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

Details

Stereochemistry ABSOLUTE
Molecular Formula C18H22F2N4O
Molecular Weight 348.391
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EFINACONAZOLE

SMILES

C=C1CCN(CC1)[C@]([H])(C)[C@](Cn2cncn2)(c3ccc(cc3F)F)O

InChI

InChIKey=NFEZZTICAUWDHU-RDTXWAMCSA-N
InChI=1S/C18H22F2N4O/c1-13-5-7-23(8-6-13)14(2)18(25,10-24-12-21-11-22-24)16-4-3-15(19)9-17(16)20/h3-4,9,11-12,14,25H,1,5-8,10H2,2H3/t14-,18-/m1/s1

HIDE SMILES / InChI

Molecular Formula C18H22F2N4O
Molecular Weight 348.391
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: description was created based on several sources, including

Efinaconazole is triazole used as a 10% topical solution for the treatment of onychomycosis, a fungal infection of the nails. It was approved for use in Canada and the USA in 2014 and is marketed by Valeant Pharmaceuticals North America LLC under the name Jublia. Like other antifungal triazoles, efinaconazole inhibits the fungal cytochrome P450 enzyme lanosterol 14α demethylase (CYP51), thereby disrupting ergosterol synthesis and, consequently, membrane integrity and growth in fungi. CYP51 is evolutionarily conserved and, in mammals, mediates conversion of lanosterol to meiosis-activating sterols (MAS); MAS are intermediates in the biosynthesis of cholesterol and may have a signaling role in initiating meiosis and oocyte maturation. Azoles have higher affinity for fungal CYP51 compared to the mammalian enzyme and such selectivity contributes to the safety of this therapeutic class. Azoles have been reported to produce reproductive and developmental toxicity in both humans and laboratory animals. The mechanism is unknown but inhibition of mammalian CYP51 as well as other CYPs, e.g. CYP17, CYP19 and CYP26, have been postulated to play a role.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
JUBLIA

Approved Use

Indicated for the topical treatment of onychomycosis of the toenail(s) due to Trichophyton rubrum and Trichophyton mentagrophytes.

Launch Date

1.40201283E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.55 ng/mL
42 mg 1 times / day multiple, topical
dose: 42 mg
route of administration: Topical
experiment type: MULTIPLE
co-administered:
EFINACONAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADOLESCENT
sex: UNKNOWN
food status: UNKNOWN
0.67 ng/mL
42 mg 1 times / day multiple, topical
dose: 42 mg
route of administration: Topical
experiment type: MULTIPLE
co-administered:
EFINACONAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
11.4 ng × h/mL
42 mg 1 times / day multiple, topical
dose: 42 mg
route of administration: Topical
experiment type: MULTIPLE
co-administered:
EFINACONAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADOLESCENT
sex: UNKNOWN
food status: UNKNOWN
12.15 ng × h/mL
42 mg 1 times / day multiple, topical
dose: 42 mg
route of administration: Topical
experiment type: MULTIPLE
co-administered:
EFINACONAZOLE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
29.9 h
42 mg 1 times / day multiple, topical
dose: 42 mg
route of administration: Topical
experiment type: MULTIPLE
co-administered:
EFINACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
3.85%
EFINACONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
healthy, adult
n = 239
Health Status: healthy
Age Group: adult
Population Size: 239
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
Other AEs: Coronary artery disease, Seizure...
Other AEs:
Coronary artery disease (0.4%)
Seizure (0.4%)
Large intestine infection (0.4%)
Pneumonia (0.4%)
Numbness in leg (0.4%)
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Disc. AE: Acute psychosis, Application site eczema...
AEs leading to
discontinuation/dose reduction:
Acute psychosis (0.1%)
Application site eczema (0.2%)
Application site erythema (0.3%)
Application site exfoliation (0.1%)
Application site irritation (0.2%)
Application site pain (0.1%)
Application site pruritus (0.2%)
Application site reaction (0.1%)
Application site swelling (0.2%)
Application site vesicles (0.5%)
Blood glucose abnormal (0.1%)
Dermatitis (0.1%)
Dermatitis contact (0.2%)
Headache (0.1%)
Intracranial aneurysm (0.1%)
Lung squamous cell carcinoma stage unspecified (0.1%)
Lymphadenopathy (0.1%)
Prostate cancer (0.1%)
Extrasystoles ventricular (0.1%)
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosiss
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Disc. AE: Application site dermatitis...
AEs leading to
discontinuation/dose reduction:
Application site dermatitis (1.1%)
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
Other AEs: Application site dermatitis, Application site vesicles...
Other AEs:
Application site dermatitis (2.2%)
Application site vesicles (1.6%)
Application site pain (1.1%)
Ingrowing nail (2.3%)
Contact dermatitis (2.2%)
Eczema (2%)
Rash (1.1%)
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
AEs

AEs

AESignificanceDosePopulation
Coronary artery disease 0.4%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
healthy, adult
n = 239
Health Status: healthy
Age Group: adult
Population Size: 239
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
Large intestine infection 0.4%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
healthy, adult
n = 239
Health Status: healthy
Age Group: adult
Population Size: 239
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
Numbness in leg 0.4%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
healthy, adult
n = 239
Health Status: healthy
Age Group: adult
Population Size: 239
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
Pneumonia 0.4%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
healthy, adult
n = 239
Health Status: healthy
Age Group: adult
Population Size: 239
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
Seizure 0.4%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
healthy, adult
n = 239
Health Status: healthy
Age Group: adult
Population Size: 239
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.108
Acute psychosis 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site exfoliation 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site pain 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site reaction 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Blood glucose abnormal 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Dermatitis 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Extrasystoles ventricular 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Headache 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Intracranial aneurysm 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Lung squamous cell carcinoma stage unspecified 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Lymphadenopathy 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Prostate cancer 0.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site eczema 0.2%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site irritation 0.2%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site pruritus 0.2%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site swelling 0.2%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Dermatitis contact 0.2%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site erythema 0.3%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site vesicles 0.5%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site dermatitis 1.1%
Disc. AE
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosiss
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.103
Application site pain 1.1%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
Rash 1.1%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
Application site vesicles 1.6%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
Eczema 2%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
Application site dermatitis 2.2%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
Contact dermatitis 2.2%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
Ingrowing nail 2.3%
10 % 1 times / day multiple, topical
Recommended
Dose: 10 %, 1 times / day
Route: topical
Route: multiple
Dose: 10 %, 1 times / day
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
unhealthy, mean age 51 years
n = 1227
Health Status: unhealthy
Condition: onychomycosis
Age Group: mean age 51 years
Sex: M+F
Population Size: 1227
Sources: Page: /nda/2014/203567Orig1s000MedR.pdf - p.104
Overview

OverviewOther

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 46.1 uM]
no [IC50 >100 uM]
no
no
no
no
yes [IC50 0.194 uM]
yes [IC50 0.731 uM]
yes [IC50 1.36 uM]
yes
yes
Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Mechanism of action of efinaconazole, a novel triazole antifungal agent.
2013 May
Efinaconazole: first global approval.
2013 Nov
Patents

Sample Use Guides

10% solution for topical application once daily for 48 weeks
Route of Administration: Topical
Efinaconazole exhibits in vitro minimum inhibitory concentrations (MICs) of 0.06 μg/mL or less against most (≥90%) isolates of the following microorganisms: Trichophyton rubrum and Trichophyton mentagrophytes.
Substance Class Chemical
Created
by admin
on Sat Jun 26 07:30:06 UTC 2021
Edited
by admin
on Sat Jun 26 07:30:06 UTC 2021
Record UNII
J82SB7FXWB
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
EFINACONAZOLE
DASH   INN   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
EFINACONAZOLE [WHO-DD]
Common Name English
IDP-108
Code English
EFINACONAZOLE [ORANGE BOOK]
Common Name English
CLENAFIN
Brand Name English
EFINACONAZOLE [JAN]
Common Name English
1-PIPERIDINEETHANOL, .ALPHA.-(2,4-DIFLUOROPHENYL)-.BETA.-METHYL-4-METHYLENE-.ALPHA.-(1H-1,2,4-TRIAZOL-1-YLMETHYL)-,(.ALPHA.R,.BETA.R)-
Common Name English
JUBLIA
Brand Name English
(2R,3R)-2-(2,4-DIFLUOROFENIL)-3-(4-METILENOPIPERIDIN-1-IL)-1-(1H-1,2,4-TRIAZIN-1-IL)BUTAN-2-OL
Common Name English
EFINACONAZOLE [MI]
Common Name English
KP-103
Code English
1-PIPERIDINEETHANOL, .ALPHA.-(2,4-DIFLUOROPHENYL)-.BETA.-METHYL-4-METHYLENE-.ALPHA.-(1H-1,2,4-TRIAZOL-1-YLMETHYL)-, (R-(R*,R*))-
Common Name English
EFINACONAZOLE [INN]
Common Name English
EFINACONAZOLE [USAN]
Common Name English
(2R,3R)-2-(2,4-DIFLUOROPHENYL)-3-(4-METHYLENEPIPERIDIN-1-YL)-1-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-OL
Systematic Name English
EFINACONAZOLE [VANDF]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175487
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
WHO-ATC D01AC19
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
NCI_THESAURUS C514
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
Code System Code Type Description
FDA UNII
J82SB7FXWB
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
EPA CompTox
164650-44-6
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
PUBCHEM
489181
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
WIKIPEDIA
Efinaconazole
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
DRUG BANK
DB09040
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
JAPANESE REVIEW
CLENAFIN
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY APPROVED JULY 2014
INN
9349
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
ChEMBL
CHEMBL2103877
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
NCI_THESAURUS
C97998
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
EVMPD
SUB177957
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
MERCK INDEX
M11729
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
HSDB
8341
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
DRUG CENTRAL
4874
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
LACTMED
Efinaconazole
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
RXCUI
1539753
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY RxNorm
CAS
164650-44-6
Created by admin on Sat Jun 26 07:30:07 UTC 2021 , Edited by admin on Sat Jun 26 07:30:07 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC DAILY APPLICATIONS