更新于：2024-12-12
Terbinafine
特比萘芬
更新于：2024-12-12
概要
基本信息
简介特比萘芬是一种小分子药物，通过阻断 SQLE 发挥其抑制作用，SQLE 是真菌细胞膜的主要成分麦角甾醇生物合成中的关键酶。由于这种抑制作用，特比萘芬攻击真菌细胞膜，导致真菌过早死亡。特比萘芬已在临床领域用于治疗一系列真菌感染，包括甲癣和股癣。该药由GSK研发，并于1998年4月获得FDA批准。 |
药物类型 小分子化药 |
别名 (E)-N-(6,6-Dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalene methanamine、(E)-N-(6,6-Dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalenemethylamine、Terbinafine (USAN/INN) + [5] |
靶点 |
作用机制 SQLE抑制剂(角鲨烯单加氧酶抑制剂) |
在研适应症 |
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)无进展 |
特殊审评- |
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结构
分子式C21H25N |
InChIKeyDOMXUEMWDBAQBQ-WEVVVXLNSA-N |
CAS号91161-71-6 |
关联
57
项与 特比萘芬 相关的临床试验Clinical and Laboratory Evaluation of Antifungal Resistance in Tinea Capitis
Randomised control trial to study the effectiveness of Tablet Fluconazole, Capsule Itraconazole and Tablet Terbinafine in Superficial Dermatophytosis - NIL
Formulation design and evaluation of the effect of hyaluronic acid hydrogel loaded with terbinafine lipid nanostructures in the treatment of patients with onychomycosis
100 项与 特比萘芬 相关的临床结果
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100 项与 特比萘芬 相关的转化医学
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100 项与 特比萘芬 相关的专利（医药）
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3,082
项与 特比萘芬 相关的文献（医药）2025-01-01DIAGNOSTIC MICROBIOLOGY AND INFECTIOUS DISEASE
In vitro and silico activity of piperlongumine against azole-susceptible/resistant Aspergillus fumigatus and terbinafine-susceptible/resistant Trichophyton species
Article
作者: Shokohi, Tahereh ; Otaševi´c, Suzana ; Hedayati, Mohammad Taghi ; Rashidi, Mohsen ; Abastabar, Mahdi ; Haghani, Iman ; Azadeh, Hossein ; Sillanpää, Mika ; Aghili, Seyed Reza ; Badali, Hamid ; Hashemi, Seyedeh Mahdieh ; Nosratabadi, Mohsen ; Hoseinnejad, Akbar ; Teymoori, Ali ; Yahyazadeh, Zahra ; Otasevic, Suzana ; Ebrahimi-Barough, Robab
In recent years, the widespread emergence of drug resistance in yeasts and filamentous fungi to existing antifungal armamentariums has become a severe threat to global health. There is also concern regarding increased rates of azole resistance in Aspergillus fumigatus and Terbinafine resistance in Trichophyton species. To overcome this concern of resistance to regular therapies, new antifungal drugs with novel and effective mechanisms are crucially needed. Herbal remedies may be promising strategies for the treatment of resistant infections. We aimed to investigate the in vitro and silico activity of piperlongumine against clinical azole susceptible/resistant A. fumigatus and terbinafine-susceptible/resistant Trichophyton species. In the current study, piperlongumine demonstrated potent antifungal activity, with minimum inhibitory concentrations (MICs) ranging from 0.016-4 μg/mL against Trichophyton isolates and 0.25-2 μg/mL for A. fumigatus isolates. Additionally, molecular docking studies indicated that piperlongumine has a strong binding affinity to the active sites of squalene epoxidase and sterol 14-alpha demethylase. However, further studies are warranted to correlate these findings with clinical outcomes and provide the basis for further investigations to pave the way for developing novel antifungal agents.
2024-12-01Medical Mycology Case Reports
Dermatophytosis caused by Trichophyton benhamiae in a sea lion. First report
Article
作者: López, Ronar ; Godoy-Martínez, Patricio ; Bown, Viviana ; Thomson, Pamela ; Silva, Víctor
Fungal infections in marine animals, particularly pinnipeds, have seen a notable increase, often linked to compromised immune systems in captive environments. Trichophyton species, while common in terrestrial mammals, have sporadically caused dermatophytosis in pinnipeds. A South American sea lion (Otaria byronia) presented with Trichophyton benhamiae infection, marking the first such case in this species. Effective treatment combined oral terbinafine with topical ozonized oil, supported by silymarin for liver protection. Accurate fungal identification and sensitivity testing were key to the successful management and recovery of the patient.
2024-12-01MYCOPATHOLOGIA
Dermatophytes: Update on Clinical Epidemiology and Treatment
Review
作者: Paglietti, Bianca ; Stevanovic, Goran ; Milosevic, Branko ; Stjepanovic, Mihailo ; Barac, Aleksandra ; Krajisnik, Snjezana
Dermatophytes represent the largest and most common group of fungal infections, impacting 25% of the global population. Among them, Trichophyton rubrum has emerged as the predominant species, responsible for a range of conditions such as tinea corporis, tinea pedis, onychomycosis, tinea cruris, and tinea manuum. Although dermatophyte incidence varies geographically, there is a noticeable rise in cases caused by T. indotineae, a strain that exhibits resistance to terbinafine. In the past decade zoophilic dermatophyte T. mentagophytes genotype VII (now known as T. interdigitale) gains a growing importance, due to its increasing frequency, the severity of the clinical manifestation and mode of transmission. Tinea infections present with various clinical symptoms and can affect individuals of all ages, from tinea pedis in adults to tinea capitis in children. Among adults globally, tinea unguium (onychomycosis) is the most common form of dermatophytosis, affecting 5.5% of the general population. Tinea unguium is more frequently seen in developed countries, while tinea capitis is more common in developing nations. The COVID-19 pandemic has led to an increase in cases of tinea faciei, likely due to prolonged mask-wearing. Terbinafine remains the preferred treatment for dermatophyte infections worldwide due to its potent fungicidal properties, minimal risk of drug interactions, and fewer side effects compared to other oral antifungals. Itraconazole and terbinafine appear to be equally effective and safe for treating tinea cruris and tinea corporis. However, the rising resistance of dermatophytes to these antifungal drugs, along with frequent recurrences of dermatophytosis in certain regions, is becoming a significant public health concern.
100 项与 特比萘芬 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 股癣 | 美国 | 2006-07-24 | |
| 糠疹 | 美国 | 1998-04-29 | |
| 癣 | 美国 | 1998-04-29 | |
| 体癣 | 美国 | 1998-04-29 | |
| 足癣 | 美国 | 1998-04-29 | |
| 花斑癣 | 美国 | 1998-04-29 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 甲癣 | 临床3期 | 美国 | 2006-12-01 | |
| 甲癣 | 临床3期 | 加拿大 | 2006-12-01 | |
| 真菌病 | 临床1期 | - | 2011-02-24 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | - | 醖網選淵鹹壓壓鏇壓願(觸觸壓憲鹹簾衊窪獵網) = 網鏇醖積願膚鑰糧鹽簾 淵鏇製顧鏇選襯構憲窪 (廠淵積觸膚築繭餘顧遞 ) | - | 2023-10-11 | |||
临床2期 | 30 | 餘餘膚壓襯鏇製範網壓(襯鹽廠鏇衊襯選襯繭鬱) = 醖餘網鏇壓鏇壓襯夢蓋 繭遞艱膚顧網鏇獵簾鑰 (夢簾淵鏇築衊壓醖簾膚, 網獵築製夢鏇製網簾襯 ~ 齋顧衊範遞鹹範獵廠鏇) 更多 | - | 2019-09-24 | |||
临床3期 | 290 | (Terbinafine) | 蓋築獵鑰積鑰積觸艱衊(簾製獵齋構網積鬱艱網) = 壓糧顧構築窪範願鹹顧 窪觸繭繭繭夢鹽鏇廠積 (網簾鑰襯範餘鬱築蓋壓, 製廠餘簾鏇憲鹽艱壓鏇 ~ 繭艱餘餘遞夢窪夢夢膚) 更多 | - | 2013-12-27 | ||
(Placebo) | 蓋築獵鑰積鑰積觸艱衊(簾製獵齋構網積鬱艱網) = 鬱顧餘齋鏇構壓積顧觸 窪觸繭繭繭夢鹽鏇廠積 (網簾鑰襯範餘鬱築蓋壓, 鏇願齋夢製醖衊膚鑰艱 ~ 鬱鑰網膚壓淵齋構觸艱) 更多 | ||||||
临床3期 | 518 | (Terbinafine 24 w) | 鹹艱繭遞憲鏇構齋簾憲(觸積蓋鏇積壓鹹構構網) = 鏇襯廠構範鑰鹽壓鹽顧 衊淵範壓遞糧膚鏇繭鹹 (窪製鏇繭觸夢鏇淵窪範, 鑰鹹構糧壓構襯觸願網 ~ 蓋蓋獵顧蓋醖憲構膚壓) 更多 | - | 2011-04-20 | ||
placebo (Vehicle 24 w) | 鹹艱繭遞憲鏇構齋簾憲(觸積蓋鏇積壓鹹構構網) = 衊築憲憲憲觸觸簾積齋 衊淵範壓遞糧膚鏇繭鹹 (窪製鏇繭觸夢鏇淵窪範, 獵繭夢窪構齋獵糧簾窪 ~ 醖鏇膚構範壓觸鬱蓋窪) 更多 | ||||||
临床3期 | 1,029 | (Terbinafine) | 齋鑰繭製壓衊願製觸鬱(鑰襯積願鹹醖鏇鬱夢製) = 顧繭夢積淵壓鬱襯窪壓 鏇願壓網醖夢淵製鬱齋 (淵鬱鹽襯鹹憲鏇遞鏇顧, 醖鹽蓋餘鹽夢獵顧衊積 ~ 顧憲膚醖鏇齋壓蓋鑰衊) 更多 | - | 2011-04-20 | ||
(Amorolfine) | 齋鑰繭製壓衊願製觸鬱(鑰襯積願鹹醖鏇鬱夢製) = 醖鏇繭願積範願淵製獵 鏇願壓網醖夢淵製鬱齋 (淵鬱鹽襯鹹憲鏇遞鏇顧, 願衊膚範範鏇遞網鬱壓 ~ 淵製築鬱鹽構鹽窪繭醖) 更多 | ||||||
临床3期 | 526 | (Terbinafine 24 Weeks) | 壓積範膚蓋繭積餘製淵(顧網願鏇築艱鑰鏇鬱窪) = 簾範築選簾淵鑰壓網簾 觸蓋簾積艱製願餘齋獵 (窪遞糧選膚醖鏇醖窪鑰, 艱範窪艱廠壓齋鹹醖鑰 ~ 積選淵顧顧餘蓋糧蓋餘) 更多 | - | 2011-04-19 | ||
placebo (Vehicle 24 Weeks) | 壓積範膚蓋繭積餘製淵(顧網願鏇築艱鑰鏇鬱窪) = 範鹹選獵築選鑰餘膚鏇 觸蓋簾積艱製願餘齋獵 (窪遞糧選膚醖鏇醖窪鑰, 範繭鬱網壓夢窪觸廠網 ~ 製糧壓艱壓願壓衊鹹觸) 更多 |
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