U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C7H6BFO2
Molecular Weight 151.931
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TAVABOROLE

SMILES

OB1OCC2=CC(F)=CC=C12

InChI

InChIKey=LFQDNHWZDQTITF-UHFFFAOYSA-N
InChI=1S/C7H6BFO2/c9-6-1-2-7-5(3-6)4-11-8(7)10/h1-3,10H,4H2

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4662369/

Tavaborole is a boron-based pharmaceutical agent indicated for the topical treatment of toenail onychomycosis, a fungal infection of the nail and nail bed due to Trichophyton rubrum or Trichophyton mentagrophytes infection. Tavaborole acts by inhibiting an aminoacyl-transfer ribonucleic acid (tRNA) synthetase (AARS) - Leucyl-tRNA synthetase. Leucyl-tRNA synthetase is an essential fungal enzyme required for protein synthesis and for the catalysis of ATP-dependent ligation of L-leucine to tRNA(Leu). Tavaborole’s low molecular weight (approximately half of most antifungals, such as terbinafine and efinaconazole) permits optimal nail plate penetration, superior to that of existing topical antifungal medications.

Originator

Approval Year

2014
494
Targets

Targets

Primary TargetPharmacologyConditionPotency
ENTREZ Gene ID: 10373871 (leucyl-tRNA synthetase)
1
Target ID: ENTREZ Gene ID: 10373871 (leucyl-tRNA synthetase)
Antagonist
2778
ENTREZ Gene ID: 10373705 (leucyl-tRNA synthetase)
1
Target ID: ENTREZ Gene ID: 10373705 (leucyl-tRNA synthetase)
Antagonist
2778
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Approved
8429
KERYDIN

Approved Use

KERYDIN (tavaborole) topical solution, 5% is an oxaborole antifungal indicated for the treatment of onychomycosis of the toenails due to Trichophyton rubrum or Trichophyton mentagrophytes.

Launch Date

2014
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
5.9 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204427s006lbl.pdf
5 % 1 times / day multiple, topical
dose: 5 %
route of administration: Topical
experiment type: MULTIPLE
co-administered:
TAVABOROLE blood
Homo sapiens
population: UNHEALTHY
age: ADOLESCENT
sex: UNKNOWN
food status: UNKNOWN
5.2 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204427s006lbl.pdf
5 % 1 times / day multiple, topical
dose: 5 %
route of administration: Topical
experiment type: MULTIPLE
co-administered:
TAVABOROLE blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
76 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204427s006lbl.pdf
5 % 1 times / day multiple, topical
dose: 5 %
route of administration: Topical
experiment type: MULTIPLE
co-administered:
TAVABOROLE blood
Homo sapiens
population: UNHEALTHY
age: ADOLESCENT
sex: UNKNOWN
food status: UNKNOWN
75.8 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204427s006lbl.pdf
5 % 1 times / day multiple, topical
dose: 5 %
route of administration: Topical
experiment type: MULTIPLE
co-administered:
TAVABOROLE blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
28.5 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000ClinPharmR.pdf
5 % 1 times / day multiple, topical
dose: 5 %
route of administration: Topical
experiment type: MULTIPLE
co-administered:
TAVABOROLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
7.5 % 1 times / day multiple, topical
Highest studied dose
Dose: 7.5 %, 1 times / day
Route: topical
Route: multiple
Dose: 7.5 %, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
Disc. AE: Application site stinging, Pruritus...
Other AEs: Application site irritation, Application site erythema...
AEs leading to
discontinuation/dose reduction:
Application site stinging (grade 2)
Pruritus (grade 2)
Irritation skin (grade 3)
Other AEs:
Application site irritation
Application site erythema
Application site reaction
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.78
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.78
Disc. AE: Application site erythema, Application site exfoliation...
AEs leading to
discontinuation/dose reduction:
Application site erythema (grade 2, 0.5%)
Application site exfoliation (grade 2, 0.5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.78
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Disc. AE: Ingrowing nail, Application site pain...
Other AEs: Skin induration...
AEs leading to
discontinuation/dose reduction:
Ingrowing nail (0.5%)
Application site pain (0.5%)
Application site discharge (0.5%)
Application site exfoliation (0.5%)
Application site edema (0.5%)
Edema peripheral (0.5%)
Application site erythema (0.5%)
Erythema (0.5%)
Application site induration (0.5%)
Application site reaction (0.5%)
Skin maceration (0.5%)
Application site pruritus (0.5%)
Pruritus (0.5%)
Other AEs:
Skin induration (0.5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 205
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 205
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Other AEs: Dermatitis contact...
Other AEs:
Dermatitis contact (0.5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
Other AEs: Upper respiratory tract infection, Back pain...
Other AEs:
Upper respiratory tract infection (5.44%)
Back pain (3.29%)
Application site exfoliation (2.65%)
Ingrowing nail (2.53%)
Procedural pain (2.53%)
Muscle strain (2.4%)
Arthralgia (2.15%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
Other AEs: Hypercholesterolaemia, Blood creatinine increased...
Other AEs:
Hypercholesterolaemia (1.01%)
Blood creatinine increased (0.51%)
Blood glucose increased (0.38%)
Blood urea increased (0.38%)
Hyperglycaemia (0.38%)
Hyperlipidaemia (0.38%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
AEs

AEs

AESignificanceDosePopulation
Application site erythema
7.5 % 1 times / day multiple, topical
Highest studied dose
Dose: 7.5 %, 1 times / day
Route: topical
Route: multiple
Dose: 7.5 %, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
Application site irritation
7.5 % 1 times / day multiple, topical
Highest studied dose
Dose: 7.5 %, 1 times / day
Route: topical
Route: multiple
Dose: 7.5 %, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
Application site reaction
7.5 % 1 times / day multiple, topical
Highest studied dose
Dose: 7.5 %, 1 times / day
Route: topical
Route: multiple
Dose: 7.5 %, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
Application site stinging grade 2
Disc. AE
7.5 % 1 times / day multiple, topical
Highest studied dose
Dose: 7.5 %, 1 times / day
Route: topical
Route: multiple
Dose: 7.5 %, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
Pruritus grade 2
Disc. AE
7.5 % 1 times / day multiple, topical
Highest studied dose
Dose: 7.5 %, 1 times / day
Route: topical
Route: multiple
Dose: 7.5 %, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
Irritation skin grade 3
Disc. AE
7.5 % 1 times / day multiple, topical
Highest studied dose
Dose: 7.5 %, 1 times / day
Route: topical
Route: multiple
Dose: 7.5 %, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/24894552/
https://pubmed.ncbi.nlm.nih.gov/25226015/
https://pubmed.ncbi.nlm.nih.gov/27224843/
Application site erythema grade 2, 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.78
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.78
Application site exfoliation grade 2, 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.78
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.78
Skin induration 0.5%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Application site discharge 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Application site edema 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Application site erythema 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Application site exfoliation 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Application site induration 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Application site pain 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Application site pruritus 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Application site reaction 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Edema peripheral 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Erythema 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Ingrowing nail 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Pruritus 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Skin maceration 0.5%
Disc. AE
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 194
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 194
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Dermatitis contact 0.5%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
unhealthy, mean age 55 years
n = 205
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 205
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Arthralgia 2.15%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
Muscle strain 2.4%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
Ingrowing nail 2.53%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
Procedural pain 2.53%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
Application site exfoliation 2.65%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
Back pain 3.29%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
Upper respiratory tract infection 5.44%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.83
Blood glucose increased 0.38%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
Blood urea increased 0.38%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
Hyperglycaemia 0.38%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
Hyperlipidaemia 0.38%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
Blood creatinine increased 0.51%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
Hypercholesterolaemia 1.01%
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
unhealthy, mean age 55 years
n = 791
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 55 years
Sex: M+F
Population Size: 791
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000MedR.pdf
Page: nda/2014/204427Orig1s000MedR.pdf - p.85
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737
inducer
389

inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2A6
707

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP2E1
882

CYP3A4/5
278
CYP3A5
395

CYP2C18
138

CYP2C19
991

FMO3
67
CYP1A2
701

CYP2B6
547

CYP2C8
168

CYP2C19
293

CYP3A4/5
124
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 unlikely [IC50 >100 uM]
CYP2B6
1001
 unlikely [IC50 >100 uM]
CYP2C19
1553
 unlikely [IC50 >100 uM]
CYP2C8
965
 unlikely [IC50 >100 uM]
CYP2C9
1819
 unlikely [IC50 >100 uM]
CYP2D6
1891
 unlikely [IC50 >100 uM]
CYP3A4/5
335
 unlikely [IC50 >100 uM]
CYP2A6
739
 unlikely [Inhibition 100 uM]
CYP2E1
970
 unlikely [Inhibition 100 uM]
CYP1A2
1692
 unlikely
CYP2B6
1001
 unlikely
CYP2C19
1553
 unlikely
CYP2C8
965
 unlikely
CYP2C9
1819
 unlikely
CYP3A4/5
335
 unlikely
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2C18
138
 yes
CYP2C19
991
 yes
CYP3A4
1737
 yes
CYP3A5
395
 yes
FMO3
67
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:77942
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:77942
ChemicalBook
CB42454906
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB42454906
MolPort
MolPort-027-845-281
https://www.molport.com/shop/molecule-link/MolPort-027-845-281
ZINC
ZINC000169990691
http://zinc15.docking.org/substances/ZINC000169990691
PubMed

PubMed

TitleDatePubMed
Recent progress on the topical therapy of onychomycosis.
2007 Feb
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
2007 Jun 22
Crystal structures of the human and fungal cytosolic Leucyl-tRNA synthetase editing domains: A structural basis for the rational design of antifungal benzoxaboroles.
2009 Jul 10
The efficacy and safety of tavaborole, a novel, boron-based pharmaceutical agent: phase 2 studies conducted for the topical treatment of toenail onychomycosis.
2014 Sep
Patents

Patents

07271264
1
08106031
3
20050261277
1
20060234981
3
20070155699
3
20070265226
2

Sample Use Guides

In Vivo Use Guide
Tavaborole 5% topical solution (each milliliter of solution contains 43.5 mg of tavaborole) should be applyed to affected toenails once daily for 48 weeks. It should be applied to the entire toenail surface and under the tip of each toenail being treated (for topical use only and not for oral, ophthalmic, or intravaginal use).
Route of Administration: Topical
In Vitro Use Guide
Tavaborole demonstrated minimum inhibitory concentration (MIC) values ranging from 0.25–2 μg/mL against all fungi tested; addition of 5% keratin powder did not affect the MIC against T rubrum. The minimum fungicidal concentration (MFC) values for tavaborole against T rubrum and T mentagrophytes were 8 and 16 μg/mL, respectively.
Name Type Language
TAVABOROLE
DASH   INN   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
Tavaborole [WHO-DD]
Common Name English
TAVABOROLE [VANDF]
Common Name English
TAVABOROLE [MI]
Common Name English
tavaborole [INN]
Common Name English
TAVABOROLE [ORANGE BOOK]
Common Name English
TAVABOROLE [USAN]
Common Name English
AN-2690
Code English
AN2690
Code English
2,1-BENZOXABOROLE, 5-FLUORO-1,3-DIHYDRO-1-HYDROXY-
Systematic Name English
KERYDIN
Brand Name English
5-Fluoro-2,1-benzoxaborol-1(3H)-ol
Systematic Name English
5-FLUORO-1,3-DIHYDRO-1-HYDROXY-2,1-BENZOXABOROLE
Systematic Name English
Classification Tree Code System Code
NDF-RT N0000191279
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
NCI_THESAURUS C28394
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
NCI_THESAURUS C514
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
WHO-ATC D01AE24
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
Code System Code Type Description
DAILYMED
K124A4EUQ3
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
DRUG CENTRAL
4877
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
NDF-RT
N0000008253
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY Boron Compounds [Chemical/Ingredient]
LACTMED
Tavaborole
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
HSDB
8342
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
MERCK INDEX
m11751
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
INN
9425
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
USAN
XX-15
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
DRUG BANK
DB09041
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
CAS
174671-46-6
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
FDA UNII
K124A4EUQ3
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
ChEMBL
CHEMBL443052
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
CHEBI
77942
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
NCI_THESAURUS
C81725
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
SMS_ID
100000174859
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
WIKIPEDIA
Tavaborole
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
RXCUI
1543173
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY RxNorm
EPA CompTox
DTXSID00169888
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
PUBCHEM
11499245
Created by admin on Fri Dec 15 16:26:19 GMT 2023 , Edited by admin on Fri Dec 15 16:26:19 GMT 2023
PRIMARY
ACTIVE MOIETY
Structure of TAVABOROLE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
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