(Econazole) - 药物靶点：CYP51A1_专利_临床

概要

基本信息

药物类型

小分子化药

别名

EcoNail、Econazole nail lacquerEconazole nail lacquer、SEPA

+ [1]

靶点

CYP51A1

作用机制

CYP51A1抑制剂(细胞色素P450家族成员51抑制剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

MacroChem Corp.

在研机构

MacroChem Corp.

非在研机构

Abeona Therapeutics, Inc.

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C18H15Cl3N2O

InChIKeyLEZWWPYKPKIXLL-UHFFFAOYSA-N

CAS号27220-47-9

关联

2

项与 Econazole 相关的临床试验

CTRI/2019/03/018237 / Not yet recruiting临床1/2期

Repurposing econazole and adding to the shorter WHO regimen for MDR tuberculosis (RESWMEN) Study - RESWMEN

开始日期2019-05-01

申办/合作机构

Indian Council of Medical Research

NCT00385502 / Completed临床2期

A Phase II Trial of the Safety, Local Tolerability, and Efficacy of EcoNail™ (Econazole 5%/SEPA® 18% Nail Lacquer) in Onychomycosis of the Great Toenail

Approximately 40 qualified subjects with mild-to-moderate great toenail fungus infection will be treated for 48 weeks with lacquer application to at least one affected great toenail. All subjects will receive treatment with EcoNail™ lacquer.

开始日期2006-09-30

申办/合作机构

Abeona Therapeutics, Inc.

100 项与 Econazole 相关的临床结果

登录后查看更多信息

100 项与 Econazole 相关的转化医学

登录后查看更多信息

100 项与 Econazole 相关的专利（医药）

登录后查看更多信息

849

项与 Econazole 相关的文献（医药）

2024-02-01·Structure

Structural mechanism of TRPV5 inhibition by econazole

Article

作者: Fluck, Edwin C ; Gabrielle, Matthew ; Moiseenkova-Bell, Vera Y ; Rohacs, Tibor ; De Jesús-Pérez, José J ; Raheem, Sumiyya

The calcium-selective TRPV5 channel activated by phosphatidylinositol 4,5-bisphosphate [PI(4,5)P₂] is involved in calcium homeostasis. Recently, cryoelectron microscopy (cryo-EM) provided molecular details of TRPV5 modulation by exogenous and endogenous molecules. However, the details of TRPV5 inhibition by the antifungal agent econazole (ECN) remain elusive due to the low resolution of the currently available structure. In this study, we employ cryo-EM to comprehensively examine how the ECN inhibits TRPV5. By combining our structural findings with site-directed mutagenesis, calcium measurements, electrophysiology, and molecular dynamics simulations, we determined that residues F472 and L475 on the S4 helix, along with residue W495 on the S5 helix, collectively constitute the ECN-binding site. Additionally, the structure of TRPV5 in the presence of ECN and PI(4,5)P₂, which does not show the bound activator, reveals a potential inhibition mechanism in which ECN competes with PI(4,5)P₂, preventing the latter from binding, and ultimately pore closure.

2024-02-01·Eye

Antifungal susceptibility profiles for fungal isolates from corneas and contact lenses in the United Kingdom

Article

作者: Borman, Andrew M ; Tuft, Stephen ; Johnson, Elizabeth M ; Burton, Matthew J ; Stone, Neil R H

AbstractObjectiveTo report the identification and results of susceptibility testing for fungal isolates from the cornea or contact lens care systems.Materials and methodsIn this retrospective epidemiological study, we searched the results of fungal cultures from cornea or contact lens systems referred for identification and susceptibility testing to the United Kingdom National Mycology Reference Laboratory between October 2016 and March 2022. For each fungal isolate, we recorded the genus and species of the fungus and the minimum inhibitory concentration (MIC) to six antifungal agents available to treat corneal infection (amphotericin, econazole, itraconazole, natamycin, posaconazole, and voriconazole).ResultsThere were 600 isolates from 585 patients, comprising 374 (62%) from corneal samples and 226 from contact lenses and care systems, of which 414 (69%) isolates were moulds (filamentous fungi) and 186 (31%) were yeasts. The most frequent moulds isolated were Fusarium spp (234 isolates, 39%) and Aspergillus spp (62, 10%). The most frequent yeasts isolated were Candida spp (112, 19%), predominantly Candida parapsilosis (65, 11%) and Candida albicans (33, 6%), with 35 isolates (6%) of Meyerozyma guilliermondii. In vitro susceptibility was greatest for natamycin (347 moulds tested, mode 4 mg/L, range 0.25–64 mg/L; 98 yeasts tested, mode 4 mg/L, range 0.5–32 mg/L), with susceptibility for 94% for moulds and 99% yeasts. Of the 16 isolates interpreted as highly resistant to natamycin (MIC ≥16 mg/L), 13 were Aspergillus flavus complex.ConclusionsIn vitro susceptibility supports the use of natamycin for the empiric treatment of fungal keratitis in the UK.

2023-12-01·Cell Reports Medicine

Econazole selectively induces cell death in NF1-homozygous mutant tumor cells

Article

作者: Moye, Stefanie L ; Lakes, Yenal B ; Charlton, Maura ; Mo, Juan ; Salinas, Gabrielle ; Tegtmeyer, Matthew ; Eggan, Kevin ; Nehme, Ralda ; McKay, Renee M ; Le, Lu Q

Cutaneous neurofibromas (cNFs) are tumors that develop in more than 99% of individuals with neurofibromatosis type 1 (NF1). They develop in the dermis and can number in the thousands. cNFs can be itchy and painful and negatively impact self-esteem. There is no US Food and Drug Administration (FDA)-approved drug for their treatment. Here, we screen a library of FDA-approved drugs using a cNF cell model derived from human induced pluripotent stem cells (hiPSCs) generated from an NF1 patient. We engineer an NF1 mutation in the second allele to mimic loss of heterozygosity, differentiate the NF1^+/- and NF1^-/- hiPSCs into Schwann cell precursors (SCPs), and use them to screen a drug library to assess for inhibition of NF1^-/- but not NF1^+/- cell proliferation. We identify econazole nitrate as being effective against NF1^-/- hiPSC-SCPs. Econazole cream selectively induces apoptosis in Nf1^-/- murine nerve root neurosphere cells and human cNF xenografts. This study supports further testing of econazole for cNF treatment.

100 项与 Econazole 相关的药物交易

登录后查看更多信息

研发状态

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


NCT00385502 (Biospace) 人工标引	临床2期	甲癣	37	EcoNail	獵遞廠衊廠鑰顧窪觸網(淵鏇壓糧獵製積範積選) = 鹽鹹簾淵積鏇膚艱齋遞繭窪築繭選糧醖範獵鹽 (膚鹹鹹鏇築選襯蓋鹹醖 ) 更多	不佳	2008-07-24