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tavaborole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4877 | 174671-46-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The mechanism of action of tavaborole is inhibition of fungal protein synthesis. Tavaborole inhibits protein synthesis by inhibition of an aminoacyl-transfer ribonucleic acid (tRNA) synthetase (AARS).Tavaborole has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections.
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 | 2.643 | Moderate | 0.76 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.594 | Moderate | 0.76 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 81.846 | 10^-6 cm/s | Moderate | 0.76 |
| dh-clint | Dog hepatocyte intrinsic clearance | 27.040 | uL/min/10^6 cells | Moderate | 0.76 |
| dppb | Dog plasma protein binding (% unbound) | 9.360 | % | Moderate | 0.76 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 17.120 | % | Moderate | 0.76 |
| herg | hERG pIC50 | 4.383 | pIC50 | Moderate | 0.76 |
| hh-clint | Human hepatocyte intrinsic clearance | 17.458 | uL/min/10^6 cells | Moderate | 0.76 |
| hlm-clint | Human liver microsomal intrinsic clearance | 22.961 | uL/min/mg protein | Moderate | 0.76 |
| hppb | Human plasma protein binding (% unbound) | 8.060 | % | Moderate | 0.76 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TGFBR1 | 18 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,RIPK1 | 4 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.521 | Moderate | 0.76 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 84.528 | Moderate | 0.76 | |
| mppb | Mouse plasma protein binding (% unbound) | 9.760 | Moderate | 0.76 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.984 | Moderate | 0.76 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 9.360 | % | Moderate | 0.76 |
| rh-clint | Rat hepatocyte intrinsic clearance | 59.156 | uL/min/10^6 cells | Moderate | 0.76 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 69.470 | % | Moderate | 0.76 |
| rppb | Rat plasma protein binding (% unbound) | 7.930 | % | Moderate | 0.76 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 36.224 | uM | Moderate | 0.76 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 7, 2014 | FDA | ANACOR PHARMS INC |
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 | D01AE24 | DERMATOLOGICALS ANTIFUNGALS FOR DERMATOLOGICAL USE ANTIFUNGALS FOR TOPICAL USE Other antifungals for topical use |
| FDA CS | M0002832 | Boron Compounds |
| FDA MoA | N0000000150 | Protein Synthesis Inhibitors |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000935 | Antifungal Agents |
| FDA EPC | N0000191279 | Oxaborole Antifungal |
| CHEBI has role | CHEBI:35718 | antifungal agent |
| CHEBI has role | CHEBI:48001 | protein synthesis inhibitor |
| CHEBI has role | CHEBI:77953 | EC 6.1.1.4 (leucine—tRNA ligase) inhibitor |
Related Drugs by ATC class:
D01AE Other antifungals for topical use 23 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Onychomycosis due to Trichophyton mentagrophytes | indication | 23549005 | |
| Onychomycosis due to Trichophyton rubrum | indication | 56922006 | |
| Onychomycosis due to dermatophyte | indication | 402134005 | |
| Onychomycosis of toenails | indication | 403059006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.49 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Carbonic anhydrase 2 | Enzyme | Ki | 6.33 | CHEMBL | |||||
| Carbonic anhydrase 1 | Enzyme | Ki | 5.70 | CHEMBL | |||||
| Leucine-tRNA ligase | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | Ki | 7.14 | CHEMBL | |||||
| Carbonic anhydrase 2 | Enzyme | Ki | 7.05 | CHEMBL | |||||
| Leucine--tRNA ligase, cytoplasmic | Enzyme | Ki | 5.73 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D10169 | KEGG_DRUG |
| 4033648 | VUID |
| N0000191084 | NUI |
| 4033648 | VANDF |
| CHEMBL443052 | ChEMBL_ID |
| C512998 | MESH_SUPPLEMENTAL_RECORD_UI |
| DB09041 | DRUGBANK_ID |
| 1543173 | RXNORM |
| 222423 | MMSL |
| 30392 | MMSL |
| 340008 | MMSL |
| 399962 | MMSL |
| 015655 | NDDF |
| 716264009 | SNOMEDCT_US |
| 763516005 | SNOMEDCT_US |
| C3642427 | UMLSCUI |
| CHEBI:77942 | CHEBI |
| A1CF8 | PDB_CHEM_ID |
| 9425 | INN_ID |
| 11499245 | PUBCHEM_CID |
| K124A4EUQ3 | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Tavaborole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21922-020 | SOLUTION | 43.50 mg | TOPICAL | ANDA | 24 sections |
| Tavaborole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 46708-467 | SOLUTION | 43.50 mg | TOPICAL | ANDA | 23 sections |
| tavaborole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-690 | SOLUTION | 43.50 mg | TOPICAL | ANDA | 28 sections |
| Tavaborole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62135-663 | SOLUTION | 43.50 mg | TOPICAL | ANDA | 16 sections |
| Tavaborole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62332-467 | SOLUTION | 43.50 mg | TOPICAL | ANDA | 23 sections |
| TAVABOROLE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-686 | SOLUTION | 43.50 mg | TOPICAL | ANDA | 25 sections |
| Tavaborole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1657 | SOLUTION | 43.50 mg | TOPICAL | ANDA | 24 sections |
| Tavaborole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1826 | SOLUTION | 43.50 mg | TOPICAL | ANDA | 1 sections |
| Tavaborole | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72578-102 | SOLUTION | 43.50 mg | TOPICAL | ANDA | 24 sections |