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 Topoisomerase IV

Mechanism

Bacterial DNA gyrase inhibitors, 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

Hunan Warner Pharmaceutical Factory Chiral Medicine Co Ltd

Guangzhou Boji New Drug Clinical Research Centre

FUJIFILM Toyama Chemical Co., Ltd.

+ [2]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (11 Apr 2002),

Bacterial Infections

Regulation-

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Structure

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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165

Literatures (Medical) associated with Pazufloxacin Mesilate

01 Jan 2023·Journal of Clinical Laboratory Analysis

UHPLC–MS/MS method for simultaneous quantification of doripenem, meropenem, ciprofloxacin, levofloxacin, pazufloxacin, linezolid, and tedizolid in filtrate during continuous renal replacement therapy

Article

Author: Kai, Makoto ; Goto, Koji ; Tatsuta, Ryosuke ; Kitano, Takaaki ; Suzuki, Yosuke ; Itoh, Hiroki ; Yasuda, Norihisa ; Ohchi, Yoshifumi ; Tanaka, Ryota

AbstractBackgroundSince severe infections frequently cause acute kidney injury (AKI), continuous renal replacement therapy (CRRT) is often initiated for regulation of inflammatory mediators and renal support. Thus, it is necessary to decide the antibiotic dosage considering the CRRT clearance in addition to residual renal function. Some of the hemofilters used in CRRT are known to adsorb antibiotics, and clearance of antibiotics may differ depending on the adsorptive characteristics of hemofilters. Although assay systems for blood and CRRT filtrate concentrations are required, no method for measuring antibiotics concentrations in filtrate has been reported. We developed a UHPLC–MS/MS method for simultaneous quantification of antibiotics commonly used in ICU, comprising carbapenems [doripenem (DRPM) and meropenem (MEPM)], quinolones [ciprofloxacin (CPFX), levofloxacin (LVFX) and pazufloxacin (PZFX)] and anti‐MRSA agents [linezolid (LZD), and tedizolid (TZD)] in CRRT filtrate samples.MethodsFiltrate samples were pretreated by protein precipitation. The analytes were separated with an ACQUITY UHPLC CSH C18 column under a gradient mobile phase consisting of water and acetonitrile containing 0.1% formic acid and 2 mM ammonium formate.ResultsThe method showed good linearity over wide ranges. Within‐batch and batch‐to‐batch accuracy and precision for each drug fulfilled the criteria of the US Food and Drug Administration guidance. The recovery rate was more than 87.20%. Matrix effect ranged from 99.57% to 115.60%. Recovery rate and matrix effect did not differ remarkably between quality control samples at different concentrations.ConclusionThis is the first report of a simultaneous quantification method of multiple antibiotics in filtrate of CRRT circuit.

19 Apr 2022·Environmental Science & TechnologyQ1 · ENVIRONMENTAL SCIENCE & ECOLOGY

Interface Engineering of Co(OH)₂ Nanosheets Growing on the KNbO₃ Perovskite Based on Electronic Structure Modulation for Enhanced Peroxymonosulfate Activation

Q1 · ENVIRONMENTAL SCIENCE & ECOLOGY

Article

Author: Wang, Chong-Chen ; Pan, Po-Yueh ; Qi, Juanjuan ; Liu, Wen ; Yang, Xiaoyong ; Yang, Xudong ; Huang, Taobo

Material-enhanced heterogonous peroxymonosulfate (PMS) activation on emerging organic pollutant degradation has attracted intensive attention, and a challenge is the electron transfer efficiency from material to PMS for radical production. Herein, an interface architecture of Co(OH)₂ nanosheets growing on the KNbO₃ perovskite [Co(OH)₂/KNbO₃] was developed, which showed high catalytic activity in PMS activation. A high reaction rate constant (k₁) of 0.631 min^-1 and complete removal of pazufloxacin within 5 min were achieved. X-ray photoelectron spectroscopy, X-ray absorption near edge structure spectra, and density functional theory (DFT) calculations revealed the successful construction of the material interface and modulated electronic structure for Co(OH)₂/KNbO₃, resulting in the hole accumulation on Co(OH)₂ and electron accumulation on KNbO₃. Bader topological analysis on charge density distribution further indicates that the occupations of Co-3d and O-2p orbitals in Co(OH)₂/KNbO₃ are pushed above the Fermi level to form antibonding states (σ*), leading to high chemisorption affinity to PMS. In addition, more reactive Co(II) with the closer d-band center to the Fermi level results in higher electron transfer efficiency and lower decomposition energy of PMS to SO₄^•-. Moreover, the reactive sites of pazufloxacin for SO₄^•- attack were precisely identified based on DFT calculation on the Fukui index. The pazufloxacin pathways proceeded as decarboxylation, nitroheterocyclic ring opening reaction, defluorination, and hydroxylation. This work can provide a potential route in developing advanced catalysts based on manipulation of the interface and electronic structure for enhanced Fenton-like reaction such as PMS activation.

01 Dec 2021·International Journal of ToxicologyQ4 · MEDICINE

Evaluation of the Expression Profile of Antibiotic-Induced Thrombocytopenia Using the Japanese Adverse Drug Event Report Database

Q4 · MEDICINE

Article

Author: Abe, Yasuharu ; Asai, Yuki ; Yamamoto, Takanori

Drug-induced thrombocytopenia (DITP) can be triggered by antibiotics; however, the details remain unclear. Here, we evaluated the expression profiles of DITP using the Japanese Adverse Drug Event Report (JADER) database. We analyzed reports of DITP between April 2004 and January 2021 from the JADER database. The reporting odds ratio (ROR) and 95% confidence interval (CI) were used to detect DITP signals. Factors thought to affect DITP, such as male sex and an age of at least 60 years, were added as covariates. We evaluated the time-to-onset profile and hazard type using the Weibull shape parameter. The JADER database contained 1,048,576 reports. Twelve of 60 antibiotics showed signals for DITP; the RORs (95% CIs) for ampicillin/sulbactam, ceftazidime, cefozopran, ciprofloxacin, fluconazole, fos-fluconazole, linezolid, pazufloxacin, piperacillin/tazobactam, teicoplanin, trimethoprim/sulfamethoxazole, and voriconazole were 1.75 (1.41-2.16), 1.77 (1.42-2.18), 1.35 (1.06-1.72), 2.56 (2.19-2.98), 1.93 (1.67-2.23), 2.08 (1.76-2.46), 5.29 (2.73-9.60), 1.92 (1.51-2.41), 1.54 (1.05-2.19), 1.47 (1.16-1.84), 1.92 (1.73-2.14), and 2.32 (1.59-3.30), respectively. In multiple logistic regression analysis, 7 and 6 antibiotics were detected for the factors age and male sex, respectively. The median times-to-onset of DITP for ciprofloxacin (oral treatment), fluconazole, linezolid, piperacillin/tazobactam, and trimethoprim/sulfamethoxazole were 91, 91, 11.5, 10, and 9 days, respectively. Furthermore, the 95% CI of the Weibull shape parameter β for these antibiotics was above and excluded 1, indicating that the antibiotics were the wear out failure type. We revealed the expression profiles of DITP following treatment with 12 antibiotics.

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	CN	Hunan Warner Pharmaceutical Factory Chiral Medicine Co Ltd	01 Jan 2004
Bacterial Infections	JP	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	CN	Guangzhou Boji New Drug Clinical Research Centre	27 Jul 2018

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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)	jwajkhlccx(ewfohmzyhc) = wtttfbomuu ilaamuqitt (vmkexiiqkc, olxxkybpvt - kblfhwsiam) View more	-	24 Aug 2021
				Zymar (Zymar)	jwajkhlccx(ewfohmzyhc) = pqxjqpyshl ilaamuqitt (vmkexiiqkc, uaasokqsgx - tnxvoimzpw) View more
NCT02980523 (Pazufloxacin, CTgov)	Phase 2	Conjunctivitis, Bacterial	150	Lagricel Ofteno®+PRO-157 (PRO-157 BID (2 Times Per Day))	vcnlhawlug(wuatknkxhw) = jqzyqgkmjg rfwsrnnmni (rmasisyomw, pclxutxpal - eiegfqdlvu) View more	-	15 Feb 2019
				Lagricel Ofteno®+PRO-157 (PRO-157 TID (3 Times Per Day))	vcnlhawlug(wuatknkxhw) = buxsxddocg rfwsrnnmni (rmasisyomw, apkszthqnh - enktntohbw) View more