Delving into the Latest Updates on Pazufloxacin Mesilate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Pazufloxacin, Pazufloxacin Mesilate Sodium Chloride, Pazufloxacin Mesilate and Sodium Chloride

+ [36]

Target

Bacterial DNA gyrase x Bacterial top IV

Action

inhibitors

Mechanism

Bacterial DNA gyrase inhibitors(Bacterial DNA gyrase inhibitors), Bacterial top IV inhibitors(Bacterial topoisomerase IV inhibitors)

Therapeutic Areas

Infectious DiseasesOtorhinolaryngologic DiseasesOther Diseases

Active Indication

Infectious DiseasesBacterial InfectionsChronic purulent otitis media

Inactive Indication-

Originator Organization

Taisho Toyama Pharmaceutical Co., Ltd.

Active Organization

Guangzhou Boji New Drug Clinical Research Centre

Hunan Warner Pharmaceutical Factory Chiral Medicine Co Ltd

Mitsubishi Tanabe Pharma Corp.

+ [2]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (11 Apr 2002),

Bacterial Infections

Regulation-

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Structure/Sequence

Molecular FormulaC17H19FN2O7S

InChIKeyUDHGFPATQWQARM-FJXQXJEOSA-N

CAS Registry163680-77-1

View All Structures (2)

Phase III clinical study of non-inferiority, multicenter, double-blind, with comparative group, of parallel groups and randomized. about a ophthalmic topical antibiotic for the treatment of bacterial conjunctivitis.
Goal:To compare the efficacy of the ophthalmic solution of pazufloxacin 0.6%, against the ophthalmic solution of gatifloxacin 0.3%, in the treatment of acute bacterial conjunctivitis.
Hypothesis:the ophthalmic solution PRO-157 is not inferior in the treatment of bacterial conjunctivitis, compared to the ophthalmic solution of gatifloxacin 0.3%, by means of the clinical remission of the disease.
Number of patients:
160 patients, each one will provide an eye for efficacy analysis, divided into 2 groups (80 eyes per group).

Start Date01 Oct 2018

Sponsor / Collaborator

Laboratorios Sophia SA de CV

NCT03675841

/ Unknown statusPhase 1

A Phase I，Pazufloxacin Mesilate Ear Drops in Patients With Chronic Suppurative Otitis Media

Objective To observe the safety and tolerability of Pazufloxacin Mesylate Ear Drops of different concentrations in patients with simple chronic suppurative otitis media.

Start Date29 Jul 2018

Sponsor / Collaborator

Lee's Pharmaceutical Holdings Ltd.

CTR20171248

/ RecruitingPhase 1

甲磺酸帕珠沙星滴耳液在慢性化脓性中耳炎患者中单次给药的I期临床试验

[Translation] Phase I clinical trial of single-dose pazufloxacin mesylate ear drops in patients with chronic suppurative otitis media

观察不同浓度甲磺酸帕珠沙星滴耳液单次给药在单纯型慢性化脓性中耳炎活动期患者的安全性和耐受性，以及评价甲磺酸帕珠沙星滴耳液的局部药代动力学和全身药代动力学。

[Translation]

To observe the safety and tolerability of a single dose of different concentrations of pazufloxacin mesylate ear drops in patients with active simple chronic suppurative otitis media, and to evaluate the local and systemic pharmacokinetics of pazufloxacin mesylate ear drops.

Start Date27 Jul 2018

Sponsor / Collaborator

Guangzhou Boji New Drug Clinical Research Centre

100 Clinical Results associated with Pazufloxacin Mesilate

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100 Translational Medicine associated with Pazufloxacin Mesilate

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100 Patents (Medical) associated with Pazufloxacin Mesilate

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674

Literatures (Medical) associated with Pazufloxacin Mesilate

24 Mar 2025·Journal of Biomolecular Structure and Dynamics

Inhibition of respiratory syncytial virus by Daclatasvir and its derivatives: synthesis of computational derivatives as a new drug development

Article

Author: Afreen, Shagufta ; Mitra, Debanjan ; Abdalla, Mohnad ; Das Mohapatra, Pradeep K.

The most common cause of respiratory tract illness in newborns and young children is the respiratory syncytial virus (RSV). There is no approved vaccination or specific antiviral medication for RSV infections. Here, an attempt has been made to explore the potential of currently marketed drugs as well as their probable derivatives to improve the possibility of developing stronger medications against RSV. From the 100 synthetic drug compounds library, the best drug molecule was identified through drug-likeness properties, toxicity, molecular docking and molecular dynamics simulations. Molecular Mechanics Generalized Born Surface Area (MM-GBSA) was also a method that was applied in this study. Daclatasvir showed the highest binding energy and appeared as the best drug to inhibit matrix protein and a fusion protein of RSV. Based on Daclatasvir, 40 computational derivatives were made. D28, D34 and D40 showed far better results than the actual drug. Changes in lipophilicity character increase the binding energy of derivatives. Molecular dynamic simulations showed their non-deviated, non-fluctuated and stable complex formation with target proteins. The high number of amino acid contacts throughout the trajectory increases the stability and effectiveness of derivatives. The key to producing a novel medicine to eradicate RSV is provided by derivatives. Daclatasvir will be employed as a potential RSV inhibitor up until that point.Communicated by Ramaswamy H. Sarma.

01 Mar 2025·Journal of Hazardous Materials

Hepatotoxicity, developmental toxicity, and neurotoxicity risks associated with co-exposure of zebrafish to fluoroquinolone antibiotics and tire microplastics: An in silico study

Article

Author: Liu, Yajing ; Ding, Xiaowen ; Xiao, Botian ; Li, Yu ; Li, Xixi ; Zhang, Zuning ; Wen, Jingya ; Qian, Feng ; Pu, Qikun

This study aimed to investigate the differences in the mechanisms of microscopic hepatotoxicity, developmental toxicity, and neurotoxicity in aquatic organisms co-exposed to styrene-butadiene rubber tire microplastics (SBR TMPs) and fluoroquinolone antibiotics (FQs). We found that hepatotoxicity in zebrafish induced by SBR TMPs and FQs was significantly higher than developmental toxicity and neurotoxicity. Furthermore, the main effects of the FQs primarily manifested as synergistic toxicity, whereas the low- and high-order interactions of the FQs mainly exhibited synergistic and antagonistic effects, respectively. Factorial analysis and the mixture toxicity index revealed that the synergistic effects of lomefloxacin × moxifloxacin and ciprofloxacin × lomefloxacin × enrofloxacin interactions significantly contributed to hepatotoxicity in zebrafish exposed to SBR TMP. SBR TMPs and antibiotics primarily induced hepatotoxicity, developmental toxicity, and neurotoxicity in zebrafish by affecting the activities of Cyp1a, Acox1, TRα, and mAChR. The observed toxicities were closely linked to the hydrophilic/hydrophobic groups, electronegativity, group mass, and structural complexity of the FQ molecules. This study provides new insights regarding the toxicological risks to aquatic organisms from co-exposure to SBR TMPs and FQs from a microscopic perspective. Future studies should include a broader range of antibiotics and tire microplastics and consider their long-term adverse effects on aquatic life.

01 Sep 2024·Journal of Hazardous Materials

In silico degradation of fluoroquinolones by a microalgae-based constructed wetland system

Article

Author: Wu, Fuxing ; Hao, Ning ; Du, Meijin ; Li, Xixi ; Wang, Renjie ; Wang, Zini ; Ling, Jianglong

Fluoroquinolone antibiotics (FQs) have been used worldwide due to their extended antimicrobial spectrum. However, the overuse of FQs leads to frequent detection in the environment and cannot be efficiently removed. Microalgae-based constructed wetland systems have been proven to be a relatively proper method to treat FQs, mainly by microalgae, plants, microorganisms, and sediments. To improve the removal efficiency of microalgae-constructed wetland, a systematic molecular design, screening, functional, and risk evaluation method was developed using three-dimensional quantitative structure-activity relationship models, molecular dynamics simulation, molecular docking, and TOPKAT approaches. Five designed ciprofloxacin alternatives with improved bactericidal effects and lower human health risks were found to be more easily degraded by microalgae (16.11-167.88 %), plants (6.72-58.86 %), microorganisms (9.10-15.02 %), and sediments (435.83 %-1763.51 %) compared with ciprofloxacin. According to the mechanism analysis, the removal effect of the FQs can be affected via changes in the number, bond energy, and molecular descriptors of favorable and unfavorable amino acids. To the best of our knowledge, this is the first comprehensive study of improving the microalgae, plants, microorganisms, and sediment removal efficiency of FQs in constructed wetlands, which provides theoretical support for the treatment of FQ pollution.

100 Deals associated with Pazufloxacin Mesilate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Pazufloxacin Mesilate	J01MA18	DB11774

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Infectious Diseases	China	Hunan Warner Pharmaceutical Factory Chiral Medicine Co Ltd	01 Jan 2004
Bacterial Infections	Japan	FUJIFILM Toyama Chemical Co., Ltd.	11 Apr 2002

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic purulent otitis media	Phase 1	China	Guangzhou Boji New Drug Clinical Research Centre	24 Jul 2015

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03696342 (PRO-157, CTgov)	Phase 3	acute bacterial conjunctivitis	46	Pazufloxacin (PRO-157)	mozxnvbxnz(tfwhidpkjf) = xqfcdylelb eohbrplqxa (ylfuibomtf, zaxjipbfye - adyyseztwi) View more	-	24 Aug 2021
				Zymar (Zymar)	mozxnvbxnz(tfwhidpkjf) = tfcjbhbrhv eohbrplqxa (ylfuibomtf, kvchxxfnwl - dzfxsovuxh) View more
NCT02980523 (Pazufloxacin, CTgov)	Phase 2	Conjunctivitis, Bacterial	150	Lagricel Ofteno®+PRO-157 (PRO-157 BID (2 Times Per Day))	cyptwppykp(yfnkpnapej) = cucweffwwm lhlfygbsjx (ifqkfznqfs, bcapdmawyp - mnvcrdlyqg) View more	-	15 Feb 2019
				Lagricel Ofteno®+PRO-157 (PRO-157 TID (3 Times Per Day))	cyptwppykp(yfnkpnapej) = jpkedgneon lhlfygbsjx (ifqkfznqfs, gpvjsyazel - bqugemilst) View more