更新于：2024-11-21

Fenticonazole Nitrate

硝酸芬替康唑

更新于：2024-11-21

概要

概要

基本信息

药物类型

小分子化药

别名

Fenticonazole、Fenticonazole nitrate (USAN)

+ [3]

靶点

Ergosterol

作用机制

麦角固醇生物合成抑制剂

治疗领域

感染泌尿生殖系统疾病皮肤和肌肉骨骼疾病

在研适应症

真菌病外阴阴道念珠菌病足癣+ [1]

非在研适应症-

原研机构-

在研机构

开封制药（集团）有限公司

北京美迪康信医药科技有限公司

南京海纳医药科技股份有限公司

+ [1]

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)临床3期

特殊审评-

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结构

分子式C24H20Cl2N2OS

InChIKeyZCJYUTQZBAIHBS-UHFFFAOYSA-N

CAS号72479-26-6

查看全部结构式(2)

关联

项与硝酸芬替康唑相关的临床试验

CTR20130445 / Not yet recruiting

硝酸芬替康唑阴道软胶囊治疗外阴阴道假丝酵母菌病多中心、随机、双盲、阳性药平行对照临床试验

评价硝酸芬替康唑阴道软胶囊治疗外阴阴道假丝酵母菌病的有效性和安全性。

开始日期-

申办/合作机构-

CTR20170167 / Recruiting临床3期

硝酸芬替康唑栓治疗外阴阴道假丝酵母菌病多中心、随机、剂量、疗程探索临床研究

评价硝酸芬替康唑栓治疗外阴阴道假丝酵母菌病的有效性和安全性

开始日期2016-08-09

申办/合作机构

山东特瑞林医药科技发展有限公司

CTR20130309 / Active, not recruiting临床2期

评价硝酸芬替康唑栓的有效性和安全性的多中心、随机、盲法、阳性药物平行对照II期临床试验

评价硝酸芬替康唑栓治疗外阴阴道念珠菌病的有效性和安全性，探索硝酸芬替康唑栓治疗外阴阴道念珠菌病的临床使用剂量。

开始日期2014-08-05

申办/合作机构

北京美迪康信医药科技有限公司

100 项与硝酸芬替康唑相关的临床结果

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100 项与硝酸芬替康唑相关的转化医学

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100 项与硝酸芬替康唑相关的专利（医药）

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项与硝酸芬替康唑相关的文献（医药）

2024-12-01·Antonie van Leeuwenhoek

Species distribution and antifungal susceptibility profiles of yeasts isolated from onychomycosis: a cross-sectional study with insights into emerging species

Article

作者: Kharazi, Mahboobeh ; Motamedi, Marjan ; Jabrodini, Ahmad ; Rezaei Arab, Maryam ; Shariat, Sahar ; Zomorodian, Kamiar ; Shabanzadeh, Shafigheh ; Ghasemi, Farnia ; Yazdanpanah, Somayeh

Candida onychomycosis is a common fungal infection affecting the nails, primarily caused by Candida (C.) species. Regarding the increasing trend of Candida onychomycosis and the antifungal resistant phenomenon in recent years, this study aims to evaluate the epidemiological characteristics of Candida onychomycosis, the distribution of emerging species, and the antifungal susceptibility profiles of isolates. Onychomycosis caused by yeast species was confirmed through direct examination and culture of nail scraping among all individuals suspected to have onychomycosis and referred to a medical mycology laboratory between June 2019 and March 2022. Species of yeast isolates were identified using the multiplex PCR and PCR-RFLP methods. The antifungal susceptibility of isolates to common antifungal agents and imidazole drugs was evaluated according to the M-27-A3 CLSI protocol. Among 101 yeast strains isolated from onychomycosis, Candida parapsilosis complex (50.49%) was the most common species, followed by C. albicans (20.79%) and C. tropicalis (10.89%). Rare species of yeasts such as C. guilliermondii and Saccharomyces cerevisiae were also identified by molecular methods. Results obtained from antifungal susceptibility testing showed significant differences in MIC values of isoconazole, fenticonazole, and sertaconazole among different species. Overall, a fluconazole-resistant rate of 3% was found among Candida species. Moreover, there was a statistically significant difference in MICs of fenticonazole and clotrimazole between the two most prevalent causative species, C. parapsilosis complex and C. albicans. Correct identification of the causative agents of onychomycosis and performing susceptibility testing could be helpful in choosing the most appropriate antifungal therapy.

2023-01-17·FEMS Microbiology Letters

Therapeutic effects of fenticonazole on bacterial vaginosis in mice

Article

作者: Peng, Peiran ; Dai, Hongbo ; Mei, Ru ; Zhu, Jun ; Yao, Chao ; Yu, Jinfen

AbstractBacterial vaginitis (BV) is a syndrome of increased vaginal discharge, fishy smelling leucorrhea, and itching and burning vulva caused by the microecological imbalance in the vagina induced by mixture of Gardnerella vaginalis (GV) and some anaerobic bacteria. Fenticonazole, an imidazole derivative and antimicrobial compound, has been demonstrated to exert effective therapeutic effects in mixed vaginitis. Accordingly, our study was designed to explore the potential role of fenticonazole in GV-infected BV mouse models. Female C57/BL6 mice were injected intraperitoneally with β-estradiol 3 days before and on the day of GV infection to maintain a pseudoestrus state. On the day of infection, mice were intravaginally inoculated with 20 µl of a suspension of GV (6 × 106 CFU/ml). Fenticonazole was administered as 2% vaginal cream (0.2 mg each mouse) by intravaginal application once a day for 3 days beginning the day of infection. At day 3 postinfection, the mice were sacrificed and vaginal washes were harvested. GV proliferation and Lactobacillus content were calculated in the vaginal lavage. Neutrophil counts in the vaginal lavage were observed through Pap staining. Myeloperoxidase (MPO) activity and proinflammatory cytokine (TNF-α, IL-1β, IL-6, iNOS, COX2, and NF-κB) levels in vaginal tissues were measured by ELISA and western blotting. Vaginal tissues were stained by hematoxylin and eosin (H&E) to examine the exfoliation of vaginal epithelial cells. GV infection increased GV proliferation and neutrophil counts but reduced Lactobacillus content in the vaginal lavage, as well as enhanced MPO activity, proinflammatory cytokine levels, and the exfoliation of vaginal epithelial cells in vaginal tissues of BV mouse models. However, administration of fenticonazole significantly ameliorated the above phenomena. Fenticonazole greatly improves the symptoms of GV-induced BV in mouse models.

2022-12-31·Drug Delivery

Corneal targeted fenticonazole nitrate-loaded novasomes for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

Article

作者: Amin, Maha M. ; Ahmed, Sadek ; Sayed, Sinar ; El-Korany, Sarah Mohamed

The purpose of this manuscript was to develop and optimize Fenticonazole Nitrate (FTN)-loaded novasomes aiming to enhance drug corneal penetration and to improve its antifungal activity. Ethanol injection was used to formulate FTN-loaded novasomes adopting a central composite design. The researched factors were: stearic acid concentration (g%) (A), span 80: drug ratio (B) and cholesterol amount (mg) (C), and their effects on percent entrapment efficiency (EE%), particle size (PS), poly-dispersity index (PDI), zeta potential (ZP), and in vitro drug release after 8 hours (Q8h) were studied. Numerical optimization by Design-Expert® software was employed to select the optimum formula in respect to highest EE%, ZP (as absolute value), and Q8h >80% and lowest PS and PDI. Additional evaluation of the optimum formula was accomplished by short term stability study, effect of gamma sterilization, determination of Minimal Inhibitory Concentration and ex vivo corneal permeation study. The in vivo evaluation of the optimum formula was done to ensure its safety via in vivo ocular irritancy and in vivo corneal tolerance studies. Also, the efficacy was confirmed through in vivo corneal uptake study and susceptibility test. The optimum formula with the highest desirability value (0.738) showed EE% (94.31%), PS (197.05 nm), ZP (-66.95 mV) and Q8h (85.33%). It revealed to be safe, with augmented corneal permeation (527.98 µg/cm²) that leads to higher antifungal activity. The above results confirmed the validity of novasomes to improve the corneal permeation and antifungal activity of Fenticonazole Nitrate.

项与硝酸芬替康唑相关的新闻（医药）

2021-04-02

·先导药物

成都先导开发出适用于DNA编码化合物库合成的碳-硫键偶联反应

▲限时免费参会名额倒计时🔥，1900+已报名成都先导研发化学中心丨成都先导药物开发股份有限公司（以下简称“成都先导”）研发团队深入研究用于DNA编码化合物（DEL）库合成的多种键的构建，比如：碳(sp2)-碳(sp3)键，碳(sp3)-碳(sp3)键，碳-杂原子键。近日，该团队报道了DNA上的铜促进的Ullmann偶联构建碳-硫键的反应。该反应普适性较好、效率高、对DNA无损伤、适用于DNA编码化合物库（DEL）的合成。该结果目前发表于Bioconjugate Chemistry1。图1. 研究结果文章发表碳-硫键的构筑对药物研发有重要意义硫醚代表了一个重要的药物结构单元广泛存在于药物结构中，例如芬替康唑(抗真菌)、沃蒂奥西汀(抗抑郁药)、阿昔替尼(抗癌药)、头孢他林福萨米尔(抗生素)和奈非那韦(抗病毒药物)。在传统的合成化学中，硫醚的构建已经有了广泛的研究，但DNA上的碳-硫键构建目前只有（1）以芳基铵盐为底物，通过芳香亲核取代反应构建2、（2）固载可逆吸附（RASS）促使的有机相的碳-硫偶联3这两则报道。这些方法都代表了非常有价值的合成工具，但还需开发直接地、高效地构建碳-硫键的方法。成都先导研发团队对Ullmann偶联进行充分的文献调研后，设计了DNA上的Ullmann偶联构筑碳-硫键的反应。反应条件优化条件优化中，作者首先考察了铜催化剂的影响。考虑到转化率和配置铜催化剂时的溶解性，作者选用了溴化亚铜为最佳催化剂。而后，探索了一系列的N,O-、N,N-、和O,O-双齿配体的影响，包括联吡啶, L-脯氨酸, ß-酮酯, N,N'-二甲基乙二胺和马大为发展的草酸酰胺配体。随后对不同碱和溶液进行了筛选，得到最优条件（图2）。图2. 最优条件底物普适性研究在最优条件下，作者探索硫酚和硫醇的反应活性。各种给电子和吸电子取代的硫酚都有中等到较好的转化率，但与吸电子相比给电子取代基的有较高的收率。含有羧基取代的和各种杂环芳香硫酚也有较好的转化率。随后，验证了芳基碘的反应活性。大部分芳基碘代物都可以良好的转化率得到预期产物。官能团如：-磺酰胺、-氯、-溴、-环丙烷等也能耐受。其他杂芳环，如吡唑、咪唑、恶唑、吡啶等，在中等转化率的条件下均可得到产物。此外，该团队研究了DNA连接的芳基碘化物与芳基硫醇的交叉底物验证。几乎所有的组合都能中等到较高的转化率(40%-90%)得到产物。（图3）图3. 底物普适性研究进一步地，研发团队通过共进实验验证了其结构并通过DNA连接和定量聚合酶链反应验证了反应对DNA无损伤。最后，该团队通过采用此方法完成了库合成的概念验证。总结综上所述，成都先导团队建立了一种直接、高效的DNA上的铜促进的 Ullmann交叉偶联构筑碳-硫键的反应。该反应以中等到较高的转化率实现了DNA连接的芳基和杂芳基碘化物和硫酚、硫醇的偶联。该方法普适性较好，对DNA无损伤，适用于DNA编码化合物（DEL）的合成。参考文献：(1) Yue Ji, Dongliang Dai, Huadong Luo, Simin Shen, Jing Fan, Zhao Wang, Min Chen, Jinqiao Wan, Jin Li, Huiyong Ma, Guansai Liu. C–S Coupling of DNA-Conjugated Aryl Iodides for DNA-Encoded Chemical Library Synthesis. Bioconjugate Chem. Article ASAP; DOI: 10.1021/acs.bioconjchem.1c00076.(2) Wang, D., Wen, X., Xiong, C., Zhao, J., Ding, C., Meng, Q., Zhou, H., Wang, C., Uchiyama, M., Lu, X., et al. (2019) Non-transition Metal-Mediated Diverse Aryl–Heteroatom Bond Formation of Arylammonium Salts. iScience 15, 307-315.(3) Flood, D. T., Zhang, X., Fu, X., Zhao, Z., Asai, S., Sanchez, B. B., Sturgell, E. J., Vantourout, J. C., Richardson, P., Flanagan, M. E., et al. (2020) RASS-Enabled S/P-C and S-N Bond Formation for DEL Synthesis. Angew. Chem., Int. Ed. 59, 7377-7383. 【关于药融圈】药融圈围绕我国生物医药产业链，针对生物医药大数据、技术和资本投资、药融园(产业园)等开展系列系统性工作，促进我国生物医药产业健康发展，完善产业链，共同面对全球合作和竞争。点分享点点赞点在看

100 项与硝酸芬替康唑相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02583	硝酸芬替康唑	D01AC12 G01AF12	DB13434

研发状态

批准上市

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适应症	国家/地区	公司	日期
真菌病	-	-	-

未上市

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适应症	最高研发状态	国家/地区	公司	日期
外阴阴道念珠菌病	临床3期	中国	山东特瑞林医药科技发展有限公司	2016-08-09
足癣	临床2期	中国	开封制药（集团）有限公司	2019-04-12
皮肤真菌病	临床1期	中国	南京海纳医药科技股份有限公司	2015-08-17