argatroban indications/contra

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: -0.57
  • LIPINSKI: 3
  • HAC: 11
  • HDO: 6
  • TPSA: 177.71
  • ALOGS: -3.48
  • ROTB: 8

Drug dosage:

DoseUnitRoute
0.20 g P

Approvals:

DateAgencyCompanyOrphan
June 30, 2000 FDA PFIZER

FDA Adverse Event Reporting System

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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
Activated partial thromboplastin time prolonged 442.77 94.48 73 547 2359 3382880
Coagulation time prolonged 432.79 94.48 59 561 486 3384753
International normalised ratio increased 393.83 94.48 88 532 14527 3370712
Heparin-induced thrombocytopenia 129.30 94.48 25 595 1931 3383308
Haemorrhage 116.54 94.48 36 584 19885 3365354

Pharmacologic Action:

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SourceCodeDescription
ATC B01AE03 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Direct thrombin inhibitors
FDA EPC N0000175980 Anti-coagulant
FDA EPC N0000175518 Direct Thrombin Inhibitor
FDA MoA N0000009963 Thrombin Inhibitors
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

Drug Use (View source of the data)

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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

Acid dissociation constants calculated using MoKa v3.0.0

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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)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
50MG/50ML (1MG/ML) ARGATROBAN IN SODIUM CHLORIDE EAGLE PHARMS N022434 June 29, 2011 RX INJECTABLE IV (INFUSION) 7589106 Sept. 26, 2027 METHOD OF TREATING THROMBOSIS
50MG/50ML (1MG/ML) ARGATROBAN IN SODIUM CHLORIDE EAGLE PHARMS N022434 June 29, 2011 RX INJECTABLE IV (INFUSION) 7687516 Sept. 26, 2027 METHOD OF TREATING AN ARGATROBAN TREATABLE CONDITION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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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
Prothrombin Enzyme Ki 8.02 CHEMBL
Cationic trypsin Enzyme Ki 5.54 CHEMBL

External reference:

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IDSource
DB00278 DRUGBANK_ID
4021239 VUID
N0000148682 NUI
C0048470 UMLSCUI
6385 IUPHAR_LIGAND_ID
D00181 KEGG_DRUG
4021239 VANDF
15202 RXNORM
63931 MMSL
N0000007126 NDFRT
N0000148682 NDFRT
008966 NDDF
116508003 SNOMEDCT_US
398738008 SNOMEDCT_US
15642 MMSL
d04698 MMSL
CHEMBL1166 ChEMBL_ID
92722 PUBCHEM_CID
IY90U61Z3S UNII
141396-28-3 SECONDARY_CAS_RN
C031942 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:94385 CHEBI
15U PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
ARGATROBAN HUMAN PRESCRIPTION DRUG LABEL 1 0007-4407 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 18 sections
ARGATROBAN HUMAN PRESCRIPTION DRUG LABEL 1 0078-0930 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9288 INJECTION 250 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9559 INJECTION 50 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0143-9674 INJECTION 250 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0409-1140 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0703-0020 INJECTION, SOLUTION 1 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0781-3285 SOLUTION 125 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0781-3314 INJECTION 1 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 0781-9314 INJECTION 1 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 42023-182 INJECTION 250 mg INTRAVENOUS ANDA 18 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 42367-202 INJECTION 1 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 42367-203 INJECTION 1 mg INTRAVENOUS NDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 63323-526 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 18 sections
ARGATROBAN HUMAN PRESCRIPTION DRUG LABEL 1 63379-010 INJECTION, SOLUTION 100 mg INTRAVENOUS Approved Drug Product Manufactured Under Contract 1 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 67457-212 INJECTION, SOLUTION 250 mg INTRAVENOUS ANDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 68083-141 SOLUTION 125 mg INTRAVENOUS ANDA 17 sections
Argatroban HUMAN PRESCRIPTION DRUG LABEL 1 70121-1037 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 16 sections