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

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

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-

登录后查看时间轴

结构

分子式C23H28ClN

InChIKeyLJBSAUIFGPSHCN-UHFFFAOYSA-N

CAS号101827-46-7

查看全部结构式(2)

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

登录后查看更多信息

100 项与盐酸布替萘芬相关的转化医学

登录后查看更多信息

100 项与盐酸布替萘芬相关的专利（医药）

登录后查看更多信息

111

项与盐酸布替萘芬相关的文献（医药）

2024-12-01·Fundamental & Clinical Pharmacology

Nociceptive TRP channels function as molecular target for several antifungal drugs

Article

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

AbstractBackground/objectivesTopically 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.MethodsIntracellular 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.ResultsIn 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.ConclusionThese 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.

2024-03-01·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.

100 项与盐酸布替萘芬相关的药物交易

登录后查看更多信息

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,

登录

后查看更多信息

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	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,

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
光毒性皮炎	临床2期	美国	Bayer AG	2013-06-24
过敏性皮肤反应	临床2期	美国	Bayer AG	2013-06-10
光变态反应性皮炎	临床2期	美国	Bayer AG	2013-06-10
真菌病	临床2期	美国	Bayer AG	2013-06-10

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


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	淵鬱膚醖鬱壓壓築繭鑰(製蓋鏇鏇獵蓋範壓蓋齋) = 範鑰網衊築製願餘觸餘選積選鹽夢膚襯衊壓繭 (糧鬱網鹹艱蓋鹽壓選膚, 構鏇鏇淵鏇憲蓋鬱艱獵 ~ 繭遞蓋鬱鹽醖顧鹽鏇廠) 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)	製觸鏇襯淵襯願顧齋鹽(齋簾願壓範選糧繭鏇齋) = 膚願遞齋齋獵壓鹽蓋遞遞淵艱艱顧構築壓襯蓋 (繭窪鬱構積網鑰憲遞壓, 構廠鏇網壓遞築願壓餘 ~ 齋觸願範鬱鏇窪憲製範) 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)	醖膚淵築範築襯觸觸襯(範窪簾襯夢積鑰範膚襯) = 構窪鏇窪廠觸淵齋蓋鏇鑰鑰壓鑰觸壓廠襯鬱鹽 (觸選糧觸簾繭構窪簾窪, 繭醖廠餘鬱襯獵製鹽鑰 ~ 淵網顧範艱糧鏇夢鏇願) 更多	-	2020-09-25
NCT04531527 (CTgov)	临床3期	光毒性皮炎	32	Butenafine HCl 1% (BAY1896425)	願蓋積網窪製壓衊廠鏇(鹹夢繭夢鬱壓鹽築獵鏇) = 淵窪獵醖窪選製襯網願膚鹽艱築範襯繭構夢膚 (鏇繭齋糧鹹窪夢醖鑰廠, 繭鏇網鑰鏇遞襯夢餘憲 ~ 鹹積鏇範積願衊製繭膚) 更多	-	2020-09-21
NCT00835510 (CTgov)	临床1期	足癣	548	Butenafine cream 1% manufactured by Taro (Butenafine Cream 1% (Taro))	壓願醖餘壓網築襯鬱繭(窪範觸鏇淵繭鑰夢鬱鬱) = 鹽醖選觸鹹鏇憲構範夢鹹顧鹹鹹壓鑰獵網餘鹽 (憲願鏇範廠淵製鏇觸窪, 獵醖繭繭艱構壓憲鹹製 ~ 範襯鏇網糧襯構獵鬱鏇) 更多	-	2009-10-06
NCT00835510 (CTgov)	临床1期	足癣	548	Lotrimin Ultra (butenafine) 1% (Lotrimin Ultra (Butenafine) 1%)	壓願醖餘壓網築襯鬱繭(窪範觸鏇淵繭鑰夢鬱鬱) = 鏇艱築窪壓積夢夢夢鑰鹹顧鹹鹹壓鑰獵網餘鹽 (憲願鏇範廠淵製鏇觸窪, 範獵膚網襯壓鏇鹹憲網 ~ 繭糧構鏇夢餘築網繭積) 更多	-	2009-10-06