JUBLIA® (efinaconazole) topical solution

JUBLIA® (efinaconazole) topical solution

JUBLIA® (efinaconazole) topical solution

JUBLIA (efinaconazole) topical solution, 10% is a clear, colorless to pale yellow solution for topical use. Each gram of JUBLIA contains 100 mg of efinaconazole. Efinaconazole is an azole antifungal with a chemical name of ((2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl) butan-2-ol).

Molecular Formula: C18H22F2N4O

Molecular Weight: 348.39

JUBLIA contains the following inactive ingredients: alcohol, anhydrous citric acid, butylated hydroxytoluene, C12-15 alkyl lactate, cyclomethicone, diisopropyl adipate, disodium edetate, and purified water.

INDICATIONS AND USAGE

JUBLIA (efinaconazole) topical solution, 10% is an azole antifungal indicated for the topical treatment of onychomycosis of the toenail(s) due to Trichophyton rubrum and Trichophyton mentagrophytes.

Mechanism of Action

JUBLIA topical solution is an azole antifungal. Efinaconazole inhibits fungal lanosterol 14α-demethylase involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes.

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Activity In Vitro and In Vivo: Efinaconazole has been shown to be active against isolates of the following microorganisms, both in vitro and in clinicalinfections. Efinaconazole exhibits in vitro minimum inhibitory concentrations (MICs) of 0.06 mcg/mL or less againstmost (≥90%) isolates of the following microorganisms:

Trichophyton rubrum

Trichophyton mentagrophytes

Mechanism of Resistance

Efinaconazole drug resistance development was studied in vitro against T. mentagrophytes, T. rubrum and C. albicans. Serial passage of fungal cultures in the presence of sub-growth inhibitory concentrations of efinaconazole increased the MIC by up to 4-fold. The clinical significance of these in vitro results is unknown.

DOSAGE AND ADMINISTRATION

Apply JUBLIA to affected toenails once daily for 48 weeks, using the integrated flow-through brush applicator. When applying JUBLIA, ensure the toenail, the toenail folds, toenail bed, hyponychium, and the undersurface of the toenail plate, are completely covered.

JUBLIA is for topical use only and not for oral, ophthalmic, or intravaginal use.

CONTRAINDICATIONS

None.

ADVERSE REACTIONS

General Disorders and Administration Site Conditions: Application site erythema and exfoliation

Skin and Subcutaneous Tissue Disorders: Onychomadesis, Nail discoloration

DRUG INTERACTIONS

In vitro studies have shown that JUBLIA, at therapeutic concentrations, neither inhibits nor induces cytochrome P450 (CYP450) enzymes.

USE IN SPECIFIC POPULATIONS

Pregnancy: There are no available human data for the use of JUBLIA during pregnancy to inform any drug associated risks of majorbirth defects, miscarriage, or adverse maternal or fetal outcomes.

Lactation: It is not known whether efinaconazole is excreted in human milk. After repeated subcutaneous administration, efinaconazole was detected in milk of nursing rats. Because many drugs are excreted in human milk, caution should be exercised when JUBLIA is administered to nursing women.

The developmental and health benefits of breastfeeding should be considered, along with the mother’s clinical need for JUBLIA, and any potential adverse effects on the breastfed infant from JUBLIA.

Pediatric Use

The safety and effectiveness of JUBLIA were established in patients 6 years and older. Use of JUBLIA in these age groups is supported by evidence from well-controlled trials in adults with additional data from an open-label safety study in 60 pediatric subjects ages 6 to 17 (including a pharmacokinetic study in 17 subjects 12 years to less than 17 years old). Safety and effectiveness of JUBLIA in pediatric subjects under 6 years of age have not been established.

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Geriatric Use

Of the total number of subjects in clinical trials of JUBLIA, 11.3% were 65 and over, while none were 75 and over. No overall differences in safety and effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and the younger subjects, but greater sensitivity of some older individuals cannot be ruled out.

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