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

Stem definitionDrug idCAS RN
anti-inflammatory agents, ibuprofen derivatives 2546 40828-46-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • suprofen
  • masterfen
  • (+/-)-Suprofen
  • profenol
  • racemic suprofen
  • sutoprofen
  • suprofen RS
An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic.
  • Molecular weight: 260.31
  • Formula: C14H12O3S
  • CLOGP: 2.54
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 54.37
  • ALOGS: -3.79
  • ROTB: 4

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.40 g O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 65.86 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 92 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.04 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.76 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 23, 1988 FDA ALCON

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC M01AE07 MUSCULO-SKELETAL SYSTEM
ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS
ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS
Propionic acid derivatives
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drug
CHEBI has role CHEBI:35481 non-narcotic analgesic
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:49110 peripheral nervous system drug
CHEBI has role CHEBI:88188 drug allergen
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D018501 Antirheumatic Agents
MeSH PA D016861 Cyclooxygenase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Herpes simplex dendritic keratitis contraindication 29943008
Blood coagulation disorder contraindication 64779008 DOID:1247

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.19 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
Prostaglandin G/H synthase 1 Enzyme INHIBITOR IC50 5.96 WOMBAT-PK CHEMBL
Prostaglandin G/H synthase 2 Enzyme INHIBITOR IC50 5.06 WOMBAT-PK CHEMBL
Cytochrome P450 2C9 Enzyme Ki 4.35 WOMBAT-PK

External reference:

IDSource
4018481 VUID
N0000146803 NUI
C0038878 UMLSCUI
D00452 KEGG_DRUG
398627003 SNOMEDCT_US
4018481 VANDF
108849007 SNOMEDCT_US
10255 RXNORM
5537 MMSL
002393 NDDF
988GU2F9PE UNII
3586 INN_ID
CHEBI:9362 CHEBI
CHEMBL956 ChEMBL_ID
DB00870 DRUGBANK_ID
5359 PUBCHEM_CID
D013496 MESH_DESCRIPTOR_UI
7298 IUPHAR_LIGAND_ID

Pharmaceutical products:

None