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

Stem definitionDrug idCAS RN
phenylazosalicylic acid derivatives antibacterial 284 80573-04-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • balsalazide
  • balsalazide disodium
  • balsalazide sodium
a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine
  • Molecular weight: 357.32
  • Formula: C17H15N3O6
  • CLOGP: 3.32
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 4
  • TPSA: 148.65
  • ALOGS: -3.76
  • ROTB: 7

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
6.75 g O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 269.86 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 1 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
July 18, 2000 FDA SALIX PHARMS

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
Colitis ulcerative 83.07 31.75 25 872 17707 46667458
Effusion 42.82 31.75 9 888 1482 46683683

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
Colitis ulcerative 57.07 31.10 18 577 14416 29937467

Pharmacologic Action:

SourceCodeDescription
ATC A07EC04 ALIMENTARY TRACT AND METABOLISM
ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
INTESTINAL ANTIINFLAMMATORY AGENTS
Aminosalicylic acid and similar agents
FDA CS M0000971 Aminosalicylic Acids
FDA EPC N0000175781 Aminosalicylate
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 D018501 Antirheumatic Agents
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drugs
CHEBI has role CHEBI:49201 anti-ulcer agents
CHEBI has role CHEBI:55324 gastrointestinal agents
CHEBI has role CHEBI:50266 prodrugs

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Ulcerative colitis indication 64766004 DOID:8577
Kidney disease contraindication 90708001 DOID:557
Pyloric obstruction contraindication 244815007

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.28 acidic
pKa2 4.08 acidic
pKa3 11.45 acidic
pKa4 12.18 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 WOMBAT-PK CHEMBL
Prostaglandin G/H synthase 2 Enzyme INHIBITOR WOMBAT-PK CHEMBL
Arachidonate 5-lipoxygenase Enzyme INHIBITOR CHEMBL CHEMBL
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor AGONIST CHEMBL CHEMBL

External reference:

IDSource
P80AL8J7ZP UNII
4021231 VUID
N0000148675 NUI
D02715 KEGG_DRUG
150399-21-6 SECONDARY_CAS_RN
4021231 VANDF
4021232 VANDF
C0052940 UMLSCUI
CHEBI:267413 CHEBI
BLQ PDB_CHEM_ID
CHEMBL1201346 ChEMBL_ID
CHEMBL1200760 ChEMBL_ID
DB01014 DRUGBANK_ID
54585 PUBCHEM_CID
5221 INN_ID
C038637 MESH_SUPPLEMENTAL_RECORD_UI
11569 IUPHAR_LIGAND_ID
153718 RXNORM
130137 MMSL
15641 MMSL
d04700 MMSL
007156 NDDF
007157 NDDF
391811002 SNOMEDCT_US
420306005 SNOMEDCT_US
420557005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 0054-0079 CAPSULE 750 mg ORAL ANDA 24 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 42291-157 CAPSULE 750 mg ORAL ANDA 24 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 50268-102 CAPSULE 750 mg ORAL ANDA 24 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 50268-102 CAPSULE 750 mg ORAL ANDA 24 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 54868-6137 CAPSULE 750 mg ORAL ANDA 25 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 60429-952 CAPSULE 750 mg ORAL ANDA 24 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 60505-2575 CAPSULE 750 mg ORAL ANDA 25 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 63629-8301 CAPSULE 750 mg ORAL ANDA 23 sections
Colazal HUMAN PRESCRIPTION DRUG LABEL 1 65649-101 CAPSULE 750 mg ORAL NDA authorized generic 21 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 72789-149 CAPSULE 750 mg ORAL ANDA 24 sections