tioconazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
systemic antifungal agents, miconazole derivatives 2675 65899-73-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • UK-20,349
  • UK-20349
  • tioconazole
  • Molecular weight: 387.70
  • Formula: C16H13Cl3N2OS
  • CLOGP: 4.79
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 27.05
  • ALOGS: -4.37
  • ROTB: 6

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.30 g V

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.492 Moderate 0.78
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.030 Moderate 0.78
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 44.259 10^-6 cm/s Moderate 0.78
dh-clint Dog hepatocyte intrinsic clearance 73.451 uL/min/10^6 cells Moderate 0.78
dppb Dog plasma protein binding (% unbound) 0.370 % Moderate 0.78
fcs-ppb Fetal calf serum protein binding (% unbound) 1.170 % Moderate 0.78
herg hERG pIC50 5.812 pIC50 Moderate 0.78
hh-clint Human hepatocyte intrinsic clearance 88.920 uL/min/10^6 cells Moderate 0.78
hlm-clint Human liver microsomal intrinsic clearance 234.423 uL/min/mg protein Moderate 0.78
hppb Human plasma protein binding (% unbound) 0.470 % Moderate 0.78
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIK3CG,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK 42
kinase-selectivity-class AKT3,AXL,BRAF,EIF2AK3,GRK2,PDK4,PIK3CB 7
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.607 Moderate 0.78
mh-clint Mouse hepatocyte intrinsic clearance 138.676 Moderate 0.78
mppb Mouse plasma protein binding (% unbound) 0.440 Moderate 0.78
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.941 Moderate 0.78
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 1.850 % Moderate 0.78
rh-clint Rat hepatocyte intrinsic clearance 190.546 uL/min/10^6 cells Moderate 0.78
rh-fuinc Rat hepatocyte fraction unbound in incubation 6.900 % Moderate 0.78
rppb Rat plasma protein binding (% unbound) 0.390 % Moderate 0.78
solubility-dd Solubility at pH 7.4 in DMSO 95.940 uM Moderate 0.78

Approvals:

DateAgencyCompanyOrphan
Feb. 18, 1983 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC D01AC07 DERMATOLOGICALS
ANTIFUNGALS FOR DERMATOLOGICAL USE
ANTIFUNGALS FOR TOPICAL USE
Imidazole and triazole derivatives
ATC G01AF08 GENITO URINARY SYSTEM AND SEX HORMONES
GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS
ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS
Imidazole derivatives
FDA CS M0002083 Azoles
FDA EPC N0000175487 Azole Antifungal
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000935 Antifungal Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006727 Hormone Antagonists
MeSH PA D058888 14-alpha Demethylase Inhibitors
MeSH PA D065088 Steroid Synthesis Inhibitors
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:77884 EC 1.14.13.70 (sterol 14α-demethylase) inhibitor

Related Drugs by ATC class:

D01AC Imidazole and triazole derivatives 20 drugs
G01AF Imidazole derivatives 16 drugs

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

DiseaseRelationSNOMED_IDDOID
Candidal vulvovaginitis indication 72605008 DOID:2272




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.49 Basic

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
Steroid 17-alpha-hydroxylase/17,20 lyase Enzyme Ki 6.30 CHEMBL
7-alpha-hydroxycholest-4-en-3-one 12-alpha-hydroxylase Enzyme INHIBITOR Kd 6.68 IUPHAR
Cysteine protease ATG4A Enzyme IC50 5.89 CHEMBL
Cysteine protease ATG4B Enzyme IC50 5.75 CHEMBL
Lanosterol 14-alpha demethylase Enzyme INHIBITOR CHEMBL CHEMBL

External reference:

IDSource
4020459 VUID
N0000148215 NUI
D00890 KEGG_DRUG
4020459 VANDF
C0076705 UMLSCUI
CHEBI:9604 CHEBI
FJQ PDB_CHEM_ID
CHEMBL1200438 ChEMBL_ID
DB01007 DRUGBANK_ID
C020527 MESH_SUPPLEMENTAL_RECORD_UI
5482 PUBCHEM_CID
13859 IUPHAR_LIGAND_ID
4572 INN_ID
S57Y5X1117 UNII
38298 RXNORM
5586 MMSL
002926 NDDF
332967005 SNOMEDCT_US
395909003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
good sense tioconazole 1 HUMAN OTC DRUG LABEL 1 0113-0426 OINTMENT 6.50 g VAGINAL ANDA 16 sections
Tioconazole 1 HUMAN OTC DRUG LABEL 1 0363-0426 OINTMENT 6.50 g VAGINAL ANDA 16 sections
VAGISTAT HUMAN OTC DRUG LABEL 1 11509-0426 OINTMENT 6.50 g VAGINAL ANDA 16 sections
Up and up tioconazole 1 HUMAN OTC DRUG LABEL 1 11673-426 OINTMENT 6.50 g VAGINAL ANDA 16 sections
signature care tioconazole 1 HUMAN OTC DRUG LABEL 1 21130-060 OINTMENT 6.50 g VAGINAL ANDA 16 sections
TIOCONAZOLE 1 HUMAN OTC DRUG LABEL 1 21130-781 OINTMENT 6.50 g VAGINAL ANDA 16 sections
Topcare Tioconazole 1 HUMAN OTC DRUG LABEL 1 36800-426 OINTMENT 6.50 g VAGINAL ANDA 16 sections
Tioconazole 1 HUMAN OTC DRUG LABEL 1 37808-426 OINTMENT 6.50 g VAGINAL ANDA 16 sections
Equaline Tioconazole 1 HUMAN OTC DRUG LABEL 1 41163-032 OINTMENT 6.50 g VAGINAL ANDA 16 sections
tioconazole 1 HUMAN OTC DRUG LABEL 1 41250-426 OINTMENT 6.50 g VAGINAL ANDA 16 sections
CareOne Tioconazole 1 HUMAN OTC DRUG LABEL 1 41520-426 OINTMENT 6.50 g VAGINAL ANDA 16 sections
Equate tioconazole 1 day HUMAN OTC DRUG LABEL 1 49035-426 OINTMENT 6.50 g VAGINAL ANDA 16 sections
dg health tioconazole 1 HUMAN OTC DRUG LABEL 1 55910-731 OINTMENT 6.50 g VAGINAL ANDA 16 sections
tioconazole 1 HUMAN OTC DRUG LABEL 1 59779-718 OINTMENT 6.50 g VAGINAL ANDA 16 sections
TIOCONAZOLEOintment 6.5% HUMAN OTC DRUG LABEL 1 63094-0426 OINTMENT 65 mg VAGINAL ANDA 12 sections
Tioconazole1 Day HUMAN OTC DRUG LABEL 1 63736-410 OINTMENT 300 mg TOPICAL ANDA 16 sections
MONISTAT TIOCONAZOLE 1 HUMAN OTC DRUG LABEL 1 63736-413 OINTMENT 6.50 g TOPICAL ANDA 15 sections
Leader Tioconazole 1 HUMAN OTC DRUG LABEL 1 70000-0357 OINTMENT 6.50 g VAGINAL ANDA 16 sections
foster and thrive tioconazole HUMAN OTC DRUG LABEL 1 70677-1224 OINTMENT 6.50 g VAGINAL ANDA 16 sections
basic care tioconazole HUMAN OTC DRUG LABEL 1 72288-426 OINTMENT 6.50 g VAGINAL ANDA 16 sections