edoxaban 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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: 1.86
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 3
  • TPSA: 136.63
  • ALOGS: -4.68
  • ROTB: 6
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 1.53 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.19 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.50 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 6.70 hours Lombardo F, Berellini G, Obach RS

Approvals:

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

FDA Adverse Event Reporting System (Female)

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
General physical health deterioration 265.94 23.02 204 7983 142230 50454707
Anaemia 141.20 23.02 188 7999 252268 50344669
Haematochezia 118.19 23.02 76 8111 39806 50557131
Melaena 104.68 23.02 61 8126 26803 50570134
Cardiac failure 95.83 23.02 87 8100 75953 50520984
Labelled drug-drug interaction medication error 88.23 23.02 40 8147 10437 50586500
Lymphatic fistula 87.38 23.02 21 8166 729 50596208
Femoral hernia incarcerated 87.07 23.02 21 8166 740 50596197
Arterial haemorrhage 85.65 23.02 24 8163 1533 50595404
Pancreatic steatosis 82.91 23.02 21 8166 908 50596029
Pallor 80.77 23.02 49 8138 23150 50573787
Product monitoring error 80.12 23.02 26 8161 2738 50594199
Wound infection pseudomonas 76.35 23.02 21 8166 1252 50595685
Atrial fibrillation 74.62 23.02 87 8100 101658 50495279
Arrhythmia 73.94 23.02 53 8134 33079 50563858
Renal impairment 73.44 23.02 75 8112 75586 50521351
Drug ineffective 71.80 23.02 22 8165 819311 49777626
Haematuria 71.40 23.02 47 8140 25566 50571371
Aortic valve stenosis 70.34 23.02 24 8163 2951 50593986
Seroma 68.69 23.02 21 8166 1820 50595117
Haemarthrosis 66.96 23.02 23 8164 2885 50594052
Tachyarrhythmia 66.41 23.02 25 8162 4080 50592857
Hyponatraemia 60.35 23.02 76 8111 96063 50500874
Eructation 56.22 23.02 26 8161 7095 50589842
Faecaloma 53.16 23.02 25 8162 7083 50589854
Wound dehiscence 51.14 23.02 21 8166 4309 50592628
Diverticulum intestinal 51.05 23.02 23 8164 5910 50591027
Hyperkalaemia 50.91 23.02 50 8137 48039 50548898
Hepatic cyst 50.39 23.02 21 8166 4472 50592465
Aortic arteriosclerosis 49.95 23.02 22 8165 5360 50591577
Gastrointestinal haemorrhage 49.26 23.02 60 8127 73261 50523676
Inflammatory marker increased 48.98 23.02 22 8165 5612 50591325
Cerebral infarction 46.90 23.02 34 8153 21570 50575367
Anuria 45.01 23.02 26 8161 11218 50585719
Internal haemorrhage 44.06 23.02 19 8168 4398 50592539
Oedema peripheral 42.93 23.02 85 8102 157876 50439061
Dyspnoea 42.66 23.02 188 7999 547420 50049517
Aplastic anaemia 42.43 23.02 22 8165 7681 50589256
Groin pain 42.22 23.02 23 8164 8868 50588069
Bradycardia 40.50 23.02 51 8136 64375 50532562
Postoperative wound infection 40.46 23.02 22 8165 8453 50588484
Escherichia infection 40.37 23.02 24 8163 10917 50586020
Chorea 36.39 23.02 12 8175 1328 50595609
Cardiovascular disorder 36.16 23.02 22 8165 10432 50586505
Myelodysplastic syndrome 35.57 23.02 25 8162 15107 50581830
Embolic stroke 34.80 23.02 15 8172 3469 50593468
Tricuspid valve incompetence 34.52 23.02 23 8164 12747 50584190
Decreased appetite 34.36 23.02 90 8097 200833 50396104
Syncope 33.65 23.02 60 8127 102942 50493995
Angina pectoris 33.00 23.02 30 8157 26158 50570779
Joint dislocation 32.83 23.02 22 8165 12311 50584626
Cardiogenic shock 32.61 23.02 24 8163 15575 50581362
Tachycardia 32.44 23.02 58 8129 99705 50497232
Left ventricular dysfunction 31.03 23.02 20 8167 10486 50586451
Pulmonary hypertension 30.35 23.02 32 8155 33385 50563552
BRASH syndrome 30.24 23.02 7 8180 206 50596731
Mitral valve incompetence 30.19 23.02 24 8163 17447 50579490
Rhonchi 30.03 23.02 12 8175 2295 50594642
Thrombophlebitis migrans 28.94 23.02 6 8181 104 50596833
Pain 28.62 23.02 31 8156 578872 50018065
Product prescribing error 28.36 23.02 25 8162 20936 50576001
Gastroenteritis clostridial 27.91 23.02 8 8179 554 50596383
Sopor 27.48 23.02 24 8163 19855 50577082
Urinary retention 27.27 23.02 27 8160 26163 50570774
Cerebral haemorrhage 26.54 23.02 27 8160 27025 50569912
Osteopenia 26.50 23.02 22 8165 16996 50579941
Electrolyte imbalance 26.33 23.02 22 8165 17147 50579790
Streptococcal sepsis 26.18 23.02 10 8177 1697 50595240
Hepatic function abnormal 25.68 23.02 29 8158 32652 50564285
Hiatus hernia 25.06 23.02 22 8165 18322 50578615
Oesophageal mucosal tear 24.29 23.02 4 8183 17 50596920
Dysuria 23.61 23.02 26 8161 28478 50568459
Ischaemic stroke 23.56 23.02 20 8167 15928 50581009

FDA Adverse Event Reporting System (Male)

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
General physical health deterioration 107.01 19.93 124 6599 102733 29465071
Pelvic mass 94.64 19.93 19 6704 193 29567611
Haematuria 90.28 19.93 77 6646 44062 29523742
Cardiac failure 83.05 19.93 96 6627 79191 29488613
Cerebral infarction 71.81 19.93 53 6670 24622 29543182
Prostate cancer recurrent 71.56 19.93 20 6703 895 29566909
Blood urea abnormal 70.68 19.93 19 6704 734 29567070
Malignant transformation 68.76 19.93 19 6704 815 29566989
Blood electrolytes abnormal 67.39 19.93 19 6704 878 29566926
Melaena 64.96 19.93 55 6668 31121 29536683
Anaemia 64.28 19.93 141 6582 200810 29366994
Renal impairment 63.49 19.93 85 6638 81248 29486556
Respiratory tract haemorrhage 57.21 19.93 17 6706 947 29566857
Atrial fibrillation 49.30 19.93 87 6636 105559 29462245
Oedema peripheral 46.67 19.93 84 6639 103473 29464331
Haematochezia 45.90 19.93 49 6674 36934 29530870
Dyspnoea 44.89 19.93 169 6554 326563 29241241
Embolic stroke 41.57 19.93 19 6704 3587 29564217
Drug ineffective 35.95 19.93 19 6704 363151 29204653
Hydronephrosis 35.37 19.93 23 6700 8707 29559097
Labelled drug-drug interaction medication error 35.08 19.93 26 6697 12133 29555671
Interstitial lung disease 34.23 19.93 53 6670 57665 29510139
Epistaxis 29.99 19.93 47 6676 51657 29516147
Pallor 29.93 19.93 30 6693 20994 29546810
Procedural failure 29.36 19.93 6 6717 67 29567737
Pseudarthrosis 28.81 19.93 6 6717 74 29567730
Cerebral haemorrhage 26.24 19.93 34 6689 31392 29536412
Haemorrhage 26.17 19.93 41 6682 45031 29522773
Tracheal pain 25.45 19.93 5 6718 45 29567759
Pulmonary alveolar haemorrhage 23.88 19.93 16 6707 6364 29561440
Skin irritation 23.78 19.93 14 6709 4447 29563357
Duodenal ulcer haemorrhage 23.73 19.93 14 6709 4465 29563339
Haematoma 22.39 19.93 27 6696 23185 29544619
Subdural haematoma 22.37 19.93 24 6699 18169 29549635
Stress urinary incontinence 21.94 19.93 5 6718 96 29567708
Haemothorax 21.57 19.93 12 6711 3424 29564380
Haemoptysis 20.88 19.93 30 6693 30520 29537284

FDA Adverse Event Reporting System (Geriatric)

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
General physical health deterioration 346.11 17.31 319 14260 204106 64280047
Anaemia 185.49 17.31 317 14262 378363 64105790
Cardiac failure 161.20 17.31 173 14406 132200 64351953
Haematochezia 151.19 17.31 123 14456 66250 64417903
Melaena 147.42 17.31 111 14468 53437 64430716
Haematuria 143.95 17.31 115 14464 60356 64423797
Renal impairment 139.54 17.31 162 14417 134855 64349298
Cerebral infarction 124.00 17.31 90 14489 40954 64443199
Atrial fibrillation 110.70 17.31 163 14416 170926 64313227
Labelled drug-drug interaction medication error 109.58 17.31 66 14513 21996 64462157
Pallor 97.07 17.31 76 14503 38705 64445448
Drug ineffective 89.98 17.31 39 14540 840208 63643945
Oedema peripheral 87.09 17.31 164 14415 210153 64274000
Product monitoring error 86.75 17.31 36 14543 5418 64478735
Lymphatic fistula 80.17 17.31 21 14558 737 64483416
Femoral hernia incarcerated 80.09 17.31 21 14558 740 64483413
Dyspnoea 80.00 17.31 347 14232 718327 63765826
Arterial haemorrhage 77.04 17.31 26 14553 2205 64481948
Prostate cancer recurrent 75.73 17.31 20 14559 725 64483428
Pancreatic steatosis 74.24 17.31 21 14558 987 64483166
Embolic stroke 73.28 17.31 34 14545 6677 64477476
Wound infection pseudomonas 65.55 17.31 21 14558 1512 64482641
Pelvic mass 63.65 17.31 19 14560 1081 64483072
Malignant transformation 62.96 17.31 19 14560 1122 64483031
Arrhythmia 62.21 17.31 68 14511 52876 64431277
Blood urea abnormal 61.89 17.31 19 14560 1189 64482964
Seroma 59.53 17.31 21 14558 2033 64482120
Aortic valve stenosis 58.87 17.31 26 14553 4554 64479599
Tachyarrhythmia 58.04 17.31 28 14551 5998 64478155
Blood electrolytes abnormal 54.54 17.31 19 14560 1772 64482381
Gastrointestinal haemorrhage 53.23 17.31 102 14477 132210 64351943
Cerebral haemorrhage 52.16 17.31 61 14518 51029 64433124
Respiratory tract haemorrhage 50.08 17.31 17 14562 1467 64482686
Haemarthrosis 49.46 17.31 24 14555 5205 64478948
Internal haemorrhage 48.90 17.31 27 14552 7640 64476513
Interstitial lung disease 47.76 17.31 82 14497 97650 64386503
Angina pectoris 46.31 17.31 54 14525 45027 64439126
Diverticulum intestinal 44.24 17.31 25 14554 7395 64476758
Hepatic cyst 43.48 17.31 22 14557 5218 64478935
Dysuria 42.57 17.31 50 14529 42007 64442146
Subdural haematoma 41.91 17.31 41 14538 28013 64456140
Eructation 41.80 17.31 26 14553 9165 64474988
Aortic arteriosclerosis 41.39 17.31 24 14555 7452 64476701
Tachycardia 40.24 17.31 98 14481 149481 64334672
Thrombophlebitis migrans 39.84 17.31 10 14569 295 64483858
Wound dehiscence 38.32 17.31 21 14558 5853 64478300
Bradycardia 36.77 17.31 82 14497 118137 64366016
Groin pain 36.71 17.31 26 14553 11367 64472786
Faecaloma 35.58 17.31 24 14555 9704 64474449
Gastric haemorrhage 34.97 17.31 27 14552 13454 64470699
Decreased appetite 34.29 17.31 140 14439 281149 64203004
Postoperative wound infection 34.26 17.31 24 14555 10312 64473841
Inflammatory marker increased 33.69 17.31 22 14557 8429 64475724
Syncope 31.97 17.31 93 14486 157542 64326611
Ischaemic stroke 31.87 17.31 36 14543 28999 64455154
Drug intolerance 31.59 17.31 3 14576 187989 64296164
Chorea 31.12 17.31 13 14566 1987 64482166
Cardiovascular disorder 31.09 17.31 27 14552 15854 64468299
Pulmonary alveolar haemorrhage 30.86 17.31 22 14557 9716 64474437
Hydronephrosis 29.66 17.31 25 14554 14100 64470053
Pain 29.45 17.31 50 14529 553461 63930692
Drug hypersensitivity 28.74 17.31 9 14570 237806 64246347
Hyponatraemia 28.63 17.31 86 14493 148253 64335900
Electrocardiogram abnormal 28.59 17.31 24 14555 13457 64470696
Procedural failure 28.41 17.31 6 14573 80 64484073
Product dose omission issue 28.20 17.31 5 14574 194742 64289411
Aplastic anaemia 27.92 17.31 24 14555 13896 64470257
Product prescribing error 27.80 17.31 37 14542 35232 64448921
Colon cancer 27.69 17.31 23 14556 12716 64471437
Joint dislocation 27.66 17.31 22 14557 11443 64472710
Thirst 27.60 17.31 24 14555 14113 64470040
Tricuspid valve incompetence 27.57 17.31 26 14553 16977 64467176
Toxicity to various agents 27.53 17.31 25 14554 363488 64120665
Anuria 26.99 17.31 27 14552 18937 64465216
Haemorrhage subcutaneous 26.83 17.31 15 14564 4346 64479807
Upper gastrointestinal haemorrhage 26.31 17.31 36 14543 35184 64448969
Escherichia infection 26.15 17.31 24 14555 15144 64469009
Epistaxis 26.06 17.31 64 14515 98067 64386086
Product used for unknown indication 26.03 17.31 9 14570 821 64483332
Hyperkalaemia 25.85 17.31 65 14514 101064 64383089
Haematoma 25.52 17.31 41 14538 46209 64437944
Tracheal pain 25.47 17.31 5 14574 45 64484108
Nasopharyngitis 24.45 17.31 7 14572 196066 64288087
Rheumatoid arthritis 24.26 17.31 4 14575 164290 64319863
Duodenal ulcer haemorrhage 24.08 17.31 16 14563 6309 64477844
BRASH syndrome 23.95 17.31 7 14572 370 64483783
Hepatic function abnormal 23.91 17.31 48 14531 64265 64419888
Left ventricular dysfunction 23.88 17.31 24 14555 16930 64467223
Haemorrhage 23.50 17.31 54 14525 79297 64404856
Oesophageal mucosal tear 23.35 17.31 4 14575 15 64484138
Sinusitis 22.82 17.31 3 14576 145925 64338228
Haemothorax 22.78 17.31 14 14565 4828 64479325
Putamen haemorrhage 22.71 17.31 7 14572 444 64483709
Haemoptysis 22.44 17.31 40 14539 49008 64435145
Urinary retention 22.35 17.31 40 14539 49161 64434992
Electrolyte imbalance 22.26 17.31 28 14551 25215 64458938
Anxiety 22.21 17.31 9 14570 202640 64281513
Mitral valve incompetence 22.00 17.31 28 14551 25510 64458643
Osteopenia 21.89 17.31 22 14557 15518 64468635
Rhonchi 21.55 17.31 12 14567 3451 64480702
Joint swelling 21.37 17.31 11 14568 215371 64268782
Cardiac failure chronic 21.07 17.31 17 14562 9024 64475129
Pneumonia bacterial 20.65 17.31 21 14558 15014 64469139
Alopecia 20.50 17.31 6 14573 165684 64318469
Depression 20.31 17.31 8 14571 183283 64300870
Feeling abnormal 20.30 17.31 3 14576 133599 64350554
Sopor 20.19 17.31 29 14550 29632 64454521
Thalamus haemorrhage 20.19 17.31 9 14570 1610 64482543
Pulmonary hypertension 19.50 17.31 35 14544 43104 64441049
Sacroiliac joint dysfunction 19.49 17.31 4 14575 46 64484107
Gastroenteritis clostridial 18.93 17.31 7 14572 775 64483378
Skin irritation 18.74 17.31 16 14563 9178 64474975
Endocarditis noninfective 18.53 17.31 5 14574 197 64483956
Infusion related reaction 18.52 17.31 7 14572 164460 64319693
Arthralgia 18.36 17.31 46 14533 442214 64041939
Drug abuse 17.90 17.31 4 14575 132370 64351783
Small intestinal haemorrhage 17.82 17.31 11 14568 3822 64480331
Swelling 17.74 17.31 7 14572 160211 64323942
Ventricular arrhythmia 17.40 17.31 14 14565 7401 64476752
Hiatus hernia 17.38 17.31 22 14557 19935 64464218
Myelodysplastic syndrome 17.38 17.31 26 14553 27553 64456600

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AF03 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Direct factor Xa inhibitors
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
FDA MoA N0000175635 Factor Xa Inhibitors
FDA EPC N0000175637 Factor Xa Inhibitor
CHEBI has role CHEBI:50249 anticoagulants
CHEBI has role CHEBI:50427 platelet aggregation inhibitors
CHEBI has role CHEBI:68581 factor Xa inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Pulmonary embolism indication 59282003 DOID:9477
Embolism indication 414086009
Ischemic stroke indication 422504002
Prevention of deep vein thrombosis indication 439993001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 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
480449-71-6 SECONDARY_CAS_RN
4034081 VANDF
CHEBI:85974 CHEBI
CHEMBL1269025 ChEMBL_ID
CHEMBL2105682 ChEMBL_ID
C552171 MESH_SUPPLEMENTAL_RECORD_UI
7575 IUPHAR_LIGAND_ID
8982 INN_ID
DB09075 DRUGBANK_ID
NDU3J18APO UNII
10280735 PUBCHEM_CID
1599538 RXNORM
232451 MMSL
30841 MMSL
30865 MMSL
d08338 MMSL
015852 NDDF
015853 NDDF
1162278009 SNOMEDCT_US
712778008 SNOMEDCT_US
714687009 SNOMEDCT_US
C2975435 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SAVAYSA HUMAN PRESCRIPTION DRUG LABEL 1 65597-201 TABLET, FILM COATED 15 mg ORAL NDA 34 sections
SAVAYSA HUMAN PRESCRIPTION DRUG LABEL 1 65597-202 TABLET, FILM COATED 30 mg ORAL NDA 34 sections
SAVAYSA HUMAN PRESCRIPTION DRUG LABEL 1 65597-203 TABLET, FILM COATED 60 mg ORAL NDA 34 sections