edoxaban Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
blood coagulation factor XA inhibitors, antithrombotics 4897 480449-70-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • edoxaban tosylate
  • edoxaban
  • edoxaban tosilate
  • edoxaban tosilate hydrate
  • lixiana
  • DU-176b
  • savaysa
An orally active inhibitor of coagulation factor Xa (activated factor X) with anticoagulant activity. Edoxaban is administered as edoxaban tosylate. This agent has an elimination half-life of 9-11 hours and undergoes renal excretion.
  • Molecular weight: 548.06
  • Formula: C24H30ClN7O4S
  • CLOGP: 0.15
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 3
  • TPSA: 136.63
  • ALOGS: -4.68
  • ROTB: 6

Drug dosage:

DoseUnitRoute
60 mg O

Approvals:

DateAgencyCompanyOrphan
June 19, 2015 EMA Daiichi Sankyo Europe GmbH
Jan. 8, 2015 FDA DAIICHI SANKYO
April 22, 2011 PMDA

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Epistaxis 91.66 38.54 28 608 14423 3370800
Cerebrovascular accident 88.18 38.54 34 602 35254 3349969
Haematuria 83.68 38.54 24 612 9928 3375295
Gastrointestinal haemorrhage 73.55 38.54 27 609 24347 3360876
Cerebral infarction 65.19 38.54 19 617 8281 3376942
Ischaemic stroke 59.33 38.54 16 620 5254 3379969
Melaena 58.56 38.54 17 619 7295 3377928
Anaemia 55.65 38.54 28 608 54305 3330918
Off label use 44.29 38.54 24 612 53953 3331270
Haemorrhage 41.87 38.54 17 619 19904 3365319

Pharmacologic Action:

SourceCodeDescription
ATC B01AF03 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Direct factor Xa inhibitors
FDA EPC N0000175637 Factor Xa Inhibitor
MeSH PA D000925 Anticoagulants
MeSH PA D000991 Antithrombins
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D065427 Factor Xa Inhibitors
MeSH PA D006401 Hematologic Agents
MeSH PA D011480 Protease Inhibitors
MeSH PA D015842 Serine Proteinase Inhibitors
CHEBI has role CHEBI:50249 anticoagulant
CHEBI has role CHEBI:50427 platelet aggregation inhibitor

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Pulmonary embolism indication 59282003 DOID:9477
Embolism indication 414086009
Prevention of deep vein thrombosis indication 439993001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.7 acidic
pKa2 12.4 acidic
pKa3 6.8 Basic
pKa4 3.01 Basic
pKa5 2.14 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 15MG BASE SAVAYSA DAIICHI SANKYO INC N206316 Jan. 8, 2015 RX TABLET ORAL Jan. 8, 2020 NEW CHEMICAL ENTITY
EQ 30MG BASE SAVAYSA DAIICHI SANKYO INC N206316 Jan. 8, 2015 RX TABLET ORAL Jan. 8, 2020 NEW CHEMICAL ENTITY
EQ 60MG BASE SAVAYSA DAIICHI SANKYO INC N206316 Jan. 8, 2015 RX TABLET ORAL Jan. 8, 2020 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Coagulation factor X Enzyme INHIBITOR Ki 9.25 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
7575 IUPHAR_LIGAND_ID
D09546 KEGG_DRUG
C3272851 UMLSCUI
32W99UE810 UNII
480449-71-6 SECONDARY_CAS_RN
CHEMBL1269025 ChEMBL_ID
DB09075 DRUGBANK_ID
CHEMBL2105682 ChEMBL_ID
8982 INN_ID
C552171 MESH_SUPPLEMENTAL_RECORD_UI
1599538 RXNORM
015852 NDDF
4034081 VANDF
d08338 MMSL
N0000191384 NDFRT
712778008 SNOMEDCT_US
714687009 SNOMEDCT_US
10280735 PUBCHEM_CID
CHEBI:85973 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SAVAYSA HUMAN PRESCRIPTION DRUG LABEL 1 65597-201 TABLET, FILM COATED 15 mg ORAL NDA 19 sections
SAVAYSA HUMAN PRESCRIPTION DRUG LABEL 1 65597-202 TABLET, FILM COATED 30 mg ORAL NDA 19 sections
SAVAYSA HUMAN PRESCRIPTION DRUG LABEL 1 65597-203 TABLET, FILM COATED 60 mg ORAL NDA 19 sections