tolfenamic acid Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
anti-inflammatory, anthranilic acid derivatives 2698 13710-19-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tolfenamic acid
  • tolfedine
  • tolfine
  • Molecular weight: 261.71
  • Formula: C14H12ClNO2
  • CLOGP: 5.51
  • LIPINSKI: 1
  • HAC: 3
  • HDO: 2
  • TPSA: 49.33
  • ALOGS: -4.22
  • ROTB: 3

Drug dosage:

DoseUnitRoute
0.30 g O
0.30 g R

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 8 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 21.83 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 60 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.16 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.37 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.15 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1976 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC M01AG02 MUSCULO-SKELETAL SYSTEM
ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS
ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS
Fenamates
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
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D018501 Antirheumatic Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D006727 Hormone Antagonists
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D011448 Prostaglandin Antagonists
MeSH PA D018689 Sensory System Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D012702 Serotonin Antagonists

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.43 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
Aldo-keto reductase family 1 member C3 Enzyme Ki 8.10 CHEMBL
Androgen receptor Nuclear hormone receptor IC50 4.33 WOMBAT-PK
Prostaglandin G/H synthase 1 Enzyme IC50 6.24 WOMBAT-PK
Prostaglandin G/H synthase 2 Enzyme IC50 8.30 WOMBAT-PK
Transthyretin Secreted IC50 4.40 CHEMBL

External reference:

IDSource
C0076799 UMLSCUI
D01183 KEGG_DRUG
3G943U18KM UNII
2926 INN_ID
322817007 SNOMEDCT_US
38377 RXNORM
395910008 SNOMEDCT_US
006023 NDDF
CHEBI:32243 CHEBI
CHEMBL121626 ChEMBL_ID
TLF PDB_CHEM_ID
DB09216 DRUGBANK_ID
610479 PUBCHEM_CID
C009500 MESH_SUPPLEMENTAL_RECORD_UI
8769 IUPHAR_LIGAND_ID

Pharmaceutical products:

None