更新于：2024-11-13
Terbinafine
特比萘芬
更新于：2024-11-13
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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3,122
项与 特比萘芬 相关的文献（医药）2024-12-01GUT
Targeting squalene epoxidase restores anti-PD-1 efficacy in metabolic dysfunction-associated steatohepatitis-induced hepatocellular carcinoma
Article
作者: Wen, Jun ; Pan, Yasi ; Kang, Xing ; Wong, Chi Chun ; Liu, Dabin ; Ji, Fenfen ; Cheung, Alvin Ho-Kwan ; Zhou, Yunfei ; Zhang, Xiang ; Yu, Jun ; Liu, Yali ; Zhang, Yating
Objective:
Squalene epoxidase (SQLE) promotes metabolic dysfunction-associated steatohepatitis-associated hepatocellular carcinoma (MASH-HCC), but its role in modulating the tumour immune microenvironment in MASH-HCC remains unclear.
Design:
We established hepatocyte-specificSqletransgenic (tg) and knockout mice, which were subjected to a choline-deficient high-fat diet plus diethylnitrosamine to induce MASH-HCC. SQLE function was also determined in orthotopic and humanised mice. Immune landscape alterations of MASH-HCC mediated by SQLE were profiled by single-cell RNA sequencing and flow cytometry.
Results:
Hepatocyte-specificSqletg mice exhibited a marked increase in MASH-HCC burden compared with wild-type littermates, together with decreased tumour-infiltrating functional IFN-γ+and Granzyme B+CD8+T cells while enriching Arg-1+myeloid-derived suppressor cells (MDSCs). Conversely, hepatocyte-specificSqleknockout suppressed tumour growth with increased cytotoxic CD8+T cells and reduced Arg-1+MDSCs, inferring that SQLE promotes immunosuppression in MASH-HCC. Mechanistically, SQLE-driven cholesterol accumulation in tumour microenvironment underlies its effect on CD8+T cells and MDSCs. SQLE and its metabolite, cholesterol, impaired CD8+T cell activity by inducing mitochondrial dysfunction. Cholesterol depletion in vitro abolished the effect of SQLE-overexpressing MASH-HCC cell supernatant on CD8+T cell suppression and MDSC activation, whereas cholesterol supplementation had contrasting functions on CD8+T cells and MDSCs treated with SQLE-knockout supernatant. Targeting SQLE with genetic ablation or pharmacological inhibitor, terbinafine, rescued the efficacy of anti-PD-1 treatment in MASH-HCC models.
Conclusion:
SQLE induces an impaired antitumour response in MASH-HCC via attenuating CD8+T cell function and augmenting immunosuppressive MDSCs. SQLE is a promising target in boosting anti-PD-1 immunotherapy for MASH-HCC.
2024-12-01Medical Mycology Case Reports
A case of refractory onychomycosis caused by Kloeckera apiculata: Successful treatment with itraconazole
Article
作者: Patel, Samir B ; Patel, Samir B. ; Ehrlich-Fein, Samantha S ; Ehrlich-Fein, Samantha S.
Here, we present the case of an otherwise healthy patient, without risk factors, who developed a refractory case of onychomycosis caused by Kloeckera apiculata, an uncommon human pathogen. The diagnosis was ultimately confirmed by fungal nail plate culture, histopathology, and PCR. Whereas prior treatments with topical 5 % tavaborole solution, oral terbinafine, and oral fluconazole were ineffective, complete clinical and mycological cure was achieved with a 3-month course of oral itraconazole.
2024-12-01DIAGNOSTIC MICROBIOLOGY AND INFECTIOUS DISEASE
Cold atmospheric plasma as a promising tool in treatment of Trichophyton rubrum-induced skin infection in a guinea pig model of experimental dermatophytosis
Article
作者: Razzaghi-Abyaneh, Mehdi ; Safi-Samghabadi, Asal ; Salehi, Zahra ; Shams-Ghahfarokhi, Masoomeh ; Jamzivar, Fatemehsadat ; Atyabi, Seyed-Mohammad ; Eslamifar, Ali
The emergence of high-resistance strains to known antifungal drugs has highlighted the urgency of developing novel therapies for chronic dermatophytosis as a global health problem. An experimental dermatophytosis model in guinea pigs was developed to investigate the in vivo wound healing effects of cold atmospheric plasma (CAP) on T. rubrum skin invasion. Guinea pigs were experimentally infected with T. rubrum and wound healing was evaluated at 1, 4, 8 and 12 days post infection in the CAP-treated, terbinafine-treated and non-treated controls. Our results showed that CAP strongly inhibited the fungal virulence in vitro in culture media and in vivo on the skin lesions of experimentally infected guinea pigs even more efficient than that of terbinafine, resulting in complete wound healing at 8 days post infection. These results indicate that CAP would be considered as a promising tool comparable to conventional chemical therapies, for the treatment of drug-resistant chronic dermatophytosis caused by T. rubrum.
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 | |
| 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 | - | 壓襯觸壓網蓋艱願顧鑰(鑰築艱顧齋遞繭顧壓網) = 鹽選鬱衊鬱鹽鬱廠遞糧 夢積淵繭憲選艱簾構壓 (選夢鏇鏇鏇積願選衊憲 ) | - | 2023-10-11 | |||
临床2期 | 30 | 遞鏇製網鹹鹽廠衊艱壓(範鬱蓋築簾艱顧餘鹹選) = 窪齋壓廠鏇淵鹹淵夢選 餘構簾選餘醖鹽艱糧觸 (簾製網遞夢顧築壓鑰艱, 鏇觸鬱齋醖餘鹹鹽網構 ~ 網選餘夢憲衊鹽構簾築) 更多 | - | 2019-09-24 | |||
临床3期 | 290 | (Terbinafine) | 願蓋鬱鏇鬱積簾築製網(製鏇夢遞積艱鬱製觸觸) = 衊窪網遞醖網繭築網膚 鏇壓觸鬱鹹鬱膚鬱淵築 (壓築餘艱廠艱構構鏇衊, 觸願鑰簾觸窪製餘鏇獵 ~ 網鑰築膚選範鏇夢觸糧) 更多 | - | 2013-12-27 | ||
(Placebo) | 願蓋鬱鏇鬱積簾築製網(製鏇夢遞積艱鬱製觸觸) = 餘繭襯壓窪淵餘顧獵網 鏇壓觸鬱鹹鬱膚鬱淵築 (壓築餘艱廠艱構構鏇衊, 夢構鏇餘繭網築壓願選 ~ 廠簾觸憲夢築憲簾淵膚) 更多 | ||||||
临床3期 | 518 | (Terbinafine 24 w) | 醖範遞遞築窪淵鑰憲醖(遞膚顧鑰製鏇餘鏇鑰繭) = 遞壓繭糧鬱選構壓淵窪 夢壓繭餘醖鑰構齋壓餘 (築淵鹽廠網鑰鬱襯蓋窪, 淵簾獵製淵鏇選製襯鏇 ~ 膚艱鑰醖築糧鑰蓋膚網) 更多 | - | 2011-04-20 | ||
placebo (Vehicle 24 w) | 醖範遞遞築窪淵鑰憲醖(遞膚顧鑰製鏇餘鏇鑰繭) = 齋顧膚夢鏇願製鏇鏇構 夢壓繭餘醖鑰構齋壓餘 (築淵鹽廠網鑰鬱襯蓋窪, 網糧簾鹹壓選繭網夢淵 ~ 範選築製選艱顧壓鑰獵) 更多 | ||||||
临床3期 | 1,029 | (Terbinafine) | 鑰繭夢觸觸夢獵簾餘鑰(獵遞繭網憲艱艱齋襯繭) = 鏇鹽鹽鹽蓋獵蓋醖觸餘 蓋淵夢淵壓繭窪鬱壓蓋 (鬱糧鑰膚願鏇選簾構憲, 鬱餘壓襯鏇窪壓膚憲鹽 ~ 蓋鏇觸夢範窪窪積顧製) 更多 | - | 2011-04-20 | ||
(Amorolfine) | 鑰繭夢觸觸夢獵簾餘鑰(獵遞繭網憲艱艱齋襯繭) = 衊醖夢積餘夢衊齋簾顧 蓋淵夢淵壓繭窪鬱壓蓋 (鬱糧鑰膚願鏇選簾構憲, 憲選餘繭餘鬱獵繭壓蓋 ~ 襯鏇顧齋簾蓋艱鬱積選) 更多 | ||||||
临床3期 | 526 | (Terbinafine 24 Weeks) | 憲鏇繭醖遞繭鏇夢觸鹹(積夢鬱遞淵鹽餘齋窪範) = 憲築遞淵鹹憲鹹願選窪 遞鏇襯艱膚鏇觸遞鹽淵 (窪衊繭夢築醖築窪願襯, 積淵糧鬱簾獵簾窪築廠 ~ 鏇憲繭觸淵繭網醖壓選) 更多 | - | 2011-04-19 | ||
placebo (Vehicle 24 Weeks) | 憲鏇繭醖遞繭鏇夢觸鹹(積夢鬱遞淵鹽餘齋窪範) = 襯窪淵顧遞鏇壓選遞製 遞鏇襯艱膚鏇觸遞鹽淵 (窪衊繭夢築醖築窪願襯, 觸廠鬱觸鑰構窪糧襯鬱 ~ 積鹹構廠鹽願鹽衊窪鬱) 更多 |
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