argatroban 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
thromboxane A2-receptor antagonists; antithrombotic agents 239 74863-84-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • argatroban
  • argatroban sodium
  • argatroban hydrate
  • novastan
  • argatroban monohydrate
  • Molecular weight: 508.64
  • Formula: C23H36N6O5S
  • CLOGP: 0.23
  • LIPINSKI: 3
  • HAC: 11
  • HDO: 6
  • TPSA: 177.71
  • ALOGS: -3.48
  • ROTB: 8
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 16 % Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution) 0.17 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.46 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.40 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
June 30, 2000 FDA PFIZER

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
Heparin-induced thrombocytopenia 239.36 49.81 44 953 4538 63483487
Coagulation time prolonged 193.26 49.81 31 966 1417 63486608
Activated partial thromboplastin time prolonged 133.66 49.81 29 968 6864 63481161
International normalised ratio increased 121.71 49.81 40 957 46385 63441640
Oesophageal intramural haematoma 52.06 49.81 7 990 90 63487935

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
Heparin-induced thrombocytopenia 302.07 37.04 65 1405 5530 34949931
Activated partial thromboplastin time prolonged 111.81 37.04 32 1438 8663 34946798
Coagulation time prolonged 110.13 37.04 22 1448 1280 34954181
International normalised ratio increased 85.55 37.04 41 1429 47286 34908175
Coagulopathy 54.34 37.04 23 1447 19766 34935695
Haemorrhage 54.02 37.04 31 1439 51339 34904122
Disseminated intravascular coagulation 52.18 37.04 23 1447 21793 34933668
Thrombosis 44.01 37.04 27 1443 50431 34905030
Subarachnoid haemorrhage 39.09 37.04 16 1454 12619 34942842

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
Heparin-induced thrombocytopenia 526.74 35.66 108 2446 9574 79732260
Activated partial thromboplastin time prolonged 176.44 35.66 48 2506 14180 79727654
Coagulation time prolonged 154.06 35.66 31 2523 2464 79739370
International normalised ratio increased 110.74 35.66 54 2500 84667 79657167
Coagulopathy 65.82 35.66 29 2525 35977 79705857
Thrombosis 65.52 35.66 38 2516 84062 79657772
Haemorrhage 62.69 35.66 38 2516 91080 79650754
Disseminated intravascular coagulation 59.54 35.66 27 2527 35815 79706019
Subarachnoid haemorrhage 59.02 35.66 24 2530 24441 79717393
Cerebral haemorrhage 52.85 35.66 29 2525 57644 79684190
Cerebral infarction 50.40 35.66 26 2528 45650 79696184
Haemorrhagic cerebral infarction 49.00 35.66 11 2543 1468 79740366
Dry gangrene 47.60 35.66 10 2544 979 79740855
Oesophageal intramural haematoma 45.28 35.66 7 2547 118 79741716
Pulmonary embolism 41.17 35.66 38 2516 171616 79570218
Deep vein thrombosis 39.61 35.66 32 2522 120887 79620947
Iliac artery occlusion 38.55 35.66 7 2547 320 79741514
Gangrene 36.89 35.66 13 2541 8951 79732883

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AE03 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Direct thrombin inhibitors
FDA MoA N0000009963 Thrombin Inhibitors
FDA EPC N0000175518 Direct Thrombin Inhibitor
MeSH PA D000925 Anticoagulants
MeSH PA D000991 Antithrombins
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006401 Hematologic Agents
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D011480 Protease Inhibitors
MeSH PA D015842 Serine Proteinase Inhibitors
FDA EPC N0000175980 Anti-coagulant

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

DiseaseRelationSNOMED_IDDOID
Percutaneous coronary intervention indication 415070008
Thrombosis Prevention in Heparin-Induced Thrombocytopenia indication
Thrombosis in Heparin Induced Thrombocytopenia indication
Peptic ulcer contraindication 13200003 DOID:750
Duodenal ulcer disease contraindication 51868009 DOID:1724
Blood coagulation disorder contraindication 64779008 DOID:1247
Procedure on central nervous system contraindication 118679007
Bleeding contraindication 131148009
Disease of liver contraindication 235856003 DOID:409
Lumbar puncture contraindication 277762005
Surgical procedure on eye proper contraindication 373353005
Surgical procedure contraindication 387713003
Gastric ulcer contraindication 397825006 DOID:10808
Hypertensive urgency contraindication 443482000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.3 acidic
pKa2 9.73 acidic
pKa3 9.18 Basic
pKa4 3.93 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
50MG/50ML (1MG/ML) **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** ARGATROBAN IN SODIUM CHLORIDE CIPLA N022434 June 29, 2011 DISCN INJECTABLE INTRAVENOUS 7589106 Sept. 26, 2027 METHOD OF TREATING THROMBOSIS
50MG/50ML (1MG/ML) **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** ARGATROBAN IN SODIUM CHLORIDE CIPLA N022434 June 29, 2011 DISCN INJECTABLE INTRAVENOUS 7687516 Sept. 26, 2027 METHOD OF TREATING AN ARGATROBAN TREATABLE CONDITION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Prothrombin Enzyme INHIBITOR Ki 7.40 WOMBAT-PK CHEMBL
Coagulation factor X Enzyme Ki 4.28 CHEMBL
Tissue-type plasminogen activator Enzyme Ki 4.06 CHEMBL
Cationic trypsin Enzyme Ki 5.54 CHEMBL
Prothrombin Enzyme Ki 8.02 CHEMBL

External reference:

IDSource
4021239 VUID
N0000148682 NUI
D00181 KEGG_DRUG
15202 RXNORM
C0048470 UMLSCUI
CHEBI:94385 CHEBI
CHEMBL1166 ChEMBL_ID
DB00278 DRUGBANK_ID
C031942 MESH_SUPPLEMENTAL_RECORD_UI
6385 IUPHAR_LIGAND_ID
IY90U61Z3S UNII
92722 PUBCHEM_CID
15642 MMSL
63931 MMSL
d04698 MMSL
116508003 SNOMEDCT_US
398738008 SNOMEDCT_US
725736007 SNOMEDCT_US
4021239 VANDF
141396-28-3 SECONDARY_CAS_RN
008966 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ARGATROBAN HUMAN PRESCRIPTION DRUG LABEL 1 0078-0930 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 27 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9288 INJECTION 250 mg INTRAVENOUS NDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9288 INJECTION 250 mg INTRAVENOUS NDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9377 INJECTION 50 mg INTRAVENOUS NDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9377 INJECTION 50 mg INTRAVENOUS NDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9559 INJECTION 50 mg INTRAVENOUS NDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9559 INJECTION 50 mg INTRAVENOUS NDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9674 INJECTION 250 mg INTRAVENOUS NDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9674 INJECTION 250 mg INTRAVENOUS NDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0409-1140 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 26 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0409-1140 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 26 sections
ARGATROBAN HUMAN PRESCRIPTION DRUG LABEL 1 16729-430 INJECTION 1 mg INTRAVENOUS NDA 27 sections
ARGATROBAN HUMAN PRESCRIPTION DRUG LABEL 1 16729-430 INJECTION 1 mg INTRAVENOUS NDA 27 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 25021-414 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 27 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 25021-414 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 27 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 42023-182 INJECTION 250 mg INTRAVENOUS ANDA 29 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 42023-182 INJECTION 250 mg INTRAVENOUS ANDA 29 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 42023-182 INJECTION 250 mg INTRAVENOUS ANDA 29 sections
Argatroban Human Prescription Drug Label 1 55150-241 INJECTION, SOLUTION 50 mg INTRAVENOUS NDA 25 sections
Argatroban Human Prescription Drug Label 1 55150-241 INJECTION, SOLUTION 50 mg INTRAVENOUS NDA 25 sections
Argatroban Human Prescription Drug Label 1 55150-241 INJECTION, SOLUTION 50 mg INTRAVENOUS NDA 25 sections
Argatroban Human Prescription Drug Label 1 63323-526 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 26 sections
ARGATROBAN Human Prescription Drug Label 1 65145-126 INJECTION 50 mg INTRAVENOUS ANDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 65219-429 INJECTION 50 mg INTRAVENOUS ANDA 28 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 67457-212 INJECTION, SOLUTION 250 mg INTRAVENOUS ANDA 26 sections
Argatroban Human Prescription Drug Label 1 68083-141 SOLUTION 125 mg INTRAVENOUS ANDA 26 sections
Argatroban Human Prescription Drug Label 1 68083-568 INJECTION, SOLUTION 50 mg INTRAVENOUS ANDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 70121-1037 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 25 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 70121-1037 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 25 sections