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

非在研适应症

原研机构

在研机构

非在研机构

Dipexium Pharmaceuticals, Inc.

Abeona Therapeutics, 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-

结构

分子式C122H210N32O22

InChIKeyKGZGFSNZWHMDGZ-KAYYGGFYSA-N

CAS号147664-63-9

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

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

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.

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.

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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120

项与培西加南相关的文献（医药）

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.

2023-05-01·Biophysical Chemistry

The role of hydrophobic patches of de novo designed MSI-78 and VG16KRKP antimicrobial peptides on fragmenting model bilayer membranes

Article

作者: Mohid, Sk Abdul ; Kim, MinSoo ; Krishnamoorthy, Janarthanan ; Won, TaeJun ; Lee, DongKuk ; Biswas, Indranil ; Choi, JiHye ; Bhunia, Anirban

Antimicrobial peptides (AMPs) with cell membrane lysing capability are considered potential candidates for the development of the next generation of antibiotics. Designing novel AMPs requires an in-depth understanding of the mechanism of action of the peptides. In this work, we used various biophysical techniques including ³¹P solid-state NMR to examine the interaction of model membranes with amphipathic de novo-designed peptides. Two such peptides, MSI-78 and VG16KRKP, were designed with different hydrophobicity and positive charges. The model lipid membranes were constituted by mixing lipids of varying degrees of 'area per lipid' (APL), which directly affected the packing properties of the membrane. The observed emergence of the isotropic peak in ³¹P NMR spectra as a function of time is a consequence of the fragmentation of the membrane mediated by the peptide interaction. The factors such as the charges, overall hydrophilicity of the AMPs, as well as lipid membrane packing, contributed to the kinetics of membrane fragmentation. Furthermore, we anticipate the designed AMPs follow the carpet and toroidal pore mechanisms when lysing the cell membrane. This study highlights the significance of the effect of the overall charges and the hydrophobicity of the novel AMPs designed for antimicrobial activity.

2023-04-14·ACS infectious diseases

The Impact of Antimicrobial Peptides on the Acinetobacter baumannii Inner Membrane Is Modulated by Lipid Polyunsaturation.

Article

作者: O'Mara, Megan L ; Wilson, Katie A ; MacDermott-Opeskin, Hugo I

The Gram-negative pathogen Acinetobacter baumannii is a primary contributor to nosocomial multi-drug-resistant (MDR) infections. To combat the rise of MDR infections, novel features of A. baumannii need to be considered for the development of new treatment options. One such feature is the preferential scavenging of exogenous lipids, including host-derived polyunsaturated fatty acids (PUFAs), for membrane phospholipid synthesis. These alterations in membrane composition impact both the lipid chemistry and the membrane biophysical properties. In this work we examine how antimicrobial peptides (AMPs) interact with the inner membranes of A. baumannii in the presence and absence of polyunsaturated phospholipids. Using coarse-grained molecular dynamics simulations of complex A. baumannii inner membrane models derived from lipidomes of bacteria grown in the presence and absence of PUFAs, we examine the impact of the adsorption of four prototypical AMPs (CAMEL, LL-37, pexiganan, and magainin-2) on the membrane biophysical properties. Our simulations reveal that the impact of AMP adsorption on the membrane biophysical properties was dependent on both the membrane composition and the specific AMP involved. Both lipid headgroup charge and tail unsaturation played important roles in driving the interactions that occurred both within the membrane and between the membrane and AMPs. The changes to the membrane biophysical properties also showed a complex relationship with the AMP's physical properties, such as AMP charge, chain length, and charge-to-mass ratio. Cumulatively, this work highlights the importance of studying AMPs using a complex membrane environment and provides insights into the mechanistic action of AMPs in polyunsaturated lipid-rich bacterial membranes.

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	临床前	美国	Dipexium Pharmaceuticals, Inc.	2014-06-01
复杂的皮肤和软组织感染	临床前	美国	-	-
脓疱疮	临床前	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 (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%)	(鹹醖築鬱製廠鹽廠淵醖) = 鹽鑰窪繭簾鹽獵鹹顧鹽選廠壓窪鹹夢窪鹽積獵 (選顧鬱壓鹹鹹鑰蓋願鹹, 淵淵簾衊淵鏇遞選蓋淵 ~ 艱簾鏇遞窪窪艱築淵獵) 更多	-	2017-06-14
				Topical placebo cream (Topical Placebo Control)	(鹹醖築鬱製廠鹽廠淵醖) = 壓壓艱廠簾廠憲鏇淵築選廠壓窪鹹夢窪鹽積獵 (選顧鬱壓鹹鹹鑰蓋願鹹, 鹽繭醖鬱壓壓鬱鏇醖願 ~ 鹹繭淵築衊齋淵廠願夢) 更多
NCT01594762 (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%)	(蓋齋淵鬱夢淵齋獵壓糧) = 鏇範鏇醖選獵鬱鬱齋觸廠廠選願範醖壓鬱鑰製 (膚構襯鑰簾憲遞齋獵鹹, 簾積築鏇夢鏇糧遞獵夢 ~ 遞鹹壓衊餘襯壓淵觸構) 更多	-	2017-06-14
				Topical placebo cream (Topical Placebo Control)	(蓋齋淵鬱夢淵齋獵壓糧) = 蓋選廠製願獵鬱夢築淵廠廠選願範醖壓鬱鑰製 (膚構襯鑰簾憲遞齋獵鹹, 選獵齋淵憲廠廠鬱艱壓 ~ 築觸膚製壓壓憲範選簾) 更多