Efinaconazole

Research use only, not for human use.

Efinaconazole(KP-103) is an Azole Antifungal currently under development as a topical treatment for onychomycosis.

Efinaconazole is a triazole antifungal. It is approved for use in Canada and the USA as a 10% topical solution for the treatment of onychomycosis (fungal infection of the nail). Efinaconazole acts as a 14α-demethylase inhibitor. Efinaconazole inhibits fungal lanosterol 14α-demethylase involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes. Efinaconazole has been shown to be active against isolates of the following microorganisms, both in vitro and in clinical infections. 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; Trichophyton mentagrophytes.(In Vivo):Topical Efinaconazole solution (0.25 to 1%) is dose-dependently effective in treating both dermatophytoses, for 10 guinea pigs with interdigital tinea pedis or tinea corporis is investigated. The follow up study performs on day-30 and day-9 posttreatment demonstrated that the relapse rates for 1% Efinaconazole-treated animals with tinea pedis and for those with tinea corporis are 20 and 30%, respectively. When a single dose of 1% Efinaconazole is applied to the back skin 48 hours before fungal inoculation, 9 of the 10 animals are protected from the dermatophytosis, suggesting that active Efinaconazole is retained in skin tissue for at least 48 hours after dosing.

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Topical Efinaconazole solution (0.25 to 1%) is dose-dependently effective in treating both dermatophytoses, for 10 guinea pigs with interdigital tinea pedis or tinea corporis is investigated. The follow up study performs on day-30 and day-9 posttreatment demonstrated that the relapse rates for 1% Efinaconazole-treated animals with tinea pedis and for those with tinea corporis are 20 and 30%, respectively. When a single dose of 1% Efinaconazole is applied to the back skin 48 hours before fungal inoculation, 9 of the 10 animals are protected from the dermatophytosis, suggesting that active Efinaconazole is retained in skin tissue for at least 48 hours after dosing.

KP103 | KP-103 | CTK5J2975 | AGJ95634 | Efinaconazole

Angiogenesis

PDGFR

Antifungle

Infection

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164650-44-6

348.34

C18H22F2N4O

>98% (HPLC)

DMSO : ≥ 100 mg/mL;287.03 mM

C=C1CCN(CC1)[C@@H]([C@@](c1ccc(cc1F)F)(Cn1cncn1)O)C

(2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol

(-20℃)

With Ice Pack

≥ 2 years