease that is required to activate fibrinogen to fibrin, which is the loose meshwork that completes the clotting process. Since one molecule of factor Xa can generate more than 1000 molecules of thrombin, selective inhibitors of factor Xa are profoundly useful in terminating the amplification of thrombin generation. The action of rivaroxaban is irreversible.
Target Actions Organism ACoagulation factor X antagonistHumans - Absorption
Following oral administration, rivaroxaban is rapidly absorbed and reaches peak plasma concentration in 2-4 hours. Bioavailability of the 10 mg dose is >80%. However, the 15-20 mg dose have a lower bioavailability if taken in the fasted state and consequently should be taken with food.
- Volume of distribution
The steady state Vd is 50 L
- Protein binding
Plasma protein binding is about 92% to 95%
- Metabolism
Approximately two-thirds of the dose is metabolized. It is metabolized by CYP3A4, CYP3A5, CYP2J2 and CYP-independant mechanisms
- Route of elimination
Approximately two-thirds of rivaroxaban is excreted into urine (via active tubular secretion in which approximately 36% as unchanged drug and 30% as inactive metabolism). The remaining third of the administered dose is excreted via feces in which 7% is in the form of unchanged drug and 21% as inactive metabolites.
- Half-life
The terminal half life is 5-9 hours in adults and 11-13 hours in the elderly.
- Clearance
Systemic clearance is approximately 10 L/h, so rivaroxaban is considered a drug with low clearance. Renal clearance is ~3-4 L/h.
- Adverse Effects
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Excessive bleeding. Overdosages should be treated using activated charcoal and supportive measures such as mechanical compression and hemodynamic support. If bleeding is not controlled, the following procoagulants can be administered: activated prothrombin complex concentrate, prothrombin complex concentrate and recombinant factor VIIa. There is also a higher chance of post procedural hemorrhage compared to enoxaparin (1.55% vs. 1.39% respectively).
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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 Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Rivaroxaban which could result in a higher serum level. Abametapir The serum concentration of Rivaroxaban can be increased when it is combined with Abametapir. Abatacept The metabolism of Rivaroxaban can be increased when combined with Abatacept. Abciximab Abciximab may increase the anticoagulant activities of Rivaroxaban. Abemaciclib Abemaciclib may decrease the excretion rate of Rivaroxaban which could result in a higher serum level. - 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. Co-administration will decrease levels of this medication.
- Take with food. Rivaroxaban 15-20mg dose should be taken with food as food significantly impacts the bioavailability at that dose.
- Take with or without food. Rivaroxaban 10mg dose can be taken with or without food as it does not significantly impact the bioavailability at that dose.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Nra-rivaroxaban Tablet 20 mg Oral Nora Pharma Inc Not applicable Not applicable Canada 
Nra-rivaroxaban Tablet 2.5 mg Oral Nora Pharma Inc Not applicable Not applicable Canada Nra-rivaroxaban Tablet 15 mg Oral Nora Pharma Inc Not applicable Not applicable Canada Nra-rivaroxaban Tablet 10 mg Oral Nora Pharma Inc Not applicable Not applicable Canada Pmsc-rivaroxaban Tablet 15 mg Oral Pharmascience Inc Not applicable Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ach-rivaroxaban Tablet 10 mg Oral Accord Healthcare Inc Not applicable Not applicable Canada Ach-rivaroxaban Tablet 20 mg Oral Accord Healthcare Inc Not applicable Not applicable Canada Ach-rivaroxaban Tablet 15 mg Oral Accord Healthcare Inc Not applicable Not applicable Canada Ach-rivaroxaban Tablet 2.5 mg Oral Accord Healthcare Inc Not applicable Not applicable Canada Apo-rivaroxaban Tablet 10 mg Oral Apotex Corporation 2023-11-01 Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image XARELTO Rivaroxaban (15 MG) + Rivaroxaban (20 MG) Tablet, film coated Oral Bayer Ag 2018-09-04 Not applicable Italy 
Xarelto Rivaroxaban (15 mg) + Rivaroxaban (20 mg) Kit; Tablet Oral Bayer 2015-11-02 2018-12-01 Canada XARELTO Rivaroxaban (15 MG) + Rivaroxaban (20 MG) Tablet, film coated Oral Bayer Ag 2018-09-04 Not applicable Italy Xarelto Rivaroxaban (15 mg/1) + Rivaroxaban (20 mg/1) Kit; Tablet, film coated Oral Janssen Pharmaceuticals, Inc. 2014-09-16 Not applicable US 
Xarelto Rivaroxaban (15 mg) + Rivaroxaban (20 mg) Kit; Tablet Oral Bayer 2015-11-02 2018-12-01 Canada
Categories
- ATC Codes
- B01AF01 — Rivaroxaban
- Drug Categories
- Anticoagulants
- Antithrombins
- BCRP/ABCG2 Substrates
- Blood and Blood Forming Organs
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Substrates
- Direct factor Xa inhibitors
- Drugs that are Mainly Renally Excreted
- Enzyme Inhibitors
- Factor Xa Inhibitors
- Hematologic Agents
- Morpholines
- Oxazines
- P-glycoprotein substrates
- Protease Inhibitors
- Serine Protease Inhibitors
- Sulfur Compounds
- Thiophenes
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylmorpholines. These are aromatic compounds containing a morpholine ring and a benzene ring linked to each other through a CC or a CN bond.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Oxazinanes
- Sub Class
- Morpholines
- Direct Parent
- Phenylmorpholines
- Alternative Parents
- Thiophene carboxamides / 2-heteroaryl carboxamides / 2,5-disubstituted thiophenes / Oxazolidinones / Aryl chlorides / Benzene and substituted derivatives / Tertiary carboxylic acid amides / Carbamate esters / Heteroaromatic compounds / Secondary carboxylic acid amides show 11 more
- Substituents
- 2,5-disubstituted thiophene / 2-heteroaryl carboxamide / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Carbamic acid ester / Carbonic acid derivative / Carbonyl group show 25 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- monocarboxylic acid amide, organochlorine compound, thiophenes, lactam, aromatic amide, morpholines, oxazolidinone (CHEBI:68579)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 9NDF7JZ4M3
- CAS number
- 366789-02-8
- InChI Key
- KGFYHTZWPPHNLQ-AWEZNQCLSA-N
- InChI
- InChI=1S/C19H18ClN3O5S/c20-16-6-5-15(29-16)18(25)21-9-14-10-23(19(26)28-14)13-3-1-12(2-4-13)22-7-8-27-11-17(22)24/h1-6,14H,7-11H2,(H,21,25)/t14-/m0/s1
- IUPAC Name
- 5-chloro-N-{[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl}thiophene-2-carboxamide
- SMILES
- ClC1=CC=C(S1)C(=O)NC[C@H]1CN(C(=O)O1)C1=CC=C(C=C1)N1CCOCC1=O
References
- Synthesis Reference
Prabhudas BODHURI, Gamini Weeratunga, "PROCESSES FOR THE PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF." U.S. Patent US20100273790, issued October 28, 2010.
US20100273790- General References
- Piccini JP, Patel MR, Mahaffey KW, Fox KA, Califf RM: Rivaroxaban, an oral direct factor Xa inhibitor. Expert Opin Investig Drugs. 2008 Jun;17(6):925-37. doi: 10.1517/13543784.17.6.925 . [Article]
- Alban S: Pharmacological strategies for inhibition of thrombin activity. Curr Pharm Des. 2008;14(12):1152-75. [Article]
- Stevenson M, Scope A, Holmes M, Rees A, Kaltenthaler E: Rivaroxaban for the prevention of venous thromboembolism: a single technology appraisal. Health Technol Assess. 2009 Oct;13 Suppl 3:43-8. doi: 10.3310/hta13suppl3/07. [Article]
- Imberti D, Dall'Asta C, Pierfranceschi MG: Oral factor Xa inhibitors for thromboprophylaxis in major orthopedic surgery: a review. Intern Emerg Med. 2009 Dec;4(6):471-7. doi: 10.1007/s11739-009-0293-9. [Article]
- Alexander D, Jeremias A: Rivaroxaban in the contemporary treatment of acute coronary syndromes. Expert Opin Investig Drugs. 2011 Jun;20(6):849-57. doi: 10.1517/13543784.2011.580274. Epub 2011 May 10. [Article]
- Cabral KP: Pharmacology of the new target-specific oral anticoagulants. J Thromb Thrombolysis. 2013 Aug;36(2):133-40. doi: 10.1007/s11239-013-0929-5. [Article]
- FDA Approved Products: XARELTO (rivaroxaban) tablets or suspension, for oral use [Link]
- FDA Approved Drug Products: Xarelto (rivaroxaban) tablets/suspension for oral administration (February 2023) [Link]
- External Links
- KEGG Drug
- D07086
- PubChem Compound
- 9875401
- PubChem Substance
- 175427064
- ChemSpider
- 8051086
- BindingDB
- 7840
- 1114195
- ChEBI
- 68579
- ChEMBL
- CHEMBL198362
- ZINC
- ZINC000003964126
- PDBe Ligand
- RIV
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Rivaroxaban
- PDB Entries
- 2w26 / 5vof
- MSDS
- Download (480 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Prevention Atrial Fibrillation / Stroke 1 4 Active Not Recruiting Treatment Coronary Artery Disease (CAD) 1 4 Completed Basic Science Acute Coronary Syndrome (ACS) / Atrial Fibrillation 1 4 Completed Basic Science Atrial Fibrillation or Pulmonary Embolism / Existent Coronary or Valvular Calcification, or Both and Agatston Score > 50 in at Least One Location / Need of Long Term Oral Anticoagulation Therapy (OAT) 1 4 Completed Basic Science Venous Thromboembolism 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 15.000 mg Tablet Oral 10.000 mg Tablet, coated Oral 15 mg Tablet Oral 2.500 mg Tablet, film coated Oral 15 MG Tablet, film coated Oral 20 MG Tablet, film coated Oral 15 mg/20mg Tablet, film coated Oral Capsule Oral 15 mg Capsule Oral 20 mg Capsule Oral 10 MG Capsule Oral 2.5 MG Tablet Oral 10.0000 mg Granule Oral 1 MG/ML Granule, for suspension Oral 103.4 mg / bottle Granule, for suspension Oral 155 mg/1 Granule, for suspension Oral 51.7 mg / bottle Kit; tablet Oral Kit; tablet, film coated Oral Suspension Oral 103.40 mg Tablet Oral 10 mg Tablet Oral 10.00 mg Tablet Oral 15 mg Tablet Oral 2.5 mg Tablet Oral 20 mg Tablet, film coated Oral Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 15 mg/1 Tablet, film coated Oral 2.5 mg/1 Tablet, film coated Oral 20 mg/1 Tablet, film coated Oral 10 mg Tablet, film coated Oral 15.00 mg Tablet, film coated Oral 20.00 mg Tablet, coated Oral Tablet Oral 20.000 mg Tablet, coated Oral 2.5 mg Tablet, film coated Oral 2.5 mg Tablet, coated Oral 10 mg Tablet, coated Oral 20 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2396561 No 2008-10-14 2020-12-11 Canada CA2547113 No 2012-01-24 2024-11-13 Canada US7157456 Yes 2007-01-02 2025-02-28 US US7585860 No 2009-09-08 2020-12-11 US US7592339 No 2009-09-22 2020-12-11 US US9539218 Yes 2017-01-10 2034-08-17 US US9415053 Yes 2016-08-16 2025-05-13 US US10828310 Yes 2020-11-10 2039-07-31 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.01 mg/mL ALOGPS logP 1.74 ALOGPS logP 1.9 Chemaxon logS -4.6 ALOGPS pKa (Strongest Acidic) 13.6 Chemaxon pKa (Strongest Basic) -1.6 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 88.18 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 104.74 m3·mol-1 Chemaxon Polarizability 43.39 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9966 Blood Brain Barrier + 0.9462 Caco-2 permeable + 0.6822 P-glycoprotein substrate Non-substrate 0.5691 P-glycoprotein inhibitor I Inhibitor 0.6325 P-glycoprotein inhibitor II Inhibitor 0.5601 Renal organic cation transporter Non-inhibitor 0.7562 CYP450 2C9 substrate Non-substrate 0.7866 CYP450 2D6 substrate Non-substrate 0.8761 CYP450 3A4 substrate Substrate 0.5964 CYP450 1A2 substrate Non-inhibitor 0.6469 CYP450 2C9 inhibitor Non-inhibitor 0.7035 CYP450 2D6 inhibitor Non-inhibitor 0.7516 CYP450 2C19 inhibitor Inhibitor 0.6475 CYP450 3A4 inhibitor Non-inhibitor 0.6667 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7463 Ames test Non AMES toxic 0.6162 Carcinogenicity Non-carcinogens 0.8838 Biodegradation Not ready biodegradable 0.9844 Rat acute toxicity 2.4353 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8938 hERG inhibition (predictor II) Inhibitor 0.6205
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-000i-0000900000-e6e423d4ca7f5ebe5767 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-052f-1934300000-ba2cc97a89aca3b5799e Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-002r-0032900000-f5c321968bcf6c28d9fd Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-00mo-0194100000-912ba9638c151892a3a2 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0kfx-2138900000-6669bf414df224cf238f Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-047l-3189200000-766cf9fb0d8b855bc057 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 193.4684 predictedDeepCCS 1.0 (2019) [M+H]+ 195.8264 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.34598 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Serine-type endopeptidase activity
- Specific Function
- Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
- Gene Name
- F10
- Uniprot ID
- P00742
- Uniprot Name
- Coagulation factor X
- Molecular Weight
- 54731.255 Da
References
- Melillo SN, Scanlon JV, Exter BP, Steinberg M, Jarvis CI: Rivaroxaban for thromboprophylaxis in patients undergoing major orthopedic surgery. Ann Pharmacother. 2010 Jun;44(6):1061-71. doi: 10.1345/aph.1M681. Epub 2010 Apr 27. [Article]
- Ufer M: Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development. Thromb Haemost. 2010 Mar;103(3):572-85. doi: 10.1160/TH09-09-0659. Epub 2010 Feb 2. [Article]
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- This enzyme metabolizes arachidonic acid predominantly via a NADPH-dependent olefin epoxidation to all four regioisomeric cis-epoxyeicosatrienoic acids. One of the predominant enzymes responsible f...
- Gene Name
- CYP2J2
- Uniprot ID
- P51589
- Uniprot Name
- Cytochrome P450 2J2
- Molecular Weight
- 57610.165 Da
References
- Ufer M: Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development. Thromb Haemost. 2010 Mar;103(3):572-85. doi: 10.1160/TH09-09-0659. Epub 2010 Feb 2. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- 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 oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Cabral KP: Pharmacology of the new target-specific oral anticoagulants. J Thromb Thrombolysis. 2013 Aug;36(2):133-40. doi: 10.1007/s11239-013-0929-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
References
- Mismetti P, Laporte S: [Rivaroxaban: clinical pharmacology]. Ann Fr Anesth Reanim. 2008 Dec;27 Suppl 3:S16-21. doi: 10.1016/S0750-7658(08)75142-6. [Article]
- Ufer M: Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development. Thromb Haemost. 2010 Mar;103(3):572-85. doi: 10.1160/TH09-09-0659. Epub 2010 Feb 2. [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
- Walenga JM, Adiguzel C: Drug and dietary interactions of the new and emerging oral anticoagulants. Int J Clin Pract. 2010 Jun;64(7):956-67. doi: 10.1111/j.1742-1241.2009.02286.x. [Article]
- Chen T, Lam S: Rivaroxaban: an oral direct factor Xa inhibitor for the prevention of thromboembolism. Cardiol Rev. 2009 Jul-Aug;17(4):192-7. doi: 10.1097/CRD.0b013e3181aa2154. [Article]
- FDA Approved Products: XARELTO (rivaroxaban) tablets or suspension, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
Drug created at March 19, 2008 16:18 / Updated at February 20, 2024 23:54