培西加南(Pexiganan Acetate) - 在研适应症：糖尿病足_专利_临床

概要

基本信息

药物类型

合成多肽

别名

Locilex、Pexiganan、Pexiganan acetate (USAN)

+ [2]

靶点-

作用机制

细胞膜通透性增强剂

治疗领域

神经系统疾病心血管疾病内分泌与代谢疾病+ [1]

在研适应症

糖尿病足

非在研适应症

复杂的皮肤和软组织感染糖尿病足感染糖尿病足溃疡+ [2]

原研机构

Genaera Corp.

在研机构

Genaera Corp.

非在研机构

Abeona Therapeutics, Inc.

Dipexium Pharmaceuticals, Inc.

最高研发阶段临床3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

分子式C122H210N32O22.C2H4O2

InChIKeyZYMCXUWEZQKVIO-IJAHCEAPSA-N

CAS号172820-23-4

序列信息

Sequence Code 44584

来源: *****

关联

5

项与培西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

NCT01594762 / Completed临床3期

A Randomized, Double-Blind, Multicenter, Superiority, Placebo-Controlled Phase 3 Study of Pexiganan Cream 0.8% Applied Twice Daily for 14 Days in the Treatment of Adults With Mild Infections of Diabetic Foot Ulcers

The purpose of this study is to establish the clinical superiority and the safety of topical pexiganan cream 0.8% plus standard local wound care as compared to placebo cream plus standard local wound care, in the treatment of mildly infected diabetic foot ulcers.

开始日期2014-06-01

申办/合作机构

Dipexium Pharmaceuticals, Inc.

NCT01590758 / Completed临床3期

A Randomized, Double-Blind, Multicenter, Superiority, Placebo-Controlled Phase 3 Study of Pexiganan Cream 0.8% Applied Twice Daily for 14 Days in the Treatment of Adults With Mild Infections of Diabetic Foot Ulcers

The purpose of this study is to establish the clinical superiority and the safety of topical pexiganan cream 0.8% plus standard local wound care, as compared to placebo cream plus standard local wound care, in the treatment of mildly infected diabetic foot ulcers.

开始日期2014-06-01

申办/合作机构

Dipexium Pharmaceuticals, Inc.

100 项与培西加南相关的临床结果

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100 项与培西加南相关的转化医学

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100 项与培西加南相关的专利（医药）

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122

项与培西加南相关的文献（医药）

2024-10-10·The Journal of Physical Chemistry B

Understanding Antimicrobial Peptide Synergy: Differential Binding Interactions and Their Impact on Membrane Integrity

Article

作者: Yoon, Jeseong ; Jo, Youngbeom ; Shin, Seokmin

Research on antimicrobial peptides (AMPs) has been conducted as a solution to overcome antibiotic resistance. In particular, the synergistic effect that appears when two or more AMPs are used in combination has been observed. To find an effective synergistic combination, it is necessary to understand the underlying mechanism. However, a consistent explanation for this phenomenon has not yet been provided due to limitations in experimentally determining or predicting the structure of the heteroaggregates formed by the interactions between different AMPs and the interaction of the aggregate surface with the lipid membrane surface. In this study, we conducted molecular dynamics simulations for two heterogeneous aggregates of melittin-indolicidin and pexiganan-indolicidin to observe their structures in the solution phase and their interactions with the lipid membrane. We aimed to determine how the surfaces of these aggregates interact with the lipid membrane. Due to the different amino acid residue sequence characteristics of melittin and pexiganan, we found that when the two AMPs bind to indolicidin, they form aggregates with completely different structural characteristics. Accordingly, the sequence characteristics of pexiganan, which exhibits a relatively unstable structure compared to melittin in aqueous solution or on lipid membranes, allow for a more stable interaction with the lipid membrane when forming aggregates with indolicidin, effectively inhibiting the integrity of the lipid membranes. We also found that the amino acid residues forming the surface of the AMP aggregate show differential binding strengths to different lipid species forming the lipid membrane, thereby disrupting the membrane in a way that weakens its integrity. Through this, we provided insight into the basic principle of how the synergistic effect of AMPs occurs.

2024-07-30·Open Life Sciences

Evaluation of the activity of antimicrobial peptides against bacterial vaginosis

Article

作者: Han, Qinqin ; Yuan, Tao ; Kang, Xuning ; Zhang, Jinyang ; Song, Yuzhu ; Zhao, Ting

AbstractNew drugs for the treatment of bacterial vaginosis (BV) are yet to be developed due to concerns that they may contribute to the increase in antibiotic resistance in BV. Antimicrobial peptides (AMPs) are one of the most promising options for next-generation antibiotics. In this study, we investigated the bacteriostatic activity of the AMPs Pexiganan, plectasin, melittin, and cathelicidin-DM against Gram-negative and Gram-positive bacteria both in vitro and in a mouse model of BV infection. The results showed that Pexiganan, melittin, and cathelicidin-DM had significant antibacterial activity against both Gram-negative and Gram-positive bacteria. AMPs have great potential for clinical application in the treatment of vaginitis, and this study provides an experimental basis for their use in the active immunoprophylaxis of BV.

2023-12-01·The Journal of Membrane Biology

Peptide Flexibility and the Hydrophobic Moment are Determinants to Evaluate the Clinical Potential of Magainins

Article

作者: Balleza, Daniel

Using a flexibility prediction algorithm and in silico structural modeling, we have calculated the intrinsic flexibility of several magainin derivatives. In the case of magainin-2 (Mag-2) and magainin H2 (MAG-H2) we have found that MAG-2 is more flexible than its hydrophobic analog, Mag-H2. This affects the degree of bending of both peptides, with a kink around two central residues (R10, R11), whereas, in Mag-H2, W10 stiffens the peptide. Moreover, this increases the hydrophobic moment of Mag-H2, which could explain its propensity to form pores in POPC model membranes, which exhibit near-to-zero spontaneous curvatures. Likewise, the protective effect described in DOPC membranes for this peptide regarding its facilitation in pore formation would be related to the propensity of this lipid to form membranes with negative spontaneous curvature. The flexibility of another magainin analog (MSI-78) is even greater than that of Mag-2. This facilitates the peptide to present a kind of hinge around the central F12 as well as a C-terminal end prone to be disordered. Such characteristics are key to understanding the broad-spectrum antimicrobial actions exhibited by this peptide. These data reinforce the hypothesis on the determinant role of spontaneous membrane curvature, intrinsic peptide flexibility, and specific hydrophobic moment in assessing the bioactivity of membrane-active antimicrobial peptides.

100 项与培西加南相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D05448	-	-	DB16293

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
糖尿病足	临床3期	-	Genaera Corp.	-
糖尿病足感染	临床1期	美国	Dipexium Pharmaceuticals, Inc.	2014-06-01
糖尿病足溃疡	临床1期	美国	Abeona Therapeutics, Inc.	1994-08-01
糖尿病溃疡	临床1期	美国	Abeona Therapeutics, Inc.	1994-08-01
复杂的皮肤和软组织感染	临床1期	美国	-	-
脓疱疮	药物发现	美国	Genaera Corp.	-

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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


NCT01590758 (OneStep-1, CTgov)	临床3期	糖尿病足感染	189	Standard wound care+Topical pexiganan cream 0.8% (Topical Pexiganan Cream 0.8%)	簾觸觸獵齋餘餘獵願製(選顧蓋餘繭齋積築廠鹽) = 鹽築齋糧願鬱艱積選積壓鬱蓋齋築夢壓積製築 (艱鹹鏇艱膚膚憲構廠觸, 構範選觸窪獵鬱鑰鑰簾 ~ 鹹構遞構製鑰築窪構壓) 更多	-	2017-06-14
				Topical placebo cream (Topical Placebo Control)	簾觸觸獵齋餘餘獵願製(選顧蓋餘繭齋積築廠鹽) = 廠艱願願願鹹築範遞衊壓鬱蓋齋築夢壓積製築 (艱鹹鏇艱膚膚憲構廠觸, 憲窪衊網蓋構襯獵觸遞 ~ 衊艱築糧鬱膚憲鬱蓋窪) 更多
NCT01594762 (OneStep-2, CTgov)	临床3期	糖尿病足感染	200	Standard wound care+Topical pexiganan cream 0.8% (Topical Pexiganan Cream 0.8%)	積鹹蓋糧範網鑰襯膚積(淵製構廠積築窪鑰襯壓) = 鑰襯鑰淵醖鑰廠衊餘糧夢窪淵製醖顧鹹網襯鏇 (鬱鑰夢構獵積憲簾鹹鏇, 願簾齋鹽襯廠衊鬱構觸 ~ 廠衊鹽餘鏇鹹憲艱鑰艱) 更多	-	2017-06-14
				Topical placebo cream (Topical Placebo Control)	積鹹蓋糧範網鑰襯膚積(淵製構廠積築窪鑰襯壓) = 衊鑰醖壓願膚顧鏇觸願夢窪淵製醖顧鹹網襯鏇 (鬱鑰夢構獵積憲簾鹹鏇, 鬱範範繭艱鑰衊簾鏇糧 ~ 夢糧膚積網夢蓋簾範製) 更多