|(2R,3R)-2-(2,4-二氟苯基)-3-(4-亚甲基哌啶-1-基)-1-(1H-1,2,4-三唑-1-基)-2-丁醇|CsnPharm

CAS No.: 164650-44-6

艾氟康唑 Catalog No. CSN13754

Synonyms: KP-103;CTK5J2975;AGJ95634

Efinaconazole is a triazole antifungal used to treat for onychomycosis, as it is a 14 alpha-demethylase inhibitor.

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实验方案

技术信息

生物活性

描述Efinaconazole is a triazole antifungal agent. Efinaconazole has broad-spectrum antifungal activity against dermatophytes, nondermatophyte molds and yeasts, and high ungual penetration due to its low keratin binding properties^[3]. Efinaconazole againsts T. mentagrophytes SM-110 and C. albicans ATCC 10231 with MICs of 0.0039 μg/mL and 0.00098 μg/mL, respectively. Efinaconazole dose-dependently decreased ergosterol production and accumulated 4,4-dimethylsterols and 4α-methylsterols at concentrations below its MICs. Efinaconazole induced morphological and ultrastructural changes in T. mentagrophytes hyphae that became more prominent with increasing drug concentrations^[1]. Onychomycosis is a common but difficult to treat nail disorder. Both efinaconazole and combination with laser were efficacious treatment, but the combination therapy leads to quicker resolution with fewer rate of relapse^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03280927	Mild to Moderate Onychomycosis... more >> Due to Dermatophyte Collapse <<	Phase 4	Recruiting	October 1, 2019	Korea, Republic of ... more >> Konkuk University Medical Center Recruiting Seoul, Korea, Republic of Contact: Yang-Won Lee, Ph. D 82-2-2030-7573 20050078@kuh.ac.kr Collapse <<
NCT03022916	Distal Lateral Subungual Onych... more >>omycosis (DLSO) Collapse <<	Not Applicable	Recruiting	December 2017	United States, Alabama ... more >> The Kirklin Clinic Recruiting Birmingham, Alabama, United States, 35249 Contact: Boni Elewski, MD 205-502-9962 dermresearch@uabmc.edu Collapse <<
NCT03168841	Onychomycosis	Phase 3	Active, not recruiting	December 20, 2018	United States, California ... more >> Western University of Health Sciences Pomona, California, United States, 91711 Collapse <<

更多
参考文献

[1] Tatsumi Y, Nagashima M, Shibanushi T, et al. Mechanism of action of efinaconazole, a novel triazole antifungal agent. Antimicrob Agents Chemother. 2013;57(5):2405‐2409
[2] Tatsum Y, Yokoo M, et al. KP-103, a novel triazole derivative, is effective in preventing relapse and successfully treating experimental interdigital tinea pedis and tinea corporis in guinea pigs. Microbiol Immunol. 2002;46(7):425-32.
[3] Gupta AK, Cernea M. How effective is efinaconazole in the management of onychomycosis?. Expert Opin Pharmacother. 2016;17(4):611‐618
[4] Bonhert K, Dorizas A, Sadick NS. Efficacy of combination therapy with efinaconazole 10% solution and 1064 nm Nd:YAG laser for treatment of toenail onychomycosis. J Cosmet Laser Ther. 2019;21(3):179‐183

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8703 mL
- 14.3517 mL
- 28.7035 mL
- 5 mM
- 0.5741 mL
- 2.8703 mL
- 5.7407 mL
- 10 mM
- 0.2870 mL
- 1.4352 mL
- 2.8703 mL

技术信息

CAS号

164650-44-6

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H22F2N4O

运输

蓝冰

分子量

348.39

别名

KP-103;CTK5J2975;AGJ95634;KB145948;trade name: Jublia;艾氟康唑

溶解度

DMSO	68.0 mg/mL (195.2 mM)
Water	Insoluble
Ethanol	68.0 mg/mL (195.2 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03280927	Mild to Moderate Onychomycosis... more >> Due to Dermatophyte Collapse <<	Phase 4	Recruiting	October 1, 2019	Korea, Republic of ... more >> Konkuk University Medical Center Recruiting Seoul, Korea, Republic of Contact: Yang-Won Lee, Ph. D 82-2-2030-7573 20050078@kuh.ac.kr Collapse <<
NCT03022916	Distal Lateral Subungual Onych... more >>omycosis (DLSO) Collapse <<	Not Applicable	Recruiting	December 2017	United States, Alabama ... more >> The Kirklin Clinic Recruiting Birmingham, Alabama, United States, 35249 Contact: Boni Elewski, MD 205-502-9962 dermresearch@uabmc.edu Collapse <<
NCT03168841	Onychomycosis	Phase 3	Active, not recruiting	December 20, 2018	United States, California ... more >> Western University of Health Sciences Pomona, California, United States, 91711 Collapse <<
NCT02812771	Onychomycosis	Phase 4	Active, not recruiting	January 2019	United States, Alabama ... more >> Valeant Site 01 Birmingham, Alabama, United States, 35201 United States, California Valeant Site 04 Fountain Valley, California, United States, 92708 Valeant Site 03 Santa Rosa, California, United States, 95403 United States, Florida Valeant SIte 05 South Miami, Florida, United States, 33143 United States, Louisiana Valeant Site 09 New Orleans, Louisiana, United States, 70130 United States, Maryland Valeant Site 08 Baltimore, Maryland, United States, 21214 United States, New York Valeant Site 02 Forest Hills, New York, United States, 11375 United States, Pennsylvania Valeant Site 06 Philadelphia, Pennsylvania, United States, 19107 United States, Texas Valeant Site 07 McAllen, Texas, United States, 78501 Dominican Republic Valeant Site 10 Santo Domingo, Dominican Republic Collapse <<
NCT03110029	Onychomycosis of Toenail	Phase 4	Active, not recruiting	July 2018	United States, Alabama ... more >> The Kirklin Clinic Birmingham, Alabama, United States, 35249 Collapse <<
NCT03098615	Onychomycosis ... more >> Dermatophytosis Collapse <<	Phase 4	Active, not recruiting	July 2018	United States, Alabama ... more >> The Kirklin Clinic Birmingham, Alabama, United States, 35249 Collapse <<

艾氟康唑 Catalog No. CSN13754

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