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

作用方式

抑制剂

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

过敏性皮肤反应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

Bayer Healthcare LLC

Kaken Pharmaceutical Co., Ltd.

Hisamitsu Pharmaceutical Co., Inc.

+ [2]

非在研机构

Bayer AGNORVIUM BIOSCIENCE

权益机构-

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/序列

分子式C23H28ClN

InChIKeyLJBSAUIFGPSHCN-UHFFFAOYSA-N

CAS号101827-46-7

关联

8

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-

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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257

项与盐酸布替萘芬相关的文献（医药）

2025-01-01·GENE

Evidence for high-risk pollutants and emerging microbial contaminants at two major bathing ghats of the river Ganga using high-resolution mass spectrometry and metagenomics

Article

作者: Pandey, Parul ; Kumar Tripathi, Anil ; Narain Singh, Durgesh ; Shankar Singh, Vijay

An efficient wastewater treatment plant is imperative to limit the entry of emerging pollutants (EPs) and emerging microbial contaminants (EMCs) in the river ecosystem. The detection of emerging EPs in aquatic environments is challenging due to complex sample preparation methods, and the need for sophisticated accurate analytical tools. In Varanasi (India), the river Ganga holds immense significance as a holy river but is consistently polluted with municipal (MWW) and hospital wastewater (HWW). We developed an efficient method for untargeted detection of EPs in the water samples using High-resolution mass spectrometry (HRMS), and identified 577 and 670 chemicals (or chemical components) in the water samples from two major bathing ghats, Assi Ghat (AG) and Dashashwamedh Ghat (DG), respectively. The presence of EPs of different categories viz chemicals from research labs, diagnostic labs, lifestyle and industrial chemicals, toxins, flavor and food additives indicated the unsafe disposal of MWW and HWW or inefficient wastewater treatment plants (WWTPs). Besides, shotgun metagenomic analysis depicted the presence of bacteria associated with MWW viz Cloacibacterium normanse, Sphaerotilus natans (sewage fungi), E. coli, and Prevotella. Also, the presence of human pathogens Arcobacter, Polynucleobacter, Pseudomonas, Klebsiella, Aeromonas, Acinetobacter, Vibrio, and Campylobacter suggests the discharge of HWW. EPs are linked to the development, and transmission of antimicrobial resistance (AMR). Occurrence of antibiotic resistance genes (ARGs), plasmid-borne β-lactamases, aminoglycoside transferases, and ARGs associated with integrons, transposons and plasmids viz mcr-3 gene that confer resistance to colistin, the last resort of antibiotics confirmed the presence of emerging microbial contaminants. Subsequent genome reconstruction studies showed the presence of uncultivable ARB and transmission of ARGs through horizontal gene transfer. This study can be used to monitor the health of aquatic bodies as well as the efficiency of WWTPs and raise an urgent need for efficient WWTPs to safeguard the river, Ganga.

2024-12-01·FUNDAMENTAL & CLINICAL PHARMACOLOGY

Nociceptive TRP channels function as molecular target for several antifungal drugs

Article

作者: Takahashi, Kenji ; Ohta, Toshio ; Okabe, Shota ; Hashimoto, Miho

Abstract:

Background/objectives:

Topically applied antifungal agents can induce adverse effects, such as pain and irritation. The transient receptor potential (TRP) channels—TRPA1 and TRPV1—mainly expressed in sensory neurons, act as sensors for detecting irritants. This study aims to evaluate the involvement of nociceptive channels in topical antifungal‐induced pain and irritation. We tested nine topical antifungals belonging five classes: isoconazole, econazole, miconazole, clotrimazole, and ketoconazole as imidazoles; liranaftate as a thiocarbamate; terbinafine as an allylamine; amorolfine as a morpholine; and butenafine as a benzylamine.

Methods:

Intracellular calcium concentrations ([Ca2+]i) and membrane currents in response to antifungals were measured to estimate channel activity using heterologously expressing cells and isolated mouse sensory neurons.

Results:

In mouse TRPA1‐expressing cells, all the tested drugs induced an increase in [Ca2+]i, which was abrogated or reduced by a TRPA1 blocker. Although many drugs evoked the TRPA1‐nonspecific [Ca2+]i response at high concentrations, responses to clotrimazole, ketoconazole, and liranaftate were TRPA1 specific and elicited current responses in TRPA1‐expressing cells. In mouse TRPV1‐expressing cells, clotrimazole and ketoconazole elicited [Ca2+]i and current responses. In mouse sensory neurons, liranaftate‐induced increase in [Ca2+]i was abrogated by a TRPA1 blocker and Trpa1 deletion. Responses to ketoconazole were inhibited by TRPA1 and TRPV1 blockers and by the genetic deletion of either channel.

Conclusion:

These results suggest that topical antifungal‐induced pain and irritation are attributable to the activation of nociceptive TRPA1 and/or TRPV1 channel/s. Consequently, caution should be exercised in the use of topical antifungals with symptoms of pain.

2024-11-25·JACS Au

CF₃-Cyclobutanes: Synthesis, Properties, and Evaluation as a Unique tert-Butyl Group Analogue

Article

作者: Trofymchuk, Serhii ; Panasiuk, Yaroslav ; Ahunovych, Volodymyr ; Kosach, Viktoriia ; Lesyk, Dmytro ; Shablykin, Oleh ; Bodenchuk, Iryna ; Boretskyi, Andrii ; Horbatok, Kateryna ; Borysko, Petro ; Razhyk, Bohdan ; Stanko, Oleh ; Mykhailiuk, Pavel K. ; Klipkov, Anton A. ; Kubyshkin, Vladimir ; Klymenko-Ulianov, Oleksii ; Bugera, Maksym ; Tarasenko, Karen ; Al-Maali, Galeb

Isosteric replacement of functional groups is an emerging strategy for optimizing bioactive molecules in drug discovery. tert-Butyl group is a particularly important moiety, yet its isosteric replacement with 1-trifluoromethyl-cyclobutyl group has been rather neglected. To enable the advance of this molecular fragment in drug discovery programs, we report the synthesis of over 30 small-molecule building blocks featuring the trifluoromethyl-cyclobutyl fragment, achieved by reacting sulfur tetrafluoride with cyclobutylcarboxylic acids on a gram-to-multigram scale. Furthermore, we characterized the structural properties of this group through X-ray analysis, studied its effect on acid-base transitions, and evaluated its Hammett parameters. Finally, we evaluated the replacement of tert-butyl with 1-trifluoromethyl-cyclobutyl in several bioactive compounds that represent commercial drugs and agrochemicals. Our findings indicate that while the trifluoromethyl-cyclobutyl group exhibited slightly larger steric size and moderately increased lipophilicity, it preserved the original mode of bioactivity in the examined cases and, in some cases, enhanced resistance to metabolic clearance.

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	Kaken Pharmaceutical Co., Ltd.	1992-01-21
足癣	日本	Hisamitsu Pharmaceutical Co., Inc.	1992-01-21
花斑癣	日本	Hisamitsu Pharmaceutical Co., Inc.	1992-01-21
花斑癣	日本	Kaken Pharmaceutical Co., Ltd.	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
瘙痒	临床3期	美国	Bayer AG	2013-09-09
光毒性皮炎	临床3期	美国	Bayer AG	2013-06-24
过敏性皮肤反应	临床3期	美国	Bayer AG	2013-06-10
光变态反应性皮炎	临床3期	美国	Bayer AG	2013-06-10
真菌病	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	艱壓鑰鹹範衊襯廠壓觸(淵繭願鏇憲壓窪鬱糧廠) = 積繭構艱襯襯範廠繭鏇鏇齋鏇製膚鹽廠鹹醖鹹 (衊艱觸蓋構醖糧範壓簾, 網構繭鹹蓋醖鹹蓋襯膚 ~ 醖鑰齋積獵繭顧鑰膚遞) 更多	-	2020-11-16
NCT04531540 (CTgov)	临床3期	瘙痒 \| 超敏反应	225	Butenafine HCl 1% (BAY1896425)	憲鏇鹹構艱壓窪糧齋襯 = 鹽餘遞鹹築願鬱壓顧製餘夢鹽鏇膚憲鏇顧蓋構 (顧構夢築窪鬱窪鬱餘廠, 廠憲夢範膚膚糧鏇鏇鏇 ~ 鑰鹹窪繭築網膚壓蓋鏇) 更多	-	2020-09-25
NCT04531527 (CTgov)	临床3期	光毒性皮炎	32	Butenafine HCl	襯艱鏇衊廠膚網顧獵願 = 遞艱齋憲獵鑰積獵襯壓淵齋選積蓋選餘蓋鑰範 (蓋選壓齋鬱膚範艱網壓, 選餘構簾膚窪範艱製壓 ~ 積鬱夢鑰憲衊簾蓋窪觸) 更多	-	2020-09-21
NCT00835510 (CTgov)	临床1期	足癣	548	Butenafine cream 1% manufactured by Taro (Butenafine Cream 1% (Taro))	網範鬱廠淵遞衊範壓壓 = 鏇簾獵製遞願齋廠觸壓鏇淵獵襯鹹齋淵獵繭繭 (網廠鑰憲夢繭壓鏇鑰鏇, 窪餘壓製襯憲築膚簾淵 ~ 積構窪構鏇觸願繭顧繭) 更多	-	2009-10-06
NCT00835510 (CTgov)	临床1期	足癣	548	Lotrimin Ultra (butenafine) 1% (Lotrimin Ultra (Butenafine) 1%)	網範鬱廠淵遞衊範壓壓 = 餘齋獵鹹淵築範積淵繭鏇淵獵襯鹹齋淵獵繭繭 (網廠鑰憲夢繭壓鏇鑰鏇, 襯網鹹廠糧衊醖構網夢 ~ 築艱選餘鬱廠蓋夢淵範) 更多	-	2009-10-06