Efinaconazole
CAS:164650-44-6
MF:C18H22F2N4O
In October 2013, efinaconazole (also known as KP-103) was approved in Canada as a 10% topical solution for the treatment of onychomycosis. Like other azole antifungal agents, efinaconazole acts by disrupting fungal cell membranes through inhibition of sterol 14α-demethylase, an enzyme involved in the biosynthesis of ergosterol, which is a key component of the fungal cell membrane. Unlike other antifungal agents, efinaconazole retains activity in the presence of keratin, indicating that more unbound drug is available at the site of action.
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Description
Efinaconazole CAS 164650-44-6 Product Information
| Product Name: | Efinaconazole |
| Synonyms: | KP 103;KP 103 (pharmaceutical);(2R,3R)-2-(2,4-Difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1,2,4-triazol-1-yl)-2-butanol;Efinaconazole(KP 103);(R,R)-2-(2,4-Difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1,2,4-triazol-1-yl)-2-butanol;(αR,βR)-α-(2,4-Difluorophenyl)-β-methyl-4-methylene-α-(1H-1,2,4-triazol-1-ylmethyl)-1-piperidineethanol;1-Piperidineethanol, α-(2,4-difluorophenyl)-β-methyl-4-methylene-α-(1H-1,2,4-triazol-1-ylmethyl)-, (αR,βR)-;Efinaconazole (Jublia) |
| CAS NO: | 164650-44-6 |
| Molecular Weight: | 348.390 |
| Molecular Formula: | C18H22F2N4O |
| Boiling Point: | 512.2±60.0 °C at 760 mmHg |
| Melting point: | 192-195°C |
| Density: | 1.26±0.1 g/cm3(Predicted) |
| Appearance: | white to beige powder |
| Applications: | Efinaconazole is a broad-spectrum triazole antifungal agent with activity against Acremonium, Aspergillus, Candida, Cryptococcus, Epidermophyton, Fusarium, Microsporum, Paecilomyces, Pseudallescheria, Scopulariopsis, Trichophyton, and Trichosporon. |
| Solubility: | Chloroform (Slightly), Methanol (Slightly) |
| Storage: | -20°C |
What is Efinaconazole?
Efinaconazole is a broad-spectrum triazole antifungal agent with activity against Acremonium, Aspergillus, Candida, Cryptococcus, Epidermophyton, Fusarium, Microsporum, Paecilomyces, Pseudallescheria, Scopulariopsis, Trichophyton, and Trichosporon. It inhibits the growth of T. rubrum and T. mentagrophytes clinical isolates with MIC values ranging from ≤2.0 to 60 ng/ml and of C. Albicans isolates with MIC values ranging from ≤0.5 to >250 ng/ml. Efinaconazole inhibits sterol 14α-demethylase, which arrests ergosterol (Item No. 19850) biosynthesis at the fungal membrane. It inhibits ergosterol biosynthesis in T. mentagrophytes and C. Albicans with IC50 values of 7.0 and 0.40 ng/ml, respectfully. Topical formulations containing efinaconazole have been used for the treatment of onychomycosis.
efinaconazole efficacy/efinaconazole how well does it work
It inhibits the growth of T. rubrum and T. mentagrophytes clinical isolates with MIC values ranging from ≤2.0 to 60 ng/ml and of C. albicans isolates with MIC values ranging from ≤0.5 to >250 ng/ml. Efinaconazole inhibits sterol 14α-demethylase, which arrests ergosterol biosynthesis at the fungal membrane. It inhibits ergosterol biosynthesis in T. mentagrophytes and C. albicans with IC50 values of 7.0 and 0.40 ng/ml, respectfully. Topical formulations containing efinaconazole have been used for the treatment of onychomycosis.
efinaconazole vs tavaborole/tavaborole vs efinaconazole/efinaconazole vs ciclopirox
Efinaconazole showed potent fungicidal activity in keratin-containing medium, whereas tavaborole was fungistatic, and ciclopirox not active. In the guinea pig model of onychomycosis, the therapeutic efficacy of efinaconazole was superior to those of tavaborole and ciclopirox.
Additional information
| Melting Point | 156°C |
|---|---|
| Boiling point | 600.0±60.0 °C(Predicted) |
| Flash Point | 9 °C |
| Density | 1.332 g/cm3 |
| Solubility | H2O: 0.5 mg/mL |
| Color | White |
| Form | Powder |
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