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sulconazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| systemic antifungal agents, miconazole derivatives | 2495 | 61318-90-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.921 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.807 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 7.079 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 40.179 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.140 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.250 | % | High | 1 |
| herg | hERG pIC50 | 5.671 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 42.756 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 208.930 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.370 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK | 50 | |||
| kinase-selectivity-class | AKT2,AKT3,AXL,BRAF,EIF2AK3,GRK2,PDK4 | 7 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.865 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 64.121 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.240 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.845 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.580 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 90.365 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 1.580 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.180 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 12.162 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 30, 1985 | FDA | RANBAXY |
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:
| Source | Code | Description |
|---|---|---|
| ATC | D01AC09 | DERMATOLOGICALS ANTIFUNGALS FOR DERMATOLOGICAL USE ANTIFUNGALS FOR TOPICAL USE Imidazole and triazole derivatives |
| FDA CS | M0002083 | Azoles |
| FDA EPC | N0000175487 | Azole Antifungal |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000935 | Antifungal Agents |
| CHEBI has role | CHEBI:35718 | antifungal agent |
Related Drugs by ATC class:
D01AC Imidazole and triazole derivatives 20 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Tinea pedis | indication | 6020002 | DOID:12403 |
| Pityriasis versicolor | indication | 56454009 | DOID:9060 |
| Tinea corporis | indication | 84849002 | |
| Tinea cruris | indication | 399029005 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.02 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Enzyme | IC50 | 7.16 | DRUG MATRIX | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 7.13 | DRUG MATRIX | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.70 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 5.95 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 5.72 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 5.84 | DRUG MATRIX | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 5.79 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 5.98 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 6.05 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 6.14 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.26 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 5.73 | DRUG MATRIX | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 6.14 | DRUG MATRIX | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 5.86 | DRUG MATRIX | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 6.10 | DRUG MATRIX | |||||
| Adenosine receptor A3 | GPCR | Ki | 5.83 | DRUG MATRIX | |||||
| Cytochrome P450 2C9 | Enzyme | IC50 | 6.70 | DRUG MATRIX | |||||
| Cytochrome P450 1A2 | Enzyme | IC50 | 6.22 | DRUG MATRIX | |||||
| Cytochrome P450 2C19 | Enzyme | IC50 | 7.80 | DRUG MATRIX | |||||
| Alkaline phosphatase, tissue-nonspecific isozyme | Enzyme | EC50 | 4.22 | CHEMBL | |||||
| Tyrosine-protein kinase Fyn | Kinase | IC50 | 5.43 | DRUG MATRIX | |||||
| Thromboxane-A synthase | Enzyme | IC50 | 6.74 | DRUG MATRIX | |||||
| Bile acid receptor | Nuclear hormone receptor | IC50 | 5.16 | CHEMBL | |||||
| Indoleamine 2,3-dioxygenase 1 | Enzyme | IC50 | 5.19 | CHEMBL | |||||
| Substance-K receptor | GPCR | Ki | 5.78 | DRUG MATRIX | |||||
| Malate dehydrogenase cytoplasmic | Enzyme | IC50 | 4.70 | CHEMBL | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 5.82 | DRUG MATRIX | |||||
| Lanosterol 14-alpha demethylase | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Beta-lactamase | Enzyme | IC50 | 4.85 | CHEMBL | |||||
| Indoleamine 2,3-dioxygenase 2 | Enzyme | IC50 | 5 | CHEMBL | |||||
| Indoleamine 2,3-dioxygenase 1 | Enzyme | IC50 | 4.53 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019938 | VUID |
| N0000148023 | NUI |
| D00886 | KEGG_DRUG |
| 61318-91-0 | SECONDARY_CAS_RN |
| 4019499 | VANDF |
| 4019938 | VANDF |
| C0075503 | UMLSCUI |
| CHEBI:9325 | CHEBI |
| CHEMBL1221 | ChEMBL_ID |
| CHEMBL1200348 | ChEMBL_ID |
| DB06820 | DRUGBANK_ID |
| C033308 | MESH_SUPPLEMENTAL_RECORD_UI |
| 5318 | PUBCHEM_CID |
| 4332 | INN_ID |
| 5D9HAA5Q5S | UNII |
| 37319 | RXNORM |
| 358697 | MMSL |
| 5521 | MMSL |
| 002933 | NDDF |
| 004964 | NDDF |
| 108920000 | SNOMEDCT_US |
| 108921001 | SNOMEDCT_US |
| 373448004 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Exelderm | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69489-711 | CREAM | 10 mg | TOPICAL | NDA | 18 sections |
| Exelderm | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69489-721 | SOLUTION | 10 mg | TOPICAL | NDA | 17 sections |
| Sulconazole Nitrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72143-311 | CREAM | 10 mg | TOPICAL | NDA | 18 sections |
| Sulconazole Nitrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72143-321 | SOLUTION | 10 mg | TOPICAL | NDA | 17 sections |