sivelestat Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
elastase inhibitors 2452 127373-66-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sivelestat sodium hydrate
  • elaspol
  • sivelestat sodium
  • sivelestat
inhibitor of neutrophil elastase; structure given in first source
  • Molecular weight: 434.46
  • Formula: C20H22N2O7S
  • CLOGP: 2.77
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 3
  • TPSA: 138.87
  • ALOGS: -4.46
  • ROTB: 8

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
None PMDA

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
Toxic epidermal necrolysis 26.38 20.97 4 9 3140 2354932

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

Pharmacologic Action:

SourceCodeDescription
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011480 Protease Inhibitors
MeSH PA D015842 Serine Proteinase Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acute lung injury indication 315345002

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.84 acidic
pKa2 7.84 acidic
pKa3 13.07 acidic

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
Neutrophil elastase Enzyme Ki 6.70 CHEMBL IUPHAR
Myeloblastin Unclassified IC50 6.47 CHEMBL
Neutrophil elastase Unclassified IC50 6.84 CHEMBL

External reference:

IDSource
D03788 KEGG_DRUG
737RR8Y409 UNII
201677-61-4 SECONDARY_CAS_RN
CHEMBL76688 ChEMBL_ID
7703 INN_ID
CHEBI:32133 CHEBI
C069195 MESH_SUPPLEMENTAL_RECORD_UI
DB12863 DRUGBANK_ID
CHEMBL2107493 ChEMBL_ID
CHEMBL3182314 ChEMBL_ID
107706 PUBCHEM_CID
6441 IUPHAR_LIGAND_ID

Pharmaceutical products:

None