特康唑(Terconazole) - 药物靶点：fungal CYP51A1_在研适应症：外阴阴道念珠菌病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Terconazole (USP/INN)

+ [4]

靶点

fungal CYP51A1

作用机制

fungal CYP51A1抑制剂(真菌细胞色素P450家族成员51抑制剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Fougera Pharmaceuticals, Inc.Taro Pharmaceuticals U.S.A., Inc.

非在研机构

Curatek Pharmaceuticals, LLCJanssen-Cilag SA

Janssen Pharmaceuticals, Inc.

最高研发阶段批准上市

首次获批日期

美国 (1987-12-31),

外阴阴道念珠菌病

最高研发阶段(中国)批准上市

特殊审评-

登录后查看时间轴

结构/序列

分子式C26H31Cl2N5O3

InChIKeyBLSQLHNBWJLIBQ-OZXSUGGESA-N

CAS号67915-31-5

关联

5

项与特康唑相关的临床试验

NCT02308007

/ Completed临床3期

Solubilized Metronidazole And/oR Terconazole Gels Intra-Vaginal Efficacy and Safety

The purpose of this study is to evaluate the safety and efficacy of terconazole/metronidazole gel in the treatment of vaginal infections

开始日期2015-06-01

申办/合作机构

Curatek Pharmaceuticals, LLC

NCT02308046

/ Completed临床3期

Solubilized Metronidazole And/oR Terconazole Gels Intra-Vaginal Efficacy and Safety

The purpose of this study is to evaluate the safety and efficacy of terconazole gel in the treatment of vaginal infections

开始日期2015-06-01

申办/合作机构

Curatek Pharmaceuticals, LLC

NCT01867164

/ Completed临床3期

A Prospective, Open-Label, Comparative, Parallel Double-Arm, Multicentric Clinical Study to Evaluate the Efficacy of an Ovule With Triple Active Agents (Terconazole, Clindamycin, Fluocinolone) Administered Once Per Day for Three Days Versus an Ovule With Triple Active Agents (Metronidazole, Nystatin, Fluocinolone) Administered Once Per Day for Ten Days to Treat Secondary Vulvar/Vaginal Symptoms of Vaginitis/Infectious Vaginosis (Bacterial and/or Mycotic and/or Parasitic)

The purpose of this comparative study is to evaluate the efficacy of an ovule with triple active agents (terconazole, clindamycin and fluocinolone) versus another ovule with triple active agents (nystatin, metronidazole and fluocinolone) in the treatment of symptoms caused by the presence of vaginitis (inflammation of the vagina) or bacterial vaginosis (polymicrobial, nonspecific vaginitis associated with positive cultures of Gardnerella vaginalis and other anaerobic organisms and a decrease in lactobacilli).

开始日期2007-12-01

申办/合作机构

Janssen-Cilag SA

100 项与特康唑相关的临床结果

登录后查看更多信息

100 项与特康唑相关的转化医学

登录后查看更多信息

100 项与特康唑相关的专利（医药）

登录后查看更多信息

121

项与特康唑相关的文献（医药）

2024-08-01·International Journal of Food Microbiology

Nobiletin enhances the antifungal activity of eugenol nanoemulsion against Penicillium italicum in both in vitro and in vivo settings

Article

作者: Guo, Long ; Liu, Yanchi ; Ye, Zimao ; Chen, Hongyang ; Zhou, Zhiqin ; Zhao, Lintao

The study prepared and used eugenol nanoemulsion loaded with nobiletin as fungistat to study its antifungal activity and potential mechanism of Penicillium italicum (P. italicum). The results showed that the minimum inhibitory concentration (MIC) of eugenol nanoemulsion loaded with nobiletin (EGN) was lower than that of pure eugenol nanoemulsion (EG), which were 160 μg/mL and 320 μg/mL, respectively. At the same time, the mycelial growth inhibition rate of EGN nanoemulsion (54.68 %) was also higher than that of EG nanoemulsion (9.92 %). This indicates that EGN nanoemulsion is more effective than EG nanoemulsion. Compared with EG nanoemulsion, the treatment of EGN nanoemulsion caused more serious damage to the cell structure of P. italicum. At the same time, in vitro inoculation experiments found that EGN nanoemulsion has better control and delay the growth and reproduction of P. italicum in citrus fruits. And the results reflected that EGN nanoemulsion may be considered as potential resouces of natural antiseptic to inhibit blue mold disease of citrus fruits, because it has good antifungal activity.

2024-08-01·International Journal for Parasitology: Drugs and Drug Resistance

Exploring therapeutic approaches against Naegleria fowleri infections through the COVID box

Article

作者: Lorenzo-Morales, Jacob ; Piñero, José E ; Chao-Pellicer, Javier ; Arberas-Jiménez, Iñigo ; Sifaoui, Ines

Naegleria fowleri, known as the brain-eating amoeba, is the pathogen that causes the primary amoebic meningoencephalitis (PAM), a severe neurodegenerative disease with a fatality rate exceeding 95%. Moreover, PAM cases commonly involved previous activities in warm freshwater bodies that allow amoebae-containing water through the nasal passages. Hence, awareness among healthcare professionals and the general public are the key to contribute to a higher and faster number of diagnoses worldwide. Current treatment options for PAM, such as amphotericin B and miltefosine, are limited by potential cytotoxic effects. In this context, the repurposing of existing compounds has emerged as a promising strategy. In this study, the evaluation of the COVID Box which contains 160 compounds demonstrated significant in vitro amoebicidal activity against two type strains of N. fowleri. From these compounds, terconazole, clemastine, ABT-239 and PD-144418 showed a higher selectivity against the parasite compared to the remaining products. In addition, programmed cell death assays were conducted with these four compounds, unveiling compatible metabolic events in treated amoebae. These compounds exhibited chromatin condensation and alterations in cell membrane permeability, indicating their potential to induce programmed cell death. Assessment of mitochondrial membrane potential disruption and a significant reduction in ATP production emphasized the impact of these compounds on the mitochondria, with the identification of increased ROS production underscoring their potential as effective treatment options. This study emphasizes the potential of the mentioned COVID Box compounds against N. fowleri, providing a path for enhanced PAM therapies.

2023-09-26·ACS omega

Expired Antifungal Drugs as Effective Corrosion Inhibitors for Carbon Steel in 1 M HCl Solution: Practical and Theoretical Approaches.

Article

作者: Motawea, Mohamed S ; Abdallah, Metwally ; Al-Bonayan, Ameena Mohsen ; Soliman, Kamal A ; Alfakeer, Majda ; Al-Juaid, Salih S ; Hawsawi, Hanaa ; Abd El Wanees, Salah

The anticorrosion potency of two expired antifungal drugs, namely, bifonazole (BIF) and terconazole (TER), for X65 carbon steel (X65CS) in a 1.0 M HCl solution was estimated using practical and computational measurements. The results of all methods applied showed that the percentage of anticorrosive efficacy (% AE) increased for expired BIF and TER and reduced at elevated temperatures. The % AE values of expired BIF and TER (375 mg L^-1) reached 92.08 and 94.19%, respectively, using polarization methods. The anticorrosion activities of the two expired drugs were interpreted based on their adsorption on the X65CS surface. The adsorption occurred according to the Langmuir isotherm model. The polarization results indicated that the expired drugs BIF and TER were mixed inhibitors. The impedance results showed a single capacitive loop, confirming that the charge transfer process controlled the corrosion of X65CS. Expired BIF and TER served as good pitting inhibitors by shifting the pitting potential to positive values. The thermodynamic functions of activation and adsorption were defined and explained. Density functional theory and Monte Carlo simulations were used to investigate the BIF and TER inhibitors. The theoretical parameters were consistent with the experimental results. The anticorrosion efficiencies determined using the various methods were in complete agreement.

1

项与特康唑相关的新闻（医药）

2006-03-22

·BioSpace

Perrigo Company Announces Approval For Terconazole Suppositories

ALLEGAN, Mich., March 21 /PRNewswire-FirstCall/ -- The Perrigo Company announced today that it has received approval from the U.S. Food and Drug Administration (FDA) to manufacture and market terconazole vaginal suppositories, 80 mg. The product is the AB-rated equivalent to Ortho-McNeil Pharmaceutical's Terazol(R) 3 Vaginal Suppositories, 80 mg, an anti-fungal medication indicated for the treatment of vaginal candida (yeast) infections. Perrigo is currently the only approved generic for this product. Shipments will begin immediately. According to NDC data, annual U.S. sales are approximately $8.5 million. The Perrigo Company is a leading global healthcare supplier and the world's largest manufacturer of over-the-counter (OTC) pharmaceutical and nutritional products for the store brand market. Store brand products are sold by food, drug, mass merchandise, dollar store and club store retailers under their own labels. The Company also develops, manufactures and markets prescription generic drugs, active pharmaceutical ingredients and consumer products, and operates manufacturing facilities in the United States, Israel, United Kingdom, Mexico and Germany. Visit Perrigo on the Internet ( ). Note: Certain statements in this press release are forward-looking statements within the meaning of Section 21E of the Securities Exchange Act of 1934, as amended, and are subject to the safe harbor created thereby. These statements relate to future events or the Company's future financial performance and involve known and unknown risks, uncertainties and other factors that may cause the actual results, levels of activity, performance or achievements of the Company or its industry to be materially different from those expressed or implied by any forward-looking statements. In some cases, forward-looking statements can be identified by terminology such as "may," "will," "could," "would," "should," "expect," "plan," "anticipate," "intend," "believe," "estimate," "predict," "potential" or other comparable terminology. Please see the "Cautionary Note Regarding Forward-Looking Statements" on pages 33 - 41 of the Company's Form 10-K for the year ended June 25, 2005, as well as the Company's subsequent filings with the Securities and Exchange Commission, for a discussion of certain important factors that relate to forward-looking statements contained in this press release. Although the Company believes that the expectations reflected in these forward-looking statements are reasonable, it can give no assurance that such expectations will prove to be correct. Unless otherwise required by applicable securities laws, the Company disclaims any intention or obligation to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise. Perrigo Company CONTACT: Ernest J. Schenk, Manager, Investor Relations and Communicationof Perrigo Company, +1-269-673-9212, E-mail: eschenk@perrigo.com Web site:

仿制药

100 项与特康唑相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D00888	特康唑	G01AG02	DB00251

研发状态

批准上市

10 条最早获批的记录,

登录

后查看更多信息

适应症	国家/地区	公司	日期
外阴阴道念珠菌病	美国	Taro Pharmaceuticals U.S.A., Inc.	2004-04-06

未上市

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
阴道疾病	临床前	美国	Curatek Pharmaceuticals, LLC	2015-06-01
感染性阴道炎	临床前	墨西哥	Janssen-Cilag SA	2007-12-01
阴道炎	临床前	墨西哥	Janssen-Cilag SA	2007-12-01

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02308007 (SMART GIVES, CTgov)	临床3期	感染性阴道炎	475	Terconazole (Terconazole Vaginal Gel)	築醖顧餘窪選壓夢齋壓(繭蓋製積鑰遞積鏇壓鹹) = 鬱夢夢獵鏇餘範餘齋壓膚鬱衊簾願製鏇製網淵 (憲範醖鹹構壓範鏇蓋鬱, 壓獵鏇醖範鏇遞艱窪餘 ~ 膚遞構築餘夢獵鏇積廠) 更多	-	2020-08-04
				Metronidazole (Metronidazole Vaginal Gel)	築醖顧餘窪選壓夢齋壓(繭蓋製積鑰遞積鏇壓鹹) = 壓醖構淵艱築壓壓築簾膚鬱衊簾願製鏇製網淵 (憲範醖鹹構壓範鏇蓋鬱, 醖鹹醖襯獵齋網艱顧遞 ~ 顧築壓範鑰夢願糧網齋) 更多
NCT02308046 (SMART GIVES, CTgov)	临床3期	感染性阴道炎	212	Terconazole (Terconazole Vaginal Gel)	齋鹽鏇鹽獵廠糧鹹膚構(鹽鏇糧鬱壓憲鏇獵範遞) = 顧齋繭鏇淵鬱繭醖遞襯醖簾衊構願獵獵餘簾鬱 (鏇網鬱築鏇遞鑰齋築糧, 糧淵窪鬱糧壓淵觸窪繭 ~ 衊願衊觸醖網蓋淵積積) 更多	-	2020-07-27
				Placebo (Gel Vehicle)	齋鹽鏇鹽獵廠糧鹹膚構(鹽鏇糧鬱壓憲鏇獵範遞) = 鹹膚築鑰積鏇網網淵醖醖簾衊構願獵獵餘簾鬱 (鏇網鬱築鏇遞鑰齋築糧, 繭獵選網衊顧繭積鹽醖 ~ 築憲製蓋醖選繭積鬱簾) 更多
NCT01867164 (CTgov)	临床3期	感染性阴道炎 \| 阴道炎	160	Terconazole+Fluocinolone Acetonide+Gynoclin V (Gynoclin V (Terconazole+Clindamycin+Fluocinolone Acetonide))	醖獵憲衊餘構鬱觸選蓋(憲顧鏇網淵獵簾繭鹹糧) = 醖衊網齋餘構遞積鹽醖選餘衊網憲醖選艱範壓 (鏇製鑰襯鏇獵選膚窪餘, 遞夢窪鏇膚齋襯衊繭遞 ~ 網構膚顧壓構築繭齋憲) 更多	-	2013-12-24
				Fluocinolone Acetonide+Nystatin+Metronidazole (Vagitrol V (Metronidazole+Fluocinolone Acetonide+Nystatin))	醖獵憲衊餘構鬱觸選蓋(憲顧鏇網淵獵簾繭鹹糧) = 憲築鑰蓋鏇糧選膚選鏇選餘衊網憲醖選艱範壓 (鏇製鑰襯鏇獵選膚窪餘, 醖鹹簾願網蓋鑰製壓艱 ~ 蓋遞夢衊積夢壓醖壓簾) 更多
NCT00803738 (CTgov)	N/A	外阴阴道念珠菌病	572	Terconazole (Terconazole Vaginal Suppositories, 80 mg - Perrigo)	憲襯範膚鹹繭衊繭選繭(膚構餘醖獵鹹獵夢衊鹹) = 願築糧鑰鏇膚齋構簾製遞觸鏇築齋壓願壓蓋蓋 (齋鏇淵鏇膚網繭襯齋網, 獵鬱網糧蓋鹹廠製醖蓋 ~ 鹽窪遞鹹淵繭衊繭遞鬱) 更多	-	2013-02-20
				Terazol 3 - Terconazole (Terazol 3 - Terconazole Vaginal Suppositories 80 mg)	憲襯範膚鹹繭衊繭選繭(膚構餘醖獵鹹獵夢衊鹹) = 廠積觸範膚憲構齋選壓遞觸鏇築齋壓願壓蓋蓋 (齋鏇淵鏇膚網繭襯齋網, 窪艱醖築鹹淵繭衊獵觸 ~ 鬱鹽餘淵壓築願構壓醖) 更多