balsalazide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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: 3.31
  • 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 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 1 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility) 87 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKC,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K1,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM1,PIM2,PLK1,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK10,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 77
kinase-selectivity-class ACVR2A,ACVR2B,AURKA,AURKB,AURKC,AXL,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK16,CDK4,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FGFR1,GRK2,GRK3,IKBKB,JAK2,MAP2K3,MAP2K6,MAP3K14,MAP3K2,MAP3K7,MAPK1,MAPK12,MAPK7,MAPK8,MARK4,MTOR,PIK3CB,PIK3CD,PIM3,PLK1,PLK2,PLK3,PLK4,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,UHMK1,ULK1,ULK2 54
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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
Effusion 56.05 34.11 10 591 2052 90625794
Colitis ulcerative 55.06 34.11 19 582 60247 90567599
Congestive cardiomyopathy 48.75 34.11 11 590 7343 90620503
Left ventricular dysfunction 36.51 34.11 10 591 14659 90613187

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
Lactobacillus infection 66.80 36.72 10 522 364 42620439
Subacute endocarditis 63.97 36.72 8 524 72 42620731
Bacterial translocation 61.23 36.72 10 522 643 42620160
Gastrointestinal bacterial infection 46.73 36.72 8 524 683 42620120

FDA Adverse Event Reporting System (Geriatric)

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 54.49 30.28 22 992 77341 110510944
Subacute endocarditis 51.19 30.28 7 1007 181 110588104
Effusion 49.88 30.28 10 1004 2747 110585538
Lactobacillus infection 44.07 30.28 7 1007 513 110587772
Bacterial translocation 43.02 30.28 8 1006 1484 110586801
Congestive cardiomyopathy 37.98 30.28 11 1003 14208 110574077
Gastrointestinal bacterial infection 37.06 30.28 7 1007 1411 110586874
Left ventricular dysfunction 32.54 30.28 11 1003 23482 110564803

FDA Adverse Event Reporting System (Pediatric)

None

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
MeSH PA D000700 Analgesics
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018501 Antirheumatic Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D018712 Analgesics, Non-Narcotic
FDA EPC N0000175781 Aminosalicylate
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drug
CHEBI has role CHEBI:49201 anti-ulcer drug
CHEBI has role CHEBI:55324 gastrointestinal drug
CHEBI has role CHEBI:50266 prodrug

Related Drugs by ATC class:

A07EC Aminosalicylic acid and similar agents 3 drugs
mesalazineolsalazinesulfasalazine

Drug Use | Suggest Off label Use Form| |View source of the data|

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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1.1GM **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** GIAZO VALEANT PHARMS INTL N022205 Feb. 3, 2012 DISCN TABLET ORAL 9192616 Aug. 2, 2026 TREATMENT OF MILDLY TO MODERATELY ACTIVE ULCERATIVE COLITIS IN MALE PATIENTS
750MG COLAZAL VALEANT PHARMS INTL N020610 July 18, 2000 RX CAPSULE ORAL 7452872 Aug. 24, 2026 TREATMENT OF ULCERATIVE COLITIS
750MG COLAZAL VALEANT PHARMS INTL N020610 July 18, 2000 RX CAPSULE ORAL 7625884 Aug. 24, 2026 TREATMENT OF ULCERATIVE COLITIS
1.1GM **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** GIAZO VALEANT PHARMS INTL N022205 Feb. 3, 2012 DISCN TABLET ORAL 7452872 Aug. 24, 2026 TREATMENT OF MILDLY TO MODERATELY ACTIVE ULCERATIVE COLITIS IN MALE PATIENTS
1.1GM **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** GIAZO VALEANT PHARMS INTL N022205 Feb. 3, 2012 DISCN TABLET ORAL 7625884 Aug. 24, 2026 TREATMENT OF MILDLY TO MODERATELY ACTIVE ULCERATIVE COLITIS IN MALE PATIENTS
1.1GM **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** GIAZO VALEANT PHARMS INTL N022205 Feb. 3, 2012 DISCN TABLET ORAL 8497256 June 23, 2031 TREATMENT OF MILDLY TO MODERATELY ACTIVE ULCERATIVE COLITIS IN MALE PATIENTS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Prostaglandin G/H synthase 2 Enzyme INHIBITOR WOMBAT-PK CHEMBL
Prostaglandin G/H synthase 1 Enzyme INHIBITOR WOMBAT-PK CHEMBL
Arachidonate 5-lipoxygenase Enzyme INHIBITOR CHEMBL CHEMBL
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor AGONIST CHEMBL CHEMBL
NAD-dependent protein deacylase sirtuin-5, mitochondrial Enzyme IC50 5.41 CHEMBL
Nucleoside diphosphate kinase, mitochondrial Enzyme EC50 4.34 CHEMBL
Glutaryl-CoA dehydrogenase, mitochondrial Enzyme EC50 4.76 CHEMBL

External reference:

IDSource
4021231 VUID
N0000148675 NUI
D02715 KEGG_DRUG
150399-21-6 SECONDARY_CAS_RN
153718 RXNORM
C0052940 UMLSCUI
CHEBI:267413 CHEBI
BLQ PDB_CHEM_ID
CHEMBL1201346 ChEMBL_ID
CHEMBL1200760 ChEMBL_ID
DB01014 DRUGBANK_ID
C038637 MESH_SUPPLEMENTAL_RECORD_UI
54585 PUBCHEM_CID
11569 IUPHAR_LIGAND_ID
5221 INN_ID
P80AL8J7ZP UNII
130137 MMSL
15641 MMSL
37855 MMSL
37856 MMSL
5056 MMSL
d01031 MMSL
d04700 MMSL
C0127615 UMLSCUI
DB00244 DRUGBANK_ID
4075 PUBCHEM_CID
4019494 VANDF
4021231 VANDF
4021232 VANDF
001600 NDDF
007156 NDDF
007157 NDDF
387501005 SNOMEDCT_US
391811002 SNOMEDCT_US
420306005 SNOMEDCT_US
420557005 SNOMEDCT_US
86977007 SNOMEDCT_US
CHEBI:6775 CHEBI
P80AL8J7ZP INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 0054-0079 CAPSULE 750 mg ORAL ANDA 23 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 50268-102 CAPSULE 750 mg ORAL ANDA 24 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 51407-820 CAPSULE 750 mg ORAL ANDA 23 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 54868-6137 CAPSULE 750 mg ORAL ANDA 25 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 60505-2575 CAPSULE 750 mg ORAL ANDA 24 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 64380-209 TABLET 1.10 g ORAL ANDA 21 sections
balsalazide disodium HUMAN PRESCRIPTION DRUG LABEL 1 70710-1626 CAPSULE 750 mg ORAL ANDA 24 sections
balsalazide disodium HUMAN PRESCRIPTION DRUG LABEL 1 70771-1841 CAPSULE 750 mg ORAL ANDA 24 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 72162-2095 CAPSULE 750 mg ORAL ANDA 23 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 72789-149 CAPSULE 750 mg ORAL ANDA 23 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 72789-149 CAPSULE 750 mg ORAL ANDA 23 sections
balsalazide disodium HUMAN PRESCRIPTION DRUG LABEL 1 80005-126 CAPSULE 750 mg ORAL ANDA 24 sections