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

Stem definitionDrug idCAS RN
phenylazosalicylic acid derivatives antibacterial 1988 6054-98-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • olsalazine
  • olsalazine sodium
  • CJ 91B
  • dipentum
  • azodisalicylate
cpd with 2 salicylate molecules linked together by an azo bond
  • Molecular weight: 302.24
  • Formula: C14H10N2O6
  • CLOGP: 4.57
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 4
  • TPSA: 139.78
  • ALOGS: -3.59
  • ROTB: 4

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
1 g O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 55.25 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 2 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.07 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.20 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) 0.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 31, 1990 FDA MEDA PHARMS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC A07EC03 ALIMENTARY TRACT AND METABOLISM
ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
INTESTINAL ANTIINFLAMMATORY AGENTS
Aminosalicylic acid and similar agents
FDA EPC N0000175781 Aminosalicylate
FDA Chemical/Ingredient N0000005760 Aminosalicylic Acids
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drug
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D018501 Antirheumatic Agents
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Ulcerative colitis in remission indication 697969008
Crohn's disease off-label use 34000006
Ulcerative colitis off-label use 64766004 DOID:8577
Allergic rhinitis contraindication 61582004
Diarrhea contraindication 62315008
Kidney disease contraindication 90708001 DOID:557
Asthma contraindication 195967001 DOID:2841
Disease of liver contraindication 235856003 DOID:409

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.98 acidic
pKa2 2.58 acidic
pKa3 11.15 acidic
pKa4 11.76 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
Arachidonate 5-lipoxygenase Enzyme INHIBITOR CHEMBL CHEMBL
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor AGONIST CHEMBL CHEMBL
Cyclooxygenase Enzyme INHIBITOR CHEMBL CHEMBL

External reference:

IDSource
4019863 VUID
N0000147949 NUI
C0069454 UMLSCUI
D00727 KEGG_DRUG
108673002 SNOMEDCT_US
4019863 VANDF
d01032 MMSL
32385 RXNORM
386890003 SNOMEDCT_US
004656 NDDF
CHEBI:7770 CHEBI
CHEMBL425 ChEMBL_ID
ULS5I8J03O UNII
5607 INN_ID
15722-48-2 SECONDARY_CAS_RN
DB01250 DRUGBANK_ID
22419 PUBCHEM_CID
CHEMBL1201013 ChEMBL_ID
C032587 MESH_SUPPLEMENTAL_RECORD_UI
DB00244 DRUGBANK_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Dipentum HUMAN PRESCRIPTION DRUG LABEL 1 0037-6860 CAPSULE, GELATIN COATED 250 mg ORAL NDA 13 sections
Dipentum HUMAN PRESCRIPTION DRUG LABEL 1 68151-0312 CAPSULE, GELATIN COATED 250 mg ORAL NDA 13 sections
Dipentum HUMAN PRESCRIPTION DRUG LABEL 1 68151-3120 CAPSULE, GELATIN COATED 250 mg ORAL NDA 14 sections