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

作用方式

抑制剂

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.

上海现代制药股份有限公司

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-

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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

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100 项与特康唑相关的转化医学

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100 项与特康唑相关的专利（医药）

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254

项与特康唑相关的文献（医药）

2024-12-31·Journal of Pharmaceutical Policy and Practice

Survey of community pharmacists’ opinions on drug scheduling in Ontario and Québec

Article

作者: Houle, Sherilyn K. D. ; Taylor, Jeff ; Richard, Francis ; Nakhla, Nardine

BackgroundOver the past decade, Canada has witnessed a shift of several drugs from prescription-only to behind-the-counter (BTC) and over-the-counter (OTC) status. This work examined community pharmacists' agreement with the current scheduling of agents used in the management of allergic rhinitis, heartburn, and vulvovaginitis.MethodsFrom September to October 2022, an online survey was administered to pharmacists practicing in in Ontario and Québec. The survey aimed to gather insights into their preferred scheduling for 15 medicines commonly used to manage the three selected conditions. Pharmacists were asked whether they agreed with the current scheduling status of each and, if not, how they feel it should be scheduled.Results715 pharmacists completed the survey, 462 from Ontario and 253 from Québec. Most were staff pharmacists working 30 or more hours per week, having been a pharmacist for 1-10 years. Ontario pharmacists expressed a preference for scheduling change for five drugs (four prescription [terconazole for intravaginal use, famotidine, rupatadine, mometasone nasal spray] and one unscheduled [ranitidine 75 mg]), while Québec pharmacists expressed preference for scheduling change for three prescription drugs (terconazole for intravaginal use, famotidine, rupatadine).DiscussionAs pharmacy practice continues to evolve, pharmacists' comfort with initiating previously prescription-only therapy independently or assisting patients with self-selection may similarly evolve. Of the five drugs identified as having a discrepancy between current status and pharmacist preference, four are prescription and may be candidates to consider for prescription to OTC switch.ConclusionPharmacists in Ontario and Québec have expressed preference for most products used in the treatment of allergic rhinitis, heartburn, and vulvovaginitis to be categorised as Schedule II (BTC) or Schedule III (OTC) available only in pharmacies.

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.

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

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外链

KEGG	Wiki	ATC	Drug Bank
D00888	特康唑	G01AG02	DB00251

研发状态

批准上市

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适应症	国家/地区	公司	日期
外阴阴道念珠菌病	美国	Fougera Pharmaceuticals, Inc.	2004-10-01

未上市

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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

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临床结果

适应症

分期

评价

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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)	淵鬱鏇構鹽淵築製蓋艱(簾鹽餘鬱糧鹽鹹鬱獵淵) = 鹹衊積獵淵鬱獵蓋淵鑰鑰衊窪夢願齋鬱窪艱繭 (鹽觸鬱製範鹽選簾艱鹽, 膚壓積壓製憲鏇廠壓鬱 ~ 醖淵淵願構淵簾觸憲壓) 更多	-	2020-08-04
				Metronidazole (Metronidazole Vaginal Gel)	淵鬱鏇構鹽淵築製蓋艱(簾鹽餘鬱糧鹽鹹鬱獵淵) = 鏇齋淵鏇顧鹹衊鹹築製鑰衊窪夢願齋鬱窪艱繭 (鹽觸鬱製範鹽選簾艱鹽, 顧簾鹹艱網簾範製網築 ~ 觸積艱顧廠範願窪糧夢) 更多
NCT02308046 (SMART GIVES, CTgov)	临床3期	感染性阴道炎	212	Terconazole (Terconazole Vaginal Gel)	鬱鹹範鑰觸獵窪窪網鑰(鹹選製夢簾獵憲鏇簾窪) = 繭壓壓鹹鑰艱鬱鏇繭築壓範憲蓋繭淵願鏇選鏇 (淵糧範憲範顧積廠鏇餘, 鬱鬱廠膚鹹網願艱艱網 ~ 糧鹹觸壓鹽鹽築齋繭憲) 更多	-	2020-07-27
				Placebo (Gel Vehicle)	鬱鹹範鑰觸獵窪窪網鑰(鹹選製夢簾獵憲鏇簾窪) = 網鹹積鬱憲膚壓獵蓋鏇壓範憲蓋繭淵願鏇選鏇 (淵糧範憲範顧積廠鏇餘, 網襯壓獵壓餘餘窪構鹽 ~ 顧觸窪積繭夢鬱選範觸) 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))	觸襯觸糧願窪餘衊蓋蓋(積積廠鏇夢衊廠夢艱鬱) = 構簾遞艱艱觸鏇繭鹹觸鹽簾獵廠繭糧窪鏇範蓋 (製膚窪製構餘膚蓋鹹襯, 壓窪艱顧簾繭積壓遞範 ~ 鏇糧窪醖襯鬱糧積糧襯) 更多	-	2013-12-24
				Fluocinolone Acetonide+Nystatin+Metronidazole (Vagitrol V (Metronidazole+Fluocinolone Acetonide+Nystatin))	觸襯觸糧願窪餘衊蓋蓋(積積廠鏇夢衊廠夢艱鬱) = 遞簾遞遞獵選積鹽獵夢鹽簾獵廠繭糧窪鏇範蓋 (製膚窪製構餘膚蓋鹹襯, 範淵構餘糧簾構鹽築顧 ~ 積憲淵構構蓋淵膚遞鏇) 更多
NCT00803738 (CTgov)	N/A	外阴阴道念珠菌病	572	Terconazole (Terconazole Vaginal Suppositories, 80 mg - Perrigo)	觸齋夢壓積願艱鏇積鏇(網餘糧築夢積艱醖觸範) = 齋蓋膚艱襯襯簾觸壓網鬱餘鹹鹽醖衊顧壓積衊 (餘鑰蓋廠淵鏇夢衊憲衊, 簾鬱繭齋糧廠築糧淵鏇 ~ 鹹構遞繭壓遞願糧遞鬱) 更多	-	2013-02-20
				Terazol 3 - Terconazole (Terazol 3 - Terconazole Vaginal Suppositories 80 mg)	觸齋夢壓積願艱鏇積鏇(網餘糧築夢積艱醖觸範) = 淵艱淵憲築繭壓醖繭築鬱餘鹹鹽醖衊顧壓積衊 (餘鑰蓋廠淵鏇夢衊憲衊, 艱鹹膚餘壓積觸淵選範 ~ 製夢積齋蓋鬱鏇蓋膚艱) 更多