奥米加南(Omiganan) - 在研适应症：大疱性角膜病变_专利_临床

概要

基本信息

药物类型

合成多肽

别名

Omiganan pentachloride、Omiganan pentahydrochloride、Omiganan pentahydrochloride (USAN)

+ [7]

靶点-

作用方式

增强剂

作用机制

细胞膜通透性增强剂

治疗领域

眼部疾病

在研适应症

大疱性角膜病变

非在研适应症

寻常痤疮菌血症尖锐湿疣+ [5]

原研机构

Carrus Technologies, Inc.

在研机构-

非在研机构

Cutanea Life Sciences, Inc.Global Gaming Technologies Corp.

权益机构-

最高研发阶段临床1/2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C90H128ClN27O12

InChIKeyXZVPZZJCWDNELR-NLRWEPRHSA-N

CAS号269062-93-3

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Sequence Code 116133

来源: *****

关联

20

项与奥米加南相关的临床试验

IRCT20190924044863N1

/ Completed临床1期IIT

Evaluate the safety, side effects and maximum tolerable dose of topical application of Antimicrobial Peptides: Pexiganan (MSI-78), Tilapia piscidin 4 (TP4), Melittin, Nisin-A and Omiganan (MX-226) on the skin of healthy volunteers to the treatment of Skin and Soft Tissue Infections.

开始日期2020-07-22

申办/合作机构

Mashhad University of Medical Sciences

NCT03688971

/ Unknown status临床2期

A Phase 2, Randomized, Vehicle and Ketoconazole-Controlled, Evaluator-Blinded, Study to Explore the Efficacy, Pharmacodynamics and Safety of Omiganan 1.75% Topical Gel BID in Patients With Mild to Moderate Facial Seborrheic Dermatitis

To explore the efficacy and pharmacodynamic effects of omiganan topical gel in facial seborrheic dermatitis.

开始日期2018-10-22

申办/合作机构

Maruho Co., Ltd.

EUCTR2017-003106-41-NL

/ Not yet recruiting临床2期

A phase 2, randomized, vehicle and ketoconazole-controlled, evaluator-blinded, study to explore the efficacy, pharmacodynamics and safety of omiganan 1.75% topical gel BID in patients with mild to moderate facial seborrheic dermatitis.

开始日期2018-09-05

申办/合作机构

Maruho Co., Ltd.

100 项与奥米加南相关的临床结果

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100 项与奥米加南相关的转化医学

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100 项与奥米加南相关的专利（医药）

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70

项与奥米加南相关的文献（医药）

2024-11-11·ACS Biomaterials Science & Engineering

Omiganan-Based Synthetic Antimicrobial Peptides for the Healthcare of Infectious Endophthalmitis

Article

作者: Wang, Yongjie ; Qu, Sheng ; Wang, Shuo ; Zheng, Zhi ; Xin, Jingguo ; Ong, Zhan Yuin ; Wu, Hong

Bacterial endophthalmitis is a severe infection of the aqueous or vitreous humor of the eye that can lead to permanent vision loss. Due to the rapid emergence of antibiotic resistance and dose-limiting toxicities, the standard treatment of bacterial endophthalmitis via the intravitreal injection of broad-spectrum antibiotics remains inadequate. Membrane active cationic antimicrobial peptides (AMPs) have emerged as a promising class of effective and broad-spectrum antimicrobial agents with potential to overcome antibiotic resistance. In this work, we investigate, for the first time, the use of omiganan (IK-12), a 12-amino acid indolicidin derivative for the treatment of bacterial endophthalmitis. Additionally, IK-12 was used as a template to perform amino acid rearrangements, without altering the length or type of amino acids, to yield a series of new derivative AMPs with varying extents of secondary structure formation under membrane mimicking conditions. IK-12 and its derivatives demonstrated strong and broad-spectrum antibacterial activities against a panel of clinically isolated Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus commonly implicated in bacterial endophthalmitis. Interestingly, two of the new IK-12 derivatives, IP-12 and WP-12, showed lower geometric mean minimum inhibitory concentration and higher 50% hemolysis concentration values, which effectively translated into 2- to 3.4-fold higher bacterial selectivity than the parent IK-12. Furthermore, the intravitreal injection of IK-12, IP-12, and WP-12 in a rabbit model of MRSA-induced endophthalmitis led to considerably improved clinical presentation and reduced recruitment of inflammatory cells. In all, these results demonstrate the potential of IK-12 and its derivatives, IP-12 and WP-12, as promising candidates for the treatment of bacterial endophthalmitis.

2023-11-01·Asian Journal of Pharmaceutical Sciences

An infection-microenvironment-targeted and responsive peptide-drug nanosystem for sepsis emergency by suppressing infection and inflammation

Article

作者: Gai, Yongkang ; Fu, Daan ; Ye, Zhilan ; Liu, Xingxin ; Chang, Bingcheng ; Chen, Xu ; Liu, Jia ; He, Wei ; Yang, Chang

Sepsis is a life-threatening emergency that causes millions of deaths every year due to severe infection and inflammation. Nevertheless, current therapeutic regimens are inadequate to promptly address the vast diversity of potential pathogens. Omiganan, an antimicrobial peptide, has shown promise for neutralizing endotoxins and eliminating diverse pathogens. However, its clinical application is hindered by safety and stability concerns. Herein, we present a nanoscale drug delivery system (Omi-hyd-Dex@HA NPs) that selectively targets infectious microenvironments (IMEs) and responds to specific stimuli for efficient intervention in sepsis. The system consists of omiganan-dexamethasone conjugates linked by hydrazone bonds which self-assemble into nanoparticles coated with a hyaluronic acid (HA). The HA coating not only facilitates IMEs-targeting through interaction with intercellular-adhesion-molecule-1 on inflamed endotheliocytes, but also improves the biosafety of the nanosystem and enhances drug accumulation in primary infection sites triggered by hyaluronidase. The nanoparticles release dual drugs in IMEs through pH-sensitive cleavage of hydrazone bonds to eradicate pathogens and suppress inflammation. In multiple tissue infection and sepsis animal models, Omi-hyd-Dex@HA NPs exhibited rapid source control and comprehensive inflammation reduction, thereby preventing subsequent fatal complications and significantly improving survival outcomes. The bio-responsive and self-delivering nanosystem offers a promising strategy for systemic sepsis treatment in emergencies.

2023-04-01·Amino Acids

Rational design of stapled antimicrobial peptides

Review

作者: Zhu, YouZhuo ; Liu, HongYu ; Zheng, Heng ; You, YuHao

The global increase in antimicrobial drug resistance has dramatically reduced the effectiveness of traditional antibiotics. Structurally diverse antibiotics are urgently needed to combat multiple-resistant bacterial infections. As part of innate immunity, antimicrobial peptides have been recognized as the most promising candidates because they comprise diverse sequences and mechanisms of action and have a relatively low induction rate of resistance. However, because of their low chemical stability, susceptibility to proteases, and high hemolytic effect, their usage is subject to many restrictions. Chemical modifications such as D-amino acid substitution, cyclization, and unnatural amino acid modification have been used to improve the stability of antimicrobial peptides for decades. Among them, a side-chain covalent bridge modification, the so-called stapled peptide, has attracted much attention. The stapled side-chain bridge stabilizes the secondary structure, induces protease resistance, and increases cell penetration and biological activity. Recent progress in computer-aided drug design and artificial intelligence methods has also been used in the design of stapled antimicrobial peptides and has led to the successful discovery of many prospective peptides. This article reviews the possible structure-activity relationships of stapled antimicrobial peptides, the physicochemical properties that influence their activity (such as net charge, hydrophobicity, helicity, and dipole moment), and computer-aided methods of stapled peptide design. Antimicrobial peptides under clinical trial: Pexiganan (NCT01594762, 2012-05-07). Omiganan (NCT02576847, 2015-10-13).

100 项与奥米加南相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D05262	-	-	DB06610

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
大疱性角膜病变	临床2期	日本	-	-
特应性皮炎	临床前	荷兰	Cutanea Life Sciences, Inc.	2016-11-25
尖锐湿疣	临床前	荷兰	Cutanea Life Sciences, Inc.	2016-04-06
外阴上皮内瘤变	临床前	荷兰	Cutanea Life Sciences, Inc.	2015-11-21
玫瑰痤疮	临床前	澳大利亚	Cutanea Life Sciences, Inc.	2015-08-13
寻常痤疮	临床前	-	Global Gaming Technologies Corp.	2000-10-01
痤疮丙酸杆菌感染	临床前	-	Global Gaming Technologies Corp.	2000-10-01
菌血症	临床前	美国	Global Gaming Technologies Corp.	2000-09-01
真菌血症	临床前	美国	Global Gaming Technologies Corp.	2000-09-01

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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


NCT02576860 (CTgov)	临床3期	玫瑰痤疮	263	Omiganan (Treatment)	範蓋網構憲鹽鑰觸鹽蓋(鏇醖網鹽淵膚觸齋遞製) = 鬱鏇鏇願鹹餘鏇願膚糧築鑰遞餘膚願願艱鹹鏇 (衊鑰糧糧選鹽齋膚繭糧, 襯夢鬱鹽蓋憲壓憲鏇窪 ~ 簾積窪夢淵構網鬱廠鹹) 更多	-	2022-07-08
				Vehicle (Vehicle Gel)	範蓋網構憲鹽鑰觸鹽蓋(鏇醖網鹽淵膚觸齋遞製) = 觸製顧鹽觸鹹糧鑰鬱襯築鑰遞餘膚願願艱鹹鏇 (衊鑰糧糧選鹽齋膚繭糧, 構繭襯齋餘積蓋鬱鹹鏇 ~ 窪鑰獵廠築窪築積獵鹽) 更多
NCT02576847 (CTgov)	临床3期	玫瑰痤疮	307	Omiganan	獵觸衊淵膚衊鬱艱鹹壓(顧顧衊網繭襯鑰鏇憲淵) = 範醖窪窪艱繭憲鹹襯構淵積鏇築艱艱觸構襯齋 (遞膚網糧窪壓顧醖鑰襯, 鑰觸餘鏇範顧衊選廠蓋 ~ 憲淵顧餘齋構糧蓋鹹顧) 更多	-	2022-07-06
NCT02849262 \| NCT02596074 (Pubmed \| Br J Clin Pharmacol) 人工标引	临床2期	尖锐湿疣 \| 鳞状上皮内病变	36	omiganan	(憲範選廠襯繭艱範糧窪) = 鹹膚網廠範窪襯網夢憲鏇襯製積壓鬱醖鹹鏇顧 (鑰積鹹願繭蓋窪積鬱廠, -99.9 ~ -7.4)	积极	2020-11-01
				Placebo	-
NCT00608959 (CTgov)	临床3期	感染	30	Omiganan (Omiganan 1% Gel (Part 2))	遞壓齋齋艱選襯廠鬱憲(顧鹽蓋艱獵觸憲鑰壓夢) = 鏇壓製積獵繭壓鬱窪壓顧鏇遞遞憲糧鑰鬱鑰餘 (襯鹹鹽網鬱糧鹽鹽艱襯, 遞憲糧膚獵醖鹽艱襯淵 ~ 鹹繭醖餘憲夢廠淵觸鑰) 更多	-	2010-01-25
				Chlorhexidine (Chlorhexidine 2%(Part 1))	遞壓齋齋艱選襯廠鬱憲(顧鹽蓋艱獵觸憲鑰壓夢) = 鹽簾糧窪餘製齋觸窪願顧鏇遞遞憲糧鑰鬱鑰餘 (襯鹹鹽網鬱糧鹽鹽艱襯, 獵淵餘獵醖壓淵製蓋鑰 ~ 鹽襯鏇遞構鏇鑰積願蓋)