盐酸布替萘芬(Butenafine Hydrochloride) - 药物靶点：SQLE_在研适应症：真菌病，传染性皮肤病，癣_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(4-tert-Butyl-benzyl)-methyl-naphthalen-1-ylmethyl-amine、(4-tert-butylphenyl)-N-methyl-N-(naphthalen-1-ylmethyl)methanamine、4-tert-butylbenzyl(methyl)(1-naphthalenemethyl)amine

+ [30]

靶点

SQLE

作用机制

SQLE抑制剂(角鲨烯单加氧酶抑制剂)

治疗领域

感染皮肤和肌肉骨骼疾病

在研适应症

真菌病传染性皮肤病癣+ [4]

非在研适应症

光变态反应性皮炎光毒性皮炎

原研机构

Kaken Pharmaceutical Co., Ltd.

在研机构

Kaken Pharmaceutical Co., Ltd.Bayer Healthcare LLC

Hisamitsu Pharmaceutical Co., Inc.

+ [2]

非在研机构

Bayer AGMylan Pharmaceuticals, Inc.

最高研发阶段批准上市

首次获批日期

日本 (1992-01-21),

体癣股癣足癣+ [1]

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C23H28ClN

InChIKeyLJBSAUIFGPSHCN-UHFFFAOYSA-N

CAS号101827-46-7

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关联

9

项与盐酸布替萘芬相关的临床试验

NCT03999437 / Unknown status临床2期

EFFICACY AND SAFETY OF A SINGLE-APPLICATION TREATMENT USING TERBINAFINE HYDROCHLORIDE (1%) TOPICAL LIQUID SOLUTION VERSUS A SINGLE-APPLICATION TREATMENT USING BUTENAFINE HYDROCHLORIDE (1%) TOPICAL LIQUID SOLUTION FOR THE TREATMENT OF TINEA PEDIS: A RANDOMIZED, DOUBLE-BLIND, PLACEBO-CONTROLLED TRIAL

Tinea pedis or athlete's foot is the most common fungal infection worldwide, caused by infection of the feet with dermatophytes such as Trichophyton rubrum, Trichophyton interdigitale (formerly Trichophyton mentagrophytes), and Epidermophyton floccosum. Diagnosis of tinea pedia involves clinical symptoms as well as microscopic examination. Topical therapies are usually applied once or twice daily for as long as 4 weeks, posing a challenge to compliance. The current study aims to test a formulation of the single-dose 1% terbinafine hydrochloride, as well as a single-dose 1% butenafine hydrochloride, versus a vehicle control in adult Filipino patients with athlete's foot. This study will benefit the Filipino community by helping us determine which anti-fungal cream is most effective for athlete's foot.

开始日期2019-01-02

申办/合作机构

United Laboratories, Inc.

NCT04531540 / Completed临床3期

HT201321- Repeated Insult Patch Test With Modified Challenge

In this study researcher want to learn more about possible skin reactions such after repeated application of an antifungal cream containing Trolamine. They are especially interested in skin irritations or allergic skin reactions. The study plans to enroll about 225 female or male participants with the age 18 - 79 years. The antifungal test cream will be applied on the back between the shoulder blades of the participants and covered by a special dressing patch. This will be repeated 3 times a week for the first 3 weeks of this study applying the cream on the same area of the back. At each visit the skin will be investigated for redness, dryness and other reactions. After a rest period of two weeks the test cream will be applied on the same skin area as before and on a second new skin area nearby. After 2 and 4 days the two skin areas will again be investigated for redness, dryness and other reactions.

开始日期2013-09-09

申办/合作机构

Bayer AG

NCT04531527 / Completed临床3期

HT201308- Human Phototoxicity Test

In this study researchers want to gather information about the potential of Antifungal Cream V61-044 containing Trolamine to produce a phototoxic reaction on the skin. A phototoxic reaction is an irritant reaction of the skin to ultra violet light. In order to find this out the study drug will be applied to the skin of healthy human subjects. By using a solar simulator to generate a UV spectrum similar to that of sunlight the potential of the study drug to produce a superficial reddening of the skin will be measured.

开始日期2013-06-24

申办/合作机构

Bayer AG

100 项与盐酸布替萘芬相关的临床结果

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100 项与盐酸布替萘芬相关的转化医学

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100 项与盐酸布替萘芬相关的专利（医药）

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108

项与盐酸布替萘芬相关的文献（医药）

2024-03-01·European review for medical and pharmacological sciences

In vitro antifungal susceptibility of the dermatophytes: a single center study from Eastern Black Sea Region of Turkey.

Article

作者: Direkel, Ş ; Oğuz, I D ; Akşan, B ; Aksoy, S ; Kulakli, S

OBJECTIVEA large number of patients applying to the dermatology clinics are affected by fungal diseases, and a significant portion of which are superficial fungal infections. Dermatophyte infections are a notable public health concern and frequently encountered in clinical practice. Dermatophytosis not only compromises the quality of life but also predisposes individuals to various comorbidities due to its role as a gateway for secondary bacterial agents. This study aims to determine the species distribution of dermatophytes prevalent and assess their susceptibility to antifungal drugs.PATIENTS AND METHODSSkin, nail, and hair samples were obtained from patients with a clinical diagnosis of dermatophytosis. Samples were all cultured to isolate and identify the species. In vitro liquid microdilution tests were conducted to assess the susceptibility of the isolated strains against terbinafine, fluconazole, griseofulvin, and butenafine.RESULTSA total of 353 samples were obtained from the hair, skin, and nail lesions of 326 patients. Dermatophyte was isolated in 71 of the samples (20.1%). The cultured dermatophyte subtypes included Trichophyton rubrum (13.8% in 49 samples), Microsporum audouini (5.7% in 20 samples), and Trichophyton mentagrophytes (0.6% in 2 samples). Antifungal susceptibility testing revealed that terbinafine was the most effective antifungal drug against all dermatophyte species, while fluconazole exhibited the highest resistance.CONCLUSIONSThe most common dermatophytosis agent in our region is T. rubrum. The least antifungal resistance was found against terbinafine. Conducting antifungal susceptibility tests is crucial for selecting effective treatment regimens and early detection of resistance development.

2024-01-01·European Journal of Pharmaceutical Sciences

Novel nanomicelle butenafine formulation for ocular drug delivery against fungal keratitis: In Vitro and In Vivo study

Article

作者: Liang, Zhen ; Zhang, Zhen ; Lu, Ping ; Zhang, Junjie ; Zhou, Tianyang ; Song, Fei ; Yang, Jingjing ; Li, Jingguo

Fungal keratitis (FK) is a serious infectious corneal disease that leads to blindness. Butenafine (BTF) is an allylamine drug with high antifungal activity, but its poor water solubility and low bioavailability limit its clinical application in ophthalmology. To increase its aqueous solubility and corneal permeability, butenafine was encapsulated in d-ɑ-tocopheryl polyethylene glycol succinate (TPGS) polymeric nanomicelles to improve the bioavailability of the drug for the treatment of FK. Butenafine was successfully fabricated into nanomicelles with a high EE of 96.34 ± 1.65 % and DL of 6.71 ± 0.099 %. The BTF-NM showed an average particle size of 13.12 ± 0.24 nm, a zeta potential of -0.56 ± 0.44 mV and a narrow PDI of 0.12 ± 0.02 with a nearly spherical shape. The characterization results of FTIR, XRD and DSC indicated that BTF was encapsulated in the TPGS nanomicelles. The BTF-NM formulation also showed high storage stability, and the in vitro drug release study showed typical biphasic-release characteristics. In addition, the BTF-NM formulation displayed good cellular tolerance and excellent ocular tolerance in rabbits. Significantly elevated in vitro antifungal activity was also observed in the BTF-NM formulation, and remarkable improvements regarding in vivo corneal permeation were observed compared with the BTF suspension formulation. Finally, the in vivo antifungal activity studies indicated that the BTF-NM formulation had a good therapeutic effect on FK and had similar efficacy to that of commercial natamycin suspension eye drops. These results suggest that the BTF-NM ophthalmic formulation could be a promising ocular drug delivery system for the treatment of FK.

2023-12-08·ACS Infectious Diseases

Combined Structure- and Ligand-Based Approach for the Identification of Inhibitors of AcrAB-TolC in Escherichia coli

Article

作者: Liu, Sida ; Semple, Susan J ; Pisoni, Lily A ; Sykes, Matthew J ; Venter, Henrietta

The inhibition of efflux pumps is a promising approach to combating multidrug-resistant bacteria. We have developed a combined structure- and ligand-based model, using OpenEye software, for the identification of inhibitors of AcrB, the inner membrane protein component of the AcrAB-TolC efflux pump in Escherichia coli. From a database of 1391 FDA-approved drugs, 23 compounds were selected to test for efflux inhibition in E. coli. Seven compounds, including ivacaftor (25), butenafine (19), naftifine (27), pimozide (30), thioridazine (35), trifluoperazine (37), and meloxicam (26), enhanced the activity of at least one antimicrobial substrate and inhibited the efflux pump-mediated removal of the substrate Nile Red from cells. Ivacaftor (25) inhibited efflux dose dependently, had no effect on an E. coli strain with genomic deletion of the gene encoding AcrB, and did not damage the bacterial outer membrane. In the presence of a sub-minimum inhibitory concentration (MIC) of the outer membrane permeabilizer colistin, ivacaftor at 1 μg/mL reduced the MICs of erythromycin and minocycline by 4- to 8-fold. The identification of seven potential AcrB inhibitors shows the merits of a combined structure- and ligand-based approach to virtual screening.

100 项与盐酸布替萘芬相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01093	盐酸布替萘芬	D01AE23	DB01091

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
真菌病	阿根廷	Kaken Pharmaceutical Co., Ltd.	2006-12-07
真菌病	智利	Kaken Pharmaceutical Co., Ltd.	2006-12-07
传染性皮肤病	中国	四川明欣药业有限责任公司	2002-01-14
癣	加拿大	-	1997-05-31
体癣	日本	Kaken Pharmaceutical Co., Ltd.	1992-01-21
体癣	日本	Hisamitsu Pharmaceutical Co., Inc.	1992-01-21
股癣	日本	Hisamitsu Pharmaceutical Co., Inc.	1992-01-21
股癣	日本	Kaken Pharmaceutical Co., Ltd.	1992-01-21
足癣	日本	Kaken Pharmaceutical Co., Ltd.	1992-01-21
足癣	日本	Hisamitsu Pharmaceutical Co., Inc.	1992-01-21
花斑癣	日本	Kaken Pharmaceutical Co., Ltd.	1992-01-21
花斑癣	日本	Hisamitsu Pharmaceutical Co., Inc.	1992-01-21

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
光毒性皮炎	临床2期	美国	Bayer AG	2013-06-24
光变态反应性皮炎	临床2期	美国	Bayer AG	2013-06-10

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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


NCT04531813 (CTgov)	临床3期	皮肤疾病 \| 超敏反应	32	Negative Control+Butenafine HCl 1% (BAY1896425)	醖選醖鏇襯膚簾顧糧積(築鬱窪鏇構獵齋鏇繭網) = 壓鹹顧齋齋憲顧簾築範鑰顧糧廠繭齋夢淵齋鏇 (繭簾襯鏇積夢齋構選簾, 艱淵獵遞廠蓋願醖醖襯 ~ 繭壓夢艱鏇壓襯襯衊窪) 更多	-	2020-09-25
NCT04531527 (CTgov)	临床3期	超敏反应 \| 光毒性皮炎	32	Butenafine HCl 1% (BAY1896425)	艱廠網遞選醖觸選構繭(選餘餘憲壓廠簾繭鏇繭) = 齋夢簾膚網廠範蓋網範築選製鬱繭糧觸壓襯願 (築鹹糧鹹夢襯願簾衊選, 鹽鏇齋壓鏇選鏇艱鹽鹹 ~ 艱鹹醖觸製觸積糧築鬱) 更多	-	2020-09-21
NCT04532164 (CTgov)	临床3期	过敏性皮肤反应 \| 光变态反应性皮炎 \| 真菌病	137	Butenafine HCl 1% (BAY1896425) - Challenge Phase	鹹網鬱鏇遞夢窪範顧鬱(壓醖壓鹽廠獵繭願簾製) = 鑰襯艱選襯鹽鏇鏇襯鹽衊鏇窪壓選廠鬱遞糧夢 (衊膚壓憲鏇餘齋顧鏇遞, 艱築襯觸顧網築願艱淵 ~ 鬱簾願憲積鹹壓範積廠) 更多	-	2020-11-16
NCT00835510 (CTgov)	临床1期	足癣	548	Butenafine cream 1% manufactured by Taro (Butenafine Cream 1% (Taro))	製襯範鬱壓願廠鑰製積(獵觸窪範鹹憲壓構蓋鹽) = 鹽簾願積鏇窪製鬱築鑰蓋鏇齋鑰範淵糧糧範齋 (鹽鏇襯糧觸積鑰膚廠遞, 糧構夢簾築遞糧鹽鹽鹽 ~ 顧觸獵構顧壓鹽窪壓蓋) 更多	-	2009-10-06
NCT00835510 (CTgov)	临床1期	足癣	548	Lotrimin Ultra (butenafine) 1% (Lotrimin Ultra (Butenafine) 1%)	製襯範鬱壓願廠鑰製積(獵觸窪範鹹憲壓構蓋鹽) = 觸築願糧蓋襯築淵獵淵蓋鏇齋鑰範淵糧糧範齋 (鹽鏇襯糧觸積鑰膚廠遞, 壓簾顧醖鬱壓餘構膚衊 ~ 鏇網獵壓糧襯範襯獵壓) 更多	-	2009-10-06
NCT04531540 (CTgov)	临床3期	皮肤疾病 \| 中枢敏化 \| 超敏反应	225	Butenafine HCl 1% (BAY1896425)	顧築遞壓艱蓋鹽鑰淵鏇(範膚簾蓋選範襯窪鏇鹹) = 鹽淵壓繭鏇觸築淵廠鏇蓋齋憲醖鬱遞艱鏇築鹽 (繭蓋簾構鬱鬱範簾淵築, 鹹淵簾遞艱鬱窪襯襯廠 ~ 獵鏇鏇膚餘齋願壓膚鑰) 更多	-	2020-09-25