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

Stem definitionDrug idCAS RN
proteolytic enzyme inhibitors 1867 81525-10-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nafamostat mesilate
  • nafamostat mesylate
  • FUT-175
  • nafamostat
  • nafamstat
  • nafamostat dihydrochloride
  • nafamostat hydrochloride
  • nafamostat HCl
  • ronastat
inhibitor of trypsin, plasmin, pancreatic kallikrein, plasma kallikrein & thrombin; strongly inhibits esterolytic activities of C1r & C1 esterase complement-mediated hemolysis; antineoplastic; RN given refers to parent cpd
  • Molecular weight: 347.38
  • Formula: C19H17N5O2
  • CLOGP: 2.30
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 5
  • TPSA: 138.07
  • ALOGS: -4.01
  • ROTB: 5

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 5.71 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 81.96 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.84 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
None PMDA

FDA Adverse Event Reporting System (Female)

None

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
Off label use 69.52 50.28 36 181 300764 29273546

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
Off label use 70.48 47.27 47 405 632759 63865521
Disseminated intravascular coagulation 48.35 47.27 15 437 32333 64465947

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D000925 Anticoagulants
MeSH PA D018501 Antirheumatic Agents
MeSH PA D051056 Complement Inactivating Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006401 Hematologic Agents
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D011480 Protease Inhibitors
MeSH PA D018689 Sensory System Agents
MeSH PA D015842 Serine Proteinase Inhibitors
MeSH PA D014361 Trypsin Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Cystic fibrosis indication 190905008 DOID:1485




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.81 Basic
pKa2 10.12 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Trypsin-1 Enzyme INHIBITOR IC50 7.77 CHEMBL IUPHAR
Tryptase alpha/beta-1 Enzyme INHIBITOR IC50 10 IUPHAR IUPHAR
Complement C1r subcomponent Enzyme INHIBITOR IC50 6 CHEMBL IUPHAR
Coagulation factor X Enzyme IC50 4.68 CHEMBL
Suppressor of tumorigenicity 14 protein Enzyme Ki 10.70 CHEMBL
Complement C1s subcomponent Enzyme IC50 6.85 CHEMBL
Acid-sensing ion channel 2 Ion channel BLOCKER IC50 4.20 IUPHAR
Acid-sensing ion channel 1 Ion channel BLOCKER IC50 4.90 IUPHAR
Acid-sensing ion channel 3 Ion channel BLOCKER IC50 5.60 IUPHAR
Serine protease hepsin Enzyme Ki 9.28 CHEMBL
Hepatocyte growth factor activator Enzyme Ki 7.60 CHEMBL
Transmembrane protease serine 2 Enzyme INHIBITOR IC50 7 IUPHAR
Plasminogen Enzyme IC50 6.62 CHEMBL
Coagulation factor XII Enzyme Ki 6.98 CHEMBL
Prothrombin Enzyme IC50 6.54 CHEMBL
Kallikrein-1 Enzyme IC50 6.19 CHEMBL
Cationic trypsin Enzyme IC50 7.77 CHEMBL

External reference:

IDSource
D01670 KEGG_DRUG
82956-11-4 SECONDARY_CAS_RN
C0207683 UMLSCUI
CHEBI:31890 CHEBI
CHEMBL273264 ChEMBL_ID
CHEMBL3989553 ChEMBL_ID
CHEMBL1091841 ChEMBL_ID
DB12598 DRUGBANK_ID
C032855 MESH_SUPPLEMENTAL_RECORD_UI
4413 PUBCHEM_CID
4262 IUPHAR_LIGAND_ID
5682 INN_ID
Y25LQ0H97D UNII

Pharmaceutical products:

None