Delving into the Latest Updates on Peceleganan with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Antimicrobial Peptides PL-5, 抗菌肽PL-5, PL-5

Target

PBPs

Action

inhibitors

Mechanism

PBPs inhibitors(Bacterial penicillin-binding protein inhibitors)

Therapeutic Areas

Infectious DiseasesNervous System DiseasesCardiovascular Diseases+ [2]

Active Indication

Infectious DiseasesWound InfectionBacterial Infections+ [1]

Inactive Indication

Burn infectionsFolliculitisImpetigo+ [3]

Originator Organization

Protelight Pharmaceuticals

Active Organization

Protelight Pharmaceuticals

Sino Biopharmaceutical Ltd.

Inactive Organization-

License Organization

Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Protelight Pharmaceuticals

Drug Highest PhaseNDA/BLA

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC138H226N36O34

InChIKeyIUYWAZJIRQDBEJ-XECNVCPKSA-N

CAS Registry850761-47-6

Sequence Code 10641

Source: *****

Primary purpose: To evaluate the effectiveness of antimicrobial peptide PL-5 spray in treating wound infection, using placebo as negative control. Secondary purpose: To evaluate the safety of antimicrobial peptide PL-5 spray in treating wound infection, using placebo as negative control. To assess the entry of antimicrobial peptide PL-5 spray into the blood circulation system through the wound.

Start Date07 Jun 2023

Sponsor / Collaborator

Protelight Pharmaceuticals

[+1]

ChiCTR2300071255

/ RecruitingPhase 3IIT

A multicenter, randomized, double-blind, placebo-controlled phase IIIb clinical trial to assess the efficacy and safety of antibacterial peptide PL-5 Spray for wound infections

Start Date15 May 2023

Sponsor / Collaborator

Shenzhen Second People's Hospital

CTR20211324

/ CompletedPhase 3

一项评估抗菌肽PL-5喷雾剂治疗创面感染的有效性和安全性的多中心、随机、开放性、阳性对照的III期临床试验

[Translation] A multicenter, randomized, open-label, active-controlled phase III clinical trial to evaluate the efficacy and safety of the antimicrobial peptide PL-5 spray in the treatment of wound infection

1、主要目的以磺胺嘧啶银乳膏为阳性对照，评价抗菌肽PL-5喷雾剂治疗创面感染的有效性。 2、次要目的以磺胺嘧啶银乳膏为阳性对照，评价抗菌肽PL-5喷雾剂治疗创面感染的安全性。

[Translation]

1. Main purpose Using sulfadiazine silver cream as a positive control, evaluate the effectiveness of antimicrobial peptide PL-5 spray in treating wound infection. 2. Secondary purpose Using sulfadiazine silver cream as a positive control, evaluate the safety of antimicrobial peptide PL-5 spray in treating wound infection.

Start Date23 Aug 2021

Sponsor / Collaborator

Protelight Pharmaceuticals

[+1]

100 Clinical Results associated with Peceleganan

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100 Translational Medicine associated with Peceleganan

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100 Patents (Medical) associated with Peceleganan

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10

Literatures (Medical) associated with Peceleganan

01 Jan 2024·JOURNAL OF ETHNOPHARMACOLOGY

Diosmin: A Daboia russelii venom PLA2s inhibitor- purified, and characterized from Oxalis corniculata L medicinal plant

Article

Author: Kameshwar, Vivek Hamse ; Varadaraju, Kavitha Raj ; Dugganaboyana, Guru Kumar ; Nanjunda Swamy, S ; Nagalambika, Prasad ; Kumar, J R ; Kiran, K S ; Mudnakudu Nagaraju, Kiran Kumar ; Krishna, K L ; Karthik, N Awathade

ETHNOPHARMACOLOGICAL RELEVANCE:

Oxalis corniculata L is a medicinal plant that belongs to the Oxalidaceae family. It is a little, slow-growing plant with a frail appearance typically found in mild temperate and tropical areas like Pakistan and India. This plant also includes many other bioactive substances, including alkaloids, flavonoids, terpenoids, cardiac glycosides, saponins, phlobatannins, and steroids.

AIM OF THE STUDY:

To investigate the anti-inflammatory effects of Compound diosmin, which is derived from Oxalis corniculata L, on VRV-PL-5 and VRV-PL-8a isolated from Vipera russelli.

MATERIALS AND METHODS:

Extraction, purification, and characterization of bioactive by TLC, HPTLC, FT-IR analysis, UV-Vis spectrophotometer, LC-MS/MS Analysis, NMR, XRD Analysis, In vitro evaluation, Circular dichroism spectroscopy, in vivo, and in silico studies.

RESULTS:

In this study, the extract of Oxalis corniculata was evaluated for its in vitro and in vivo anti-inflammatory effect against PLA₂. The methanolic extract decreased hemolytic activity by about 60% at 1:75 w/w and neutralized the hemolytic activity completely at 1:100 w/w concentration. Diosmin inhibited VRV-PL-5 and VRV-PL-8a in a dose-dependent manner, with the extent of inhibition being about 56% for VRV-PL-5120 μM and VRV-PL-8a by 62% at the same concentration with IC₅₀ concentrations of 87.08 μM for VRV-PL-5 and 82.08 μM for VRV-PL-8a, while at 75 μM. Diosmin inhibited the hemolytic activity of VRV-PL-5 by about 85%, and at the same concentration, VRV-PL-8a inhibited by about 75%. UV-CD spectra at the IC₅₀ concentration of diosmin disrupted the secondary structure of VRV-PL-5 &VRV-PL-8a. In vivo, studies showed decreased myotoxicity and cardiotoxicity of the VRV-PL-5 &VRV-PL-8a, which was seen in the decrease in cytoplasmic markers LDH and CPK levels in the serum when incubated with diosmin. Furthermore, Histopathological studies of Muscles and lungs revealed that diosmin considerably protects against cellular abnormality caused by VRV-PL-5 & VRV-PL-8a. Molecular docking, MM/GBSA, and molecular dynamics simulation studies show that the diosmin is a potent inhibitor for VRV-PL-5 and VRV-PL-8a.

CONCLUSION:

This study shows that diosmin is a potentially effective VRV-PL-5 and VRV-PL-8a.

01 Jan 2023·Annals of surgery

Efficacy and Safety of PL-5 (Peceleganan) Spray for Wound Infections

Article

Author: Liu, Chang ; Zhang, Pihong ; Liu, Wenjun ; Rong, Xinzhou ; Song, Guodong ; Fan, Kunwu ; Zhang, Yi ; Wei, Yating ; Su, Yongtao ; Yu, Jia’ao ; Chen, Mingxia ; Zhu, Feng ; Han, Chunmao ; Xia, Chengde ; Sun, Bingwei ; Li, Yi ; Lv, Guozhong ; Zhao, Yaohua ; Wu, Jun ; Chen, Yuxin ; Zhang, Baolin ; Wang, Lei ; Ji, Geng ; Lai, Wen ; Ahemaiti, Akebaer ; Yu, Xuming ; Lin, Cai ; Chen, Xiaodong ; Dong, Hu ; Wang, Haitao ; Li, Xiaojian ; Zu, Hongxu ; Liu, Jinhui

Objective::

To assess the safety and efficacy of antimicrobial peptide PL-5 (Peceleganan) spray in the treatment of wound infections.

Background::

Antimicrobial peptide PL-5 spray is a novel topical antimicrobial agent.

Methods::

We conducted a multicenter, open-label, randomized, controlled phase IIb clinical trial to evaluate the efficacy and safety of PL-5 spray, as compared with silver sulfadiazine, in patients with skin wound infections. The primary efficacy outcome was the clinical efficacy rate on the first day after ending the treatment (D8). The secondary efficacy outcome was the clinical efficacy rate on the fifth day posttreatment (D5), the bacteria clearance rate, and the overall efficacy rate at the mentioned 2 time points. The safety outcomes included adverse reactions and pharmacokinetic analysis posttreatment.

Results::

A total of 220 patients from 27 hospitals in China were randomly assigned to 4 groups. On D8, the efficacy rate was 100.0%, 96.7%, 96.7% for the 1‰ PL-5, 2‰ PL-5, 4‰ PL-5 groups, respectively, as compared with 87.5% for the control group. The efficacy rate among the 4 groups was significantly different (P<0.05). On D5, the efficacy rate was 100.0%, 93.4%, 98.3% for the 1‰ PL-5, 2‰ PL-5, 4‰ PL-5 groups, respectively, as compared with 82.5% for the control group. The efficacy rate among the 4 groups was significantly different (P<0.05). The blood concentration of PL-5 was not detectable in pharmacokinetic analysis. No severe adverse event related to the application of PL-5 was reported.

Conclusions::

Antimicrobial peptide PL-5 spray is safe and effective for the treatment of skin wound infections.

Trial Registration::

ChiCTR2000033334.

10 Oct 2022·Angewandte Chemie (International ed. in English)

Tandem Electrochemical Oxidative Azidation/Heterocyclization of Tryptophan‐Containing Peptides under Buffer Conditions

Article

Author: Zhuo, Xianfeng ; Xu, Xiaobin ; Chen, Hantao ; Zhang, Yiyang ; Weng, Yiyi

Abstract:

As the aromatic tryptophan (Trp) side chain plays a pivotal role in influencing the structure and function of peptides and proteins, it has become an attractive target for the late‐stage modification of these important biomolecules. Herein, we report an electrochemical approach for late‐stage functionalization of peptides containing a Trp side chain through manganese‐catalyzed tandem radical azidation/heterocyclization. This electrochemical oxidative strategy provides access to azide‐substituted tetrazolo[1,5‐a]indole‐containing peptides with broad functional group tolerance, high site selectivity, and good yields of products (up to 87 %) under mild buffer conditions. Moreover, the modified Trp‐containing peptides bearing an azide functionality are promising building blocks, paving the way for the construction of various derivatives, such as “click” chemistry products.

100 Deals associated with Peceleganan

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Infectious Diseases	NDA/BLA	China	Protelight Pharmaceuticals	24 Dec 2024
Wound Infection	Phase 3	China	Protelight Pharmaceuticals	23 Aug 2021
Bacterial Infections	Phase 2	United States	Protelight Pharmaceuticals	11 May 2023
Secondary infection	Phase 2	China	Protelight Pharmaceuticals	28 Jul 2020
Post-traumatic wound infection	Phase 2	China	Protelight Pharmaceuticals	24 Jul 2018
Diabetic foot infection	Phase 2	United States	Protelight Pharmaceuticals	-
Burn infections	Phase 1	China	Protelight Pharmaceuticals	07 Nov 2016
Diabetic Foot	Phase 1	China	Protelight Pharmaceuticals	07 Nov 2016
Folliculitis	Phase 1	China	Protelight Pharmaceuticals	07 Nov 2016
Impetigo	Phase 1	China	Protelight Pharmaceuticals	07 Nov 2016

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ADA2024 Manual	Not Applicable	Diabetic foot infection	47	PL-5 spray	lldvtctoxq(fzdqsxemtv) = huxvwfdrla vcubfqwitk (sjpgjamjdf ) View more	Positive	21 Jun 2024
				Placebo	lldvtctoxq(fzdqsxemtv) = jndomhrqgk vcubfqwitk (sjpgjamjdf ) View more

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