阿巴康唑(Albaconazole) - 药物靶点：fungal CYP51A1_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Albaconazole (USAN/INN)

+ [1]

靶点

fungal CYP51A1

作用机制

fungal CYP51A1抑制剂(真菌细胞色素P450家族成员51抑制剂)

治疗领域

感染皮肤和肌肉骨骼疾病泌尿生殖系统疾病+ [1]

在研适应症-

非在研适应症

外阴阴道念珠菌病Chagas病真菌病+ [2]

原研机构

Palau Pharma SA

在研机构-

非在研机构

GSK PlcActavis A/S

Palau Pharma SA

+ [1]

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C20H16ClF2N5O2

InChIKeyUHIXWHUVLCAJQL-MPBGBICISA-N

CAS号187949-02-6

关联

7

项与阿巴康唑相关的临床试验

CTIS2023-504727-32-00

/ Recruiting临床2期IIT

A double-blind, randomised, dose-finding trial to assess the efficacy, safety and pharmacokinetics of a single dose of albaconazole versus fluconazole and placebo in the treatment of acute Candida vulvovaginitis - DC13ALB/2/21

开始日期2023-11-10

申办/合作机构-

NCT01039883

/ Completed临床1期

A Phase 1, Randomized, Open-Label, Crossover Safety and Pharmacokinetic Study of 400 mg Albaconazole as a Tablet Formulation Versus a Capsule Formulation in Healthy Subjects

The purpose of this study is to determine whether albaconazole tablets and albaconazole capsules (single 400mg dose) act in the body in the same way over a period of time.

开始日期2009-11-23

申办/合作机构

Stiefel Laboratories, Inc.

[+1]

NCT01014962

/ Completed临床1期

A Randomized, Double-Blind, Multiple-Dose, Placebo-Controlled Tolerability And Pharmacokinetic Study Of Escalating Doses Of Albaconazole In Healthy Subjects

The purpose of this study is to determine an upper dose of albaconzole to be administered in a Thorough QTc study.

开始日期2009-08-24

申办/合作机构

Stiefel Laboratories, Inc.

[+1]

100 项与阿巴康唑相关的临床结果

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100 项与阿巴康唑相关的转化医学

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100 项与阿巴康唑相关的专利（医药）

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52

项与阿巴康唑相关的文献（医药）

2024-06-01·Mucosal Immunology

MZB1-mediated IgA secretion suppresses the development and progression of colorectal cancer triggered by gut inflammation

Article

作者: Lu, Chunhui ; Luan, Yingying ; Wang, Ji-Yang ; Lu, Qing ; Cui, Chaoqun ; Liu, Jie ; Feng, Xiaoqian ; Hase, Koji ; Dong, Lulu ; Tang, Yue ; Hu, Ziying ; Yu, Meiping ; Shinkura, Reiko ; Wen, Zichao ; Zhang, Runyun

Colorectal cancer (CRC) ranks among the top causes of mortality globally. Gut inflammation is one crucial risk factor that augments CRC development since patients suffering from inflammatory bowel disease have an increased incidence of CRC. The role of immunoglobulin (Ig)A in maintaining gut homeostasis and preventing inflammation has been well established. Our earlier work demonstrated that the marginal zone and B1 cell-specific protein (MZB1) promotes gut IgA secretion and its absence results in pronounced dextran sulfate sodium salt (DSS)-induced colitis. In the present study, we explored the role of MZB1 in CRC development using the azoxymethane (AOM)/DSS-induced CRC model. We observed an increase in both the number and size of the tumor nodules in Mzb1^-/- mice compared with Mzb1^+/+ mice. The increase in CRC development and progression in Mzb1^-/- mice was associated with reduced intestinal IgA levels, altered gut flora, and more severe gut and systemic inflammation. Oral administration of the monoclonal IgA, W27, alleviated both the gut inflammation and AOM/DSS-induced CRC. Notably, cohousing Mzb1^+/+ and Mzb1^-/- mice from the 10th day after birth led to similar CRC development. Our findings underscore the pivotal role of MZB1-mediated IgA secretion in suppressing the onset and progression of CRC triggered by gut inflammation. Moreover, our study highlights the profound impact of microbiota composition, modulated by gut IgA levels, on gut inflammation. Nonetheless, establishing a direct correlation between the severity of colitis and subsequent CRC development and the presence or absence of a particular microbiota is challenging.

2024-04-25·Journal of Medicinal Chemistry

Discovery of a Novel Potent Tetrazole Antifungal Candidate with High Selectivity and Broad Spectrum

Article

作者: Wang, Ting ; Xie, Fei ; Ding, Zichao ; Yan, Lan ; Bao, Junhe ; Hao, Yumeng ; Wang, Ruina ; Zhang, Dazhi ; Chi, Xiaochen ; Ni, Tingjunhong ; Jiang, Yuanying ; Li, Liping

Thirty-one novel albaconazole derivatives were designed and synthesized based on our previous work. All compounds exhibited potent in vitro antifungal activities against seven pathogenic fungi. Among them, tetrazole compound D2 was the most potent antifungal with MIC values of <0.008, <0.008, and 2 μg/mL against Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus, respectively, the three most common and critical priority pathogenic fungi. In addition, compound D2 also exhibited potent activity against fluconazole-resistant C. auris isolates. Notably, compound D2 showed a lower inhibitory activity in vitro against human CYP450 enzymes as well as a lower inhibitory effect on the hERG K⁺ channel, indicating a low risk of drug-drug interactions and QT prolongation. Moreover, with improved pharmacokinetic profiles, compound D2 showed better in vivo efficacy than albaconazole at reducing fungal burden and extending the survival of C. albicans-infected mice. Taken together, compound D2 will be further investigated as a promising candidate.

2022-03-01·European Journal of Medicinal Chemistry1区 · 医学

Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development

1区 · 医学

Review

作者: Emami, Saeed ; Saednia, Shahnaz ; Ghobadi, Elham

Voriconazole (VCZ) was the first approved triazole antifungal drug with 1-(1H-1,2,4-triazol-1-yl)butan-2-ol substructure. This drug showed a broad spectrum of activity, especially against yeasts and molds, and opened a new avenue toward the novel class of systemic antifungal agents. Modification of 2-fluoropyrimidine in the side chain of VCZ resulted in a newer generation of triazolylbutanols including efinaconazole, albaconazole, ravuconazole, and isavuconazole with the favorable antifungal spectrum, enhanced pharmacokinetic properties, and tolerable toxicity profiles. Due to the importance of triazolylbutanols in the discovery and development of new antifungal agents, in this review we have focused on the synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole. This comprehensive review provides highlighting scope for medicinal chemists for the design, synthesis and development of novel potential antifungal drugs having better activity, pharmacokinetic property and toxicity profile.

100 项与阿巴康唑相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D09702	阿巴康唑	-	DB12073

研发状态

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
甲癣	临床2期	加拿大	GSK Plc	2008-07-16
甲癣	临床2期	美国	GSK Plc	2008-07-16
甲癣	临床2期	冰岛	GSK Plc	2008-07-16
足癣	临床2期	美国	GSK Plc	2007-07-01
足癣	临床2期	澳大利亚	GSK Plc	2007-07-01
外阴阴道念珠菌病	临床2期	-	Grupo J Uriach SL	2004-06-01
Chagas病	临床2期	西班牙	-	-
真菌病	临床2期	-	Palau Pharma SA	-
真菌病	临床2期	-	Actavis A/S	-

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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


NCT00730405 (CTgov)	临床2期	甲癣	582	Albaconazole (Albaconazole 400 mg (36 Weeks) Oral Weekly)	簾齋獵鑰夢蓋壓鹹製鏇(窪膚衊壓鏇簾齋網鹹淵) = 觸糧觸齋淵衊顧憲選鑰製蓋製蓋鏇鹽廠積膚網 (膚夢廠憲襯淵餘鏇壓願, 衊膚廠鏇鑰選廠醖網築 ~ 鑰蓋蓋範鬱鏇餘鬱構膚) 更多	-	2018-02-07
				Albaconazole (Albaconazole 400 mg (24 Weeks) Oral Weekly)	簾齋獵鑰夢蓋壓鹹製鏇(窪膚衊壓鏇簾齋網鹹淵) = 鬱蓋鹽繭鬱遞願簾遞壓製蓋製蓋鏇鹽廠積膚網 (膚夢廠憲襯淵餘鏇壓願, 簾衊衊鹽選醖製鬱積觸 ~ 餘艱積範齋衊鑰鏇鏇夢) 更多