Apixaban

Identification

Summary

Apixaban is an anticoagulant used for the prophylaxis of stroke and systemic embolism in nonvalvular atrial fibrillation, and deep vein thrombosis(DVT) leading to pulmonary embolism(PE), including in patients after a hip or knee replacement surgery.

Brand Names
Eliquis
Generic Name
Apixaban
DrugBank Accession Number
DB06605
Background

Apixaban is an oral, direct, and highly selective factor Xa (FXa) inhibitor of both free and bound FXa, as well as prothrombinase, independent of antithrombin III for the prevention and treatment of thromboembolic diseasesLabel,2. It is marketed under the name EliquisLabel,3. Apixaban was approved by the FDA on December 28, 20123.

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 459.4971
Monoisotopic: 459.190654313
Chemical Formula
C25H25N5O4
Synonyms
  • apixabán
  • Apixaban
  • apixabanum
External IDs
  • BMS 562247-01
  • BMS-562247
  • BMS-562247-01

Pharmacology

Indication

Apixaban is indicated for reducing the risk of stroke and systemic embolism in patients who have nonvalvular atrial fibrillation, prophylaxis of deep vein thrombosis(DVT) leading to pulmonary embolism(PE) in patients after a hip or knee replacement surgery, and treatment of DVT and PE to reduce the risk of recurrenceLabel,1,2.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Prophylaxis ofDeep vein thrombosis••••••••••••••••••
Prophylaxis ofDeep vein thrombosis••••••••••••••••••
Treatment ofDeep vein thrombosis••••••••••••••••••
Treatment ofPulmonary embolism••••••••••••••••••
Prophylaxis ofRecurrent pulmonary embolism••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin IIILabel. Apixaban also inhibits prothrominaseLabel. These effects prevent the formation of a thrombusLabel.

Mechanism of action

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin IIILabel. Apixaban also inhibits prothrominaseLabel. These effects prevent the formation of a thrombusLabel.

TargetActionsOrganism
ACoagulation factor X
inhibitor
Humans
Absorption

Apixaban is approximately 50% bioavailableLabel though other studies report 43-46% oral bioavailability1.

Volume of distribution

Approximately 21LLabel.

Protein binding

92-94%Label.

Metabolism

50% of the orally administered dose is excreted as the unchanged parent compound, however 25% of the dose is excreted as O-demethyl apixaban sulfateLabel,1. All apixaban metabolites account for approximately 32% of the excreted dose though the structure of all metabolites are not well defined1. Apixaban is mainly metabolized by cytochrome p450(CYP)3A4 and to a lesser extent by CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2J2Label.

Hover over products below to view reaction partners

Route of elimination

56% of an orally administered dose is recovered in the feces and 24.5-28.8% of the dose is recovered in the urineLabel,1,2. 83-88% of the dose recovered in the urine was the unchanged parent compound1.

Half-life

12.7±8.55hLabel,1,2.

Clearance

3.3L/hLabel though other studies report 4876mL/h1.

Adverse Effects
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Toxicity

Animal studies have shown an increased risk of maternal bleeding during pregnancy but no increase in fetal malformations or fetal or maternal deathsLabel. It is unknown if this animal data also translates to humans so apixaban should only be used in pregnancy if the benefits outweigh the risksLabel. It is not know whether apixaban is safe and effective in labor and during birth, though animal studies have shown an increased rate of maternal bleedingLabel. Animal studies in rats show apixaban excreted in milk, though it is not know if this also applies to humansLabel. Nursing mothers should either stop breastfeeding or stop taking apixaban depending on the risk and benefit of each optionLabel. Studies to determine safety and effectiveness in pediatric patients have yet to be performedLabel. Studies that involved geriatric patients (at least 75 years old) saw no difference in safety or effectiveness compared to younger patients, though geriatric patients at an especially advanced age may be more susceptible to adverse effectsLabel. Dosage adjustments for patients with end stage renal disease(ESRD) are based on estimates of pharmacokinetic principles and not clinical studyLabel. Patients with ESRD may experience pharmacodynamics similar to those seen in well controlled studies but it may not lead to the same clinical effectsLabel. Dosage adjustments are not necessary in mild hepatic impairmentLabel. In moderate hepatic impairment patients may already experience abnormalities in coagulation and so no dose recommendations are possibleLabel. Apixaban is not recommended for patients with severe hepatic impairmentLabel.

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.
DrugInteraction
AbametapirThe serum concentration of Apixaban can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Apixaban can be increased when combined with Abatacept.
AbciximabApixaban may increase the anticoagulant activities of Abciximab.
AbemaciclibAbemaciclib may decrease the excretion rate of Apixaban which could result in a higher serum level.
AbirateroneThe metabolism of Apixaban can be decreased when combined with Abiraterone.
Food Interactions
  • Avoid grapefruit products.
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • Avoid St. John's Wort. St. John's Wort will decrease levels of this medication.
  • Take with or without food.

Products

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Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ApixabanTablet5 mgOralSivem Pharmaceuticals Ulc2022-11-01Not applicableCanada flag
ApixabanTablet2.5 mgOralSivem Pharmaceuticals Ulc2022-11-01Not applicableCanada flag
Apixaban AccordTablet2.5 mgOralAccord Healthcare S.L.U.2021-02-08Not applicableEU flag
Apixaban AccordTablet5 mgOralAccord Healthcare S.L.U.2021-02-08Not applicableEU flag
Apixaban AccordTablet5 mgOralAccord Healthcare S.L.U.2021-02-08Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ach-apixabanTablet2.5 mgOralAccord Healthcare Inc2022-09-27Not applicableCanada flag
Ach-apixabanTablet5 mgOralAccord Healthcare Inc2022-09-27Not applicableCanada flag
Ag-apixabanTablet2.5 mgOralAngita Pharma Inc.2022-10-28Not applicableCanada flag
Ag-apixabanTablet5 mgOralAngita Pharma Inc.2022-10-28Not applicableCanada flag
ApixabanTablet, film coated2.5 mg/1OralIndoco Remedies Limited2020-09-16Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
ELIQUIS 30-Day Starter PackApixaban (5 mg/1) + Apixaban (5 mg/1)Kit; Tablet, coatedOralE.R. Squibb & Sons, L.L.C.2017-11-29Not applicableUS flag
ELIQUIS 30-Day Starter PackApixaban (5 mg/1) + Apixaban (5 mg/1)Kit; Tablet, coatedOralE.R. Squibb & Sons, L.L.C.2017-11-29Not applicableUS flag

Categories

ATC Codes
B01AF02 — Apixaban
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Piperidines
Sub Class
Phenylpiperidines
Direct Parent
Phenylpiperidines
Alternative Parents
Phenylpyrazoles / Pyridinecarboxamides / Methoxyanilines / 2-heteroaryl carboxamides / Pyrazole-5-carboxamides / Anisoles / Phenoxy compounds / Methoxybenzenes / Alkyl aryl ethers / Delta lactams
show 10 more
Substituents
2-heteroaryl carboxamide / Alkyl aryl ether / Anisole / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Carbonyl group / Carboxamide group / Carboxylic acid derivative
show 24 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
aromatic ether, lactam, piperidones, pyrazolopyridine (CHEBI:72296)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
3Z9Y7UWC1J
CAS number
503612-47-3
InChI Key
QNZCBYKSOIHPEH-UHFFFAOYSA-N
InChI
InChI=1S/C25H25N5O4/c1-34-19-11-9-18(10-12-19)30-23-20(22(27-30)24(26)32)13-15-29(25(23)33)17-7-5-16(6-8-17)28-14-3-2-4-21(28)31/h5-12H,2-4,13-15H2,1H3,(H2,26,32)
IUPAC Name
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridine-3-carboxamide
SMILES
COC1=CC=C(C=C1)N1N=C(C(N)=O)C2=C1C(=O)N(CC2)C1=CC=C(C=C1)N1CCCCC1=O

References

General References
  1. Raghavan N, Frost CE, Yu Z, He K, Zhang H, Humphreys WG, Pinto D, Chen S, Bonacorsi S, Wong PC, Zhang D: Apixaban metabolism and pharmacokinetics after oral administration to humans. Drug Metab Dispos. 2009 Jan;37(1):74-81. doi: 10.1124/dmd.108.023143. Epub 2008 Oct 2. [Article]
  2. Granger CB, Alexander JH, McMurray JJ, Lopes RD, Hylek EM, Hanna M, Al-Khalidi HR, Ansell J, Atar D, Avezum A, Bahit MC, Diaz R, Easton JD, Ezekowitz JA, Flaker G, Garcia D, Geraldes M, Gersh BJ, Golitsyn S, Goto S, Hermosillo AG, Hohnloser SH, Horowitz J, Mohan P, Jansky P, Lewis BS, Lopez-Sendon JL, Pais P, Parkhomenko A, Verheugt FW, Zhu J, Wallentin L: Apixaban versus warfarin in patients with atrial fibrillation. N Engl J Med. 2011 Sep 15;365(11):981-92. doi: 10.1056/NEJMoa1107039. Epub 2011 Aug 27. [Article]
  3. FDA Drug Approval Package: Apixaban [Link]
KEGG Drug
D03213
PubChem Compound
10182969
PubChem Substance
175427077
ChemSpider
8358471
BindingDB
19023
RxNav
1364430
ChEBI
72296
ChEMBL
CHEMBL231779
ZINC
ZINC000011677837
PharmGKB
PA166163740
PDBe Ligand
GG2
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Apixaban
PDB Entries
2p16 / 6w70
FDA label
Download (926 KB)
MSDS
Download (52.4 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentDeep Vein Thrombosis / Pulmonary Embolism / Venous Thromboembolism1
4CompletedNot AvailableEnd Stage Renal Disease (ESRD)1
4CompletedBasic ScienceObesity / Post-gastrointestinal bypass surgery1
4CompletedDiagnosticLeft Atrial Appendage Occlusion1
4CompletedOtherAcute Coronary Syndrome (ACS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral2.500 mg
TabletOral2.5 mg
TabletOral5 mg
Tablet, film coatedOral
Tablet, film coatedOral2.5 mg/1
Tablet, film coatedOral2.5 MG
Tablet, film coatedOral5 MG
Tablet, film coatedOral5 mg/1
Tablet, coatedOral2.5 mg
Kit; tablet, coatedOral
TabletOral5.000 mg
Tablet, coatedOral5 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2349330No2009-09-292019-12-17Canada flag
CA2461202No2011-07-122022-09-17Canada flag
US6413980No2002-07-022019-12-22US flag
US6967208No2005-11-222023-02-03US flag
US9326945No2016-05-032031-02-24US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)326.53[MSDS]
boiling point (°C)770.5[MSDS]
water solubility0.11mg/mLhttp://www.chemspider.com/Chemical-Structure.8358471.html?rid=2f601343-f676-4fcd-ad7d-1151c737876f
logP2.71[MSDS]
Predicted Properties
PropertyValueSource
Water Solubility0.0679 mg/mLALOGPS
logP2.22ALOGPS
logP1.83Chemaxon
logS-3.8ALOGPS
pKa (Strongest Acidic)13.07Chemaxon
pKa (Strongest Basic)-1.6Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area110.76 Å2Chemaxon
Rotatable Bond Count5Chemaxon
Refractivity126.9 m3·mol-1Chemaxon
Polarizability49.74 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9974
Blood Brain Barrier+0.9329
Caco-2 permeable-0.5308
P-glycoprotein substrateSubstrate0.6144
P-glycoprotein inhibitor IInhibitor0.6804
P-glycoprotein inhibitor IIInhibitor0.594
Renal organic cation transporterNon-inhibitor0.5628
CYP450 2C9 substrateNon-substrate0.8528
CYP450 2D6 substrateNon-substrate0.811
CYP450 3A4 substrateSubstrate0.764
CYP450 1A2 substrateNon-inhibitor0.9271
CYP450 2C9 inhibitorInhibitor0.5555
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.5
CYP450 3A4 inhibitorInhibitor0.5
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6447
Ames testNon AMES toxic0.5062
CarcinogenicityNon-carcinogens0.8796
BiodegradationNot ready biodegradable0.9965
Rat acute toxicity2.3038 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8351
hERG inhibition (predictor II)Inhibitor0.6205
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
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03di-0210900000-941cd1e773f20ff3a0d7
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-0000900000-51d5e249f3d4d2777048
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4i-0000900000-0f8a58d153fedcd8c81e
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-01ox-0000900000-35bce86cd4652e679fca
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0apr-0004900000-55fa8e38f6604ea164b1
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-02cu-0035900000-265422d81a1f0e931f36
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4r-1029600000-4df3de4a06cc59f5265a
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-238.9257875
predicted
DarkChem Lite v0.1.0
[M-H]-213.47229
predicted
DeepCCS 1.0 (2019)
[M+H]+239.1317875
predicted
DarkChem Lite v0.1.0
[M+H]+215.86786
predicted
DeepCCS 1.0 (2019)
[M+Na]+238.4341875
predicted
DarkChem Lite v0.1.0
[M+Na]+221.78038
predicted
DeepCCS 1.0 (2019)

Targets

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Details
1. Coagulation factor X
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
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
  1. Spyropoulos AC: Investigational treatments of venous thromboembolism. Expert Opin Investig Drugs. 2007 Apr;16(4):431-40. [Article]
  2. Harenberg J, Wehling M: Current and future prospects for anticoagulant therapy: inhibitors of factor Xa and factor IIa. Semin Thromb Hemost. 2008 Feb;34(1):39-57. doi: 10.1055/s-2008-1066023. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
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
  1. Wang L, Zhang D, Raghavan N, Yao M, Ma L, Frost CE, Maxwell BD, Chen SY, He K, Goosen TC, Humphreys WG, Grossman SJ: In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies. Drug Metab Dispos. 2010 Mar;38(3):448-58. doi: 10.1124/dmd.109.029694. Epub 2009 Nov 25. [Article]
  2. Apixaban FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Cada DJ, Levien TL, Baker DE: Apixaban. Hosp Pharm. 2013 Jun;48(6):494-509. doi: 10.1310/hpj4806-494. [Article]
  2. Apixaban FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Cada DJ, Levien TL, Baker DE: Apixaban. Hosp Pharm. 2013 Jun;48(6):494-509. doi: 10.1310/hpj4806-494. [Article]
  2. Budovich A, Zargarova O, Nogid A: Role of apixaban (eliquis) in the treatment and prevention of thromboembolic disease. P T. 2013 Apr;38(4):206-31. [Article]
  3. Wu Z, Lee D, Joo J, Shin JH, Kang W, Oh S, Lee do Y, Lee SJ, Yea SS, Lee HS, Lee T, Liu KH: CYP2J2 and CYP2C19 are the major enzymes responsible for metabolism of albendazole and fenbendazole in human liver microsomes and recombinant P450 assay systems. Antimicrob Agents Chemother. 2013 Nov;57(11):5448-56. doi: 10.1128/AAC.00843-13. Epub 2013 Aug 19. [Article]
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
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
  1. Authors unspecified: Apixaban. After hip or knee replacement: LMWH remains the standard treatment. Prescrire Int. 2012 Sep;21(130):201-2, 204. [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. Budovich A, Zargarova O, Nogid A: Role of apixaban (eliquis) in the treatment and prevention of thromboembolic disease. P T. 2013 Apr;38(4):206-31. [Article]
  2. Apixaban FDA label [File]
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
  1. Heyes N, Kapoor P, Kerr ID: Polymorphisms of the Multidrug Pump ABCG2: A Systematic Review of Their Effect on Protein Expression, Function, and Drug Pharmacokinetics. Drug Metab Dispos. 2018 Dec;46(12):1886-1899. doi: 10.1124/dmd.118.083030. Epub 2018 Sep 28. [Article]

Drug created at March 19, 2008 16:40 / Updated at February 20, 2024 23:54