盐酸布替萘芬(Butenafine Hydrochloride) - 药物靶点：SQLE_在研适应症：传染性皮肤病，体癣，股癣_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

传染性皮肤病体癣股癣+ [2]

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

Hisamitsu Pharmaceutical Co., Inc.

Kaken Pharmaceutical Co., Ltd.

四川明欣药业有限责任公司

+ [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

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）

2024-01-01·European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

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

Article

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

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: Semple, Susan J ; Sykes, Matthew J ; Pisoni, Lily A ; Liu, Sida ; 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.

2023-10-01·Mycopathologia

Iranian National Survey on Tinea Capitis: Antifungal Susceptibility Profile, Epidemiological Characteristics, and Report of Two Strains with a Novel Mutation in SQLE Gene with Homology Modeling

Article

作者: Zaedi, Arezoo ; Kiasat, Neda ; Taghizadeh-Armaki, Mojtaba ; Shokohi, Tahereh ; Kharazi, Mahboobeh ; Babaei, Maryam ; Hedayati, Mohammad Taghi ; Ghasemi, Zeinab ; Khojasteh, Shaghayegh ; Keikha, Naser ; Aghili, Seyed Reza ; Abastabar, Mahdi ; Mohammadi, Rasoul ; Khodadadi, Hossein ; Reazaei-Matehkolaei, Ali ; Valadan, Reza ; Haghani, Iman ; Hesari, Kambiz Kamyab ; Azish, Maryam ; Zarrinfar, Hossein ; Javidnia, Javad

BACKGROUND:

The data on the epidemiological and antifungal susceptibility profile of tinea capitis (TC) in Iran has not been updated in recent decades. This report presents the Iranian epidemiological and drug susceptibility data regarding the distribution of dermatophytes species isolated by six national mycology centers for a period of one year (2020-2021).

MATERIAL AND METHODS:

A total of 2100 clinical samples from individuals suspeted to TC were subjected to mycological analysis of direct microscopy and culture. For definite species identification, the culture isolates were additionally subjected to PCR-RFLP and PCR-sequencing of the ITS ribosomal DNA (ITS-rDNA) region. Antifungal susceptibility profiles for eight common antifungal drugs were determined by CLSI M38-A3 guidelines. The SQLE gene was partially amplified and sequenced in two terbinafine-resistant and two susceptible T. mentagrophytes isolates to elucidate probable substitutions involved in resistance.

RESULTS:

TC (n = 94) was diagnosed in 75 children (79.8%) and 19 adults (20.2%) by direct microscopy and culture. Frequency of TC was significantly more among males (66 males = 70.2% vs 28 females = 29.8%). The prevalent age group affected was 5-9 years (39.36%). Thirty-two (34.04%) T. mentagrophytes, 27 (28.7%) T. tonsurans, 14 (14.9%) M. canis, 13 (13.8%) T. violaceum, 5 (5.32%) T. indotineae, 2 (2.1%) T. benhamiae, and 1 (1.1%) T. schoenleinii were identified as the causative agents. MIC values of isolates showed susceptibility to all antifungal agents, except for fluconazole and griseofulvin with GM MIC of 11.91 μg/ml and 2.01 μg/ml, respectively. Terbinafine exhibited more activity against isolates, with GM MIC 0.084 μg/ml followed by ketoconazole (0.100 μg/ml), econazole (0.107 μg/ml), itraconazole (0.133 μg/ml), butenafine (0.142 μg/ml), and miconazole (0.325 μg/ml). Two resistant T. mentagrophytes isolates harbored missense mutations in SQLE gene, corresponding to amino acid substitution F397L. Remarkably, one unique mutation, C1255T, in the SQLE sequence of two terbinafine-susceptible T. mentagrophytes strains leading to a change of leucine at the 419th position to phenylalanine (L419F) was detected.

CONCLUSIONS:

T. mentagrophytes, T. tonsurans, and M. canis remained the main agents of TC in Iran, however less known species such as T. indotinea and T. benhamiae are emerging as new ones. Terbinafine could still be the appropriate choice for the treatment of diverse forms of TC.

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
传染性皮肤病	中国	四川明欣药业有限责任公司	2002-01-14
体癣	日本	Hisamitsu Pharmaceutical Co., Inc.	1992-01-21
体癣	日本	Kaken Pharmaceutical Co., Ltd.	1992-01-21
股癣	日本	Kaken Pharmaceutical Co., Ltd.	1992-01-21
股癣	日本	Hisamitsu Pharmaceutical Co., Inc.	1992-01-21
足癣	日本	Hisamitsu Pharmaceutical Co., Inc.	1992-01-21
足癣	日本	Kaken Pharmaceutical Co., Ltd.	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3期	美国	Bayer AG	2013-06-24
光变态反应性皮炎	临床3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


NCT04532164 (CTgov)	临床3期	真菌病 \| 过敏性皮肤反应 \| 光变态反应性皮炎	137	Butenafine HCl 1% (BAY1896425) - Challenge Phase	窪選廠繭願構夢網膚構(淵夢製餘鬱淵鏇範廠繭) = 遞選繭艱簾齋遞壓糧網範廠遞鬱淵選繭願鏇淵 (網範壓簾糧夢膚膚積齋, 餘築繭夢鹽鏇憲糧糧淵 ~ 網遞鹹鹽鹽憲糧鏇艱襯) 更多	-	2020-11-16
NCT04531813 (CTgov)	临床3期	超敏反应 \| 皮肤疾病	32	Negative Control+Butenafine HCl 1% (BAY1896425)	築醖選襯艱鏇觸選構繭(顧憲窪獵獵艱構獵簾顧) = 繭夢製齋範網願選鏇範範醖遞壓鏇衊網遞遞獵 (膚淵製積壓廠膚憲蓋蓋, 鑰鹽壓觸獵願觸積餘鑰 ~ 觸鹹範醖簾襯膚壓壓糧) 更多	-	2020-09-25
NCT04531540 (CTgov)	临床3期	超敏反应 \| 中枢敏化 \| 皮肤疾病	225	Butenafine HCl 1% (BAY1896425)	範壓醖鏇繭餘膚膚糧鏇(製鹽繭網醖鏇願鬱廠觸) = 蓋壓觸網觸築觸醖製餘範構築積鏇餘獵繭淵壓 (餘鑰獵憲膚齋蓋壓願蓋, 選觸齋齋積獵糧範鹽醖 ~ 願顧齋願積遞鹽鹹鏇襯) 更多	-	2020-09-25
NCT04531527 (CTgov)	临床3期	光毒性皮炎 \| 超敏反应	32	Butenafine HCl 1% (BAY1896425)	鹹壓憲醖願顧鑰廠膚壓(糧繭選膚積蓋衊鏇觸鑰) = 醖鑰襯蓋製鏇淵願鏇網襯獵廠鹽網鬱鏇艱艱憲 (壓糧糧範壓衊選廠選觸, 廠簾製醖鏇膚衊廠廠齋 ~ 積網齋淵遞艱蓋選壓範) 更多	-	2020-09-21
NCT00835510 (CTgov)	临床1期	足癣	548	Butenafine cream 1% manufactured by Taro (Butenafine Cream 1% (Taro))	夢簾繭襯餘衊鏇遞憲網(顧選積憲鬱繭積鬱糧餘) = 夢襯衊膚淵網簾膚願廠鏇膚齋膚鬱衊窪獵艱遞 (餘願製憲襯鑰餘淵蓋蓋, 顧蓋餘醖獵夢醖襯觸積 ~ 廠齋積蓋築鹹範鹹廠夢) 更多	-	2009-10-06
NCT00835510 (CTgov)	临床1期	足癣	548	Lotrimin Ultra (butenafine) 1% (Lotrimin Ultra (Butenafine) 1%)	夢簾繭襯餘衊鏇遞憲網(顧選積憲鬱繭積鬱糧餘) = 餘膚獵糧構願獵衊鹽繭鏇膚齋膚鬱衊窪獵艱遞 (餘願製憲襯鑰餘淵蓋蓋, 積憲壓繭夢醖顧壓餘觸 ~ 繭願夢積糧遞簾構憲餘) 更多	-	2009-10-06