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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

Molecular Formula C7H6BFO2
Molecular Weight 151.931
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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.

Approval Year

Targets

Targets

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

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
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
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
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
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
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
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:
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
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:
5 % 1 times / day multiple, topical
Recommended
Dose: 5 %, 1 times / day
Route: topical
Route: multiple
Dose: 5 %, 1 times / day
Sources: 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: 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: 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: 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: 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: 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: 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: Page: nda/2014/204427Orig1s000MedR.pdf - p.79
Other AEs: Dermatitis contact...
Other AEs:
Dermatitis contact (0.5%)
Sources: 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: 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: 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: 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: 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: 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: 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:
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
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:
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
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:
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
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:
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
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:
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
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:
unhealthy, 18-65 years
n = 15
Health Status: unhealthy
Condition: onychomycosis
Age Group: 18-65 years
Sex: M+F
Population Size: 15
Sources:
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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: Page: nda/2014/204427Orig1s000MedR.pdf - p.85
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
unlikely [IC50 >100 uM]
unlikely [IC50 >100 uM]
unlikely [IC50 >100 uM]
unlikely [IC50 >100 uM]
unlikely [IC50 >100 uM]
unlikely [IC50 >100 uM]
unlikely [IC50 >100 uM]
unlikely [Inhibition 100 uM]
unlikely [Inhibition 100 uM]
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis.
2006 Jul 27
Spotlight on targeting aminoacyl-tRNA synthetases for the treatment of fungal infections.
2006 Jul-Aug
AN-2690, a novel antifungal for the topical treatment of onychomycosis.
2007 Aug
A genomic glimpse of aminoacyl-tRNA synthetases in malaria parasite Plasmodium falciparum.
2009 Dec 31
Post-transfer editing by a eukaryotic leucyl-tRNA synthetase resistant to the broad-spectrum drug AN2690.
2010 Sep 1
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
Tavaborole: first global approval.
2014 Sep
Patents

Sample Use Guides

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.
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:26:19 GMT 2023
Edited
by admin
on Fri Dec 15 16:26:19 GMT 2023
Record UNII
K124A4EUQ3
Record Status Validated (UNII)
Record Version
  • Download
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
Related Record Type Details
TARGET ORGANISM->INHIBITOR
TARGET ORGANISM->INHIBITOR
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METABOLITE -> PARENT
MINOR
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC SINGLE TOPICAL APPLICATION ON DAY 1