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
Anaemia 390.39 51.67 152 1752 71408 4565680
Haematuria 343.94 51.67 92 1812 12878 4624210
Cerebrovascular accident 322.72 51.67 115 1789 41885 4595203
Gastrointestinal haemorrhage 277.98 51.67 95 1809 30440 4606648
Ischaemic stroke 197.02 51.67 53 1851 7501 4629587
Cerebral infarction 195.72 51.67 57 1847 10775 4626313
Lymphatic fistula 193.07 51.67 23 1881 7 4637081
Femoral hernia incarcerated 192.32 51.67 23 1881 8 4637080
Melaena 186.98 51.67 54 1850 9904 4627184
Pancreatic steatosis 166.32 51.67 23 1881 73 4637015
Epistaxis 166.19 51.67 58 1846 19585 4617503
Wound infection pseudomonas 158.31 51.67 23 1881 113 4636975
Haemorrhage 144.13 51.67 56 1848 25506 4611582
Aortic valve stenosis 141.65 51.67 26 1878 621 4636467
Arterial haemorrhage 139.87 51.67 24 1880 384 4636704
Seroma 130.16 51.67 23 1881 440 4636648
Dyspnoea 128.72 51.67 90 1814 138895 4498193
Haemarthrosis 125.52 51.67 26 1878 1179 4635909
Tachyarrhythmia 118.43 51.67 25 1879 1243 4635845
Cerebral haemorrhage 114.74 51.67 40 1864 13401 4623687
Subdural haematoma 113.55 51.67 33 1871 6153 4630935
Inflammatory marker increased 111.89 51.67 23 1881 1003 4636085
Hepatic cyst 111.58 51.67 23 1881 1017 4636071
Diverticulum intestinal 111.54 51.67 24 1880 1308 4635780
Aortic arteriosclerosis 107.85 51.67 23 1881 1201 4635887
Wound dehiscence 104.07 51.67 23 1881 1420 4635668
Eructation 102.51 51.67 24 1880 1919 4635169
Postoperative wound infection 101.88 51.67 24 1880 1971 4635117
Joint dislocation 100.05 51.67 24 1880 2130 4634958
Faecaloma 99.95 51.67 23 1881 1705 4635383
Fall 99.86 51.67 62 1842 77984 4559104
Pulmonary embolism 99.44 51.67 47 1857 34379 4602709
Aplastic anaemia 98.37 51.67 23 1881 1828 4635260
Dizziness 97.63 51.67 67 1837 99804 4537284
Escherichia infection 96.41 51.67 24 1880 2485 4634603
Mitral valve incompetence 94.68 51.67 27 1877 4701 4632387
Groin pain 94.29 51.67 23 1881 2190 4634898
Tricuspid valve incompetence 91.27 51.67 24 1880 3090 4633998
Osteopenia 89.96 51.67 23 1881 2651 4634437
Left ventricular dysfunction 89.37 51.67 23 1881 2722 4634366
Hiatus hernia 89.29 51.67 24 1880 3360 4633728
General physical health deterioration 85.25 51.67 40 1864 28738 4608350
Cardiogenic shock 82.48 51.67 25 1879 5373 4631715
Cardiac failure 81.04 51.67 38 1866 27250 4609838
Cardiovascular disorder 80.97 51.67 25 1879 5715 4631373
Anuria 80.70 51.67 23 1881 3992 4633096
Syncope 76.65 51.67 39 1865 33356 4603732
Atrial thrombosis 75.71 51.67 17 1887 1127 4635961
Urinary retention 75.20 51.67 27 1877 9820 4627268
Embolic stroke 73.91 51.67 18 1886 1700 4635388
Myelodysplastic syndrome 71.88 51.67 24 1880 7034 4630054
Transient ischaemic attack 70.83 51.67 27 1877 11595 4625493
Dyspepsia 69.02 51.67 29 1875 16025 4621063
Thrombosis 68.44 51.67 30 1874 18374 4618714
Decreased appetite 67.45 51.67 43 1861 56354 4580734
Pulmonary hypertension 67.34 51.67 24 1880 8539 4628549
Abdominal discomfort 64.65 51.67 33 1871 28375 4608713
Impaired healing 63.79 51.67 23 1881 8456 4628632
Acute kidney injury 63.37 51.67 45 1859 70386 4566702
Haematochezia 61.35 51.67 24 1880 11040 4626048
Oedema peripheral 60.32 51.67 36 1868 41936 4595152
Vomiting 59.56 51.67 54 1850 119645 4517443
Rectal haemorrhage 58.89 51.67 24 1880 12272 4624816
Ischaemic cerebral infarction 58.42 51.67 12 1892 520 4636568
Cerebral ischaemia 57.84 51.67 16 1888 2488 4634600
Peripheral swelling 57.81 51.67 30 1874 26662 4610426
Drug interaction 57.51 51.67 41 1863 64467 4572621
Hyponatraemia 57.04 51.67 29 1875 24701 4612387
Hyperkalaemia 56.23 51.67 25 1879 15812 4621276
Atrial fibrillation 56.14 51.67 31 1873 31184 4605904
Pruritus 55.39 51.67 42 1862 72530 4564558
Urinary tract infection 54.85 51.67 34 1870 42356 4594732
Coronary artery disease 52.45 51.67 24 1880 16228 4620860

Pharmacologic Action:

SourceCodeDescription
ATC B01AF03 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Direct factor Xa inhibitors
CHEBI has role CHEBI:50249 anticoagulant
CHEBI has role CHEBI:50427 platelet aggregation inhibitor
FDA EPC N0000175637 Factor Xa Inhibitor
FDA MoA N0000175635 Factor Xa Inhibitors

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
EQ 15MG BASE SAVAYSA DAIICHI SANKYO INC N206316 Jan. 8, 2015 RX TABLET ORAL Aug. 9, 2022 INFORMATION ADDED TO LABELING FROM PROSPECTIVE, RANDOMIZED, OPEN-LABEL, BLIND EVALUATOR (PROBE) STUDY EVALUATING THE EFFICACY AND SAFETY OF LOW MOLECULAR WEIGHT HEPARIN/EDOXABAN VERSUS DALTEPARIN IN VENOUS THROMBOEMBOLISM ASSOCIATED WITH CANCER
EQ 30MG BASE SAVAYSA DAIICHI SANKYO INC N206316 Jan. 8, 2015 RX TABLET ORAL Aug. 9, 2022 INFORMATION ADDED TO LABELING FROM PROSPECTIVE, RANDOMIZED, OPEN-LABEL, BLIND EVALUATOR (PROBE) STUDY EVALUATING THE EFFICACY AND SAFETY OF LOW MOLECULAR WEIGHT HEPARIN/EDOXABAN VERSUS DALTEPARIN IN VENOUS THROMBOEMBOLISM ASSOCIATED WITH CANCER
EQ 60MG BASE SAVAYSA DAIICHI SANKYO INC N206316 Jan. 8, 2015 RX TABLET ORAL Aug. 9, 2022 INFORMATION ADDED TO LABELING FROM PROSPECTIVE, RANDOMIZED, OPEN-LABEL, BLIND EVALUATOR (PROBE) STUDY EVALUATING THE EFFICACY AND SAFETY OF LOW MOLECULAR WEIGHT HEPARIN/EDOXABAN VERSUS DALTEPARIN IN VENOUS THROMBOEMBOLISM ASSOCIATED WITH CANCER

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SAVAYSA HUMAN PRESCRIPTION DRUG LABEL 1 65597-201 TABLET, FILM COATED 15 mg ORAL NDA 20 sections
SAVAYSA HUMAN PRESCRIPTION DRUG LABEL 1 65597-202 TABLET, FILM COATED 30 mg ORAL NDA 20 sections
SAVAYSA HUMAN PRESCRIPTION DRUG LABEL 1 65597-203 TABLET, FILM COATED 60 mg ORAL NDA 20 sections