甲磺酸帕珠沙星(Pazufloxacin Mesilate) - 药物靶点：Bacterial DNA gyrase x Topoisomerase IV_在研适应症：感染，细菌感染，慢性化脓性中耳炎_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Pazufloxacin、Pazufloxacin Mesilate Sodium Chloride、Pazufloxacin Mesilate and Sodium Chloride

+ [36]

靶点

Bacterial DNA gyrase x Topoisomerase IV

作用机制

细菌DNA旋转酶复合体抑制剂、拓扑异构酶 IV抑制剂

治疗领域

感染耳鼻咽喉疾病其他疾病

在研适应症

感染细菌感染慢性化脓性中耳炎+ [1]

非在研适应症-

原研机构

Taisho Toyama Pharmaceutical Co., Ltd.

在研机构

湖南华纳大药厂手性药物有限公司

广州博济新药临床研究中心有限公司

Mitsubishi Tanabe Pharma Corp.

+ [2]

非在研机构-

最高研发阶段批准上市

首次获批日期

日本 (2002-04-11),

细菌感染

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C17H19FN2O7S

InChIKeyUDHGFPATQWQARM-FJXQXJEOSA-N

CAS号163680-77-1

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关联

11

项与甲磺酸帕珠沙星相关的临床试验

NCT03696342 / Terminated临床3期

Clinical Study of the Efficacy of the Ophthalmic Solution of Pazufloxacin 0.6% (PRO-157) for the Treatment of Acute Bacterial Conjunctivitis, Compared to the Ophthalmic Solution of Gatifloxacin 0.3%.

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).

开始日期2018-10-01

申办/合作机构

Laboratorios Sophia SA de CV

NCT03675841 / Unknown status临床1期

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.

开始日期2018-07-29

申办/合作机构

李氏大药厂控股有限公司

CTR20171248 / Recruiting临床1期

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

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。

开始日期2018-07-27

申办/合作机构

广州博济新药临床研究中心有限公司

100 项与甲磺酸帕珠沙星相关的临床结果

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100 项与甲磺酸帕珠沙星相关的转化医学

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100 项与甲磺酸帕珠沙星相关的专利（医药）

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166

项与甲磺酸帕珠沙星相关的文献（医药）

2023-01-01·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

作者: Goto, Koji ; Kai, Makoto ; 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.

2022-04-19·Environmental Science & Technology1区 · 环境科学与生态学

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

1区 · 环境科学与生态学

Article

作者: 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.

2021-12-01·International Journal of Toxicology4区 · 医学

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

4区 · 医学

Article

作者: 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.

2

项与甲磺酸帕珠沙星相关的新闻（医药）

2024-04-17

·米内网

【瞩目】10亿注射剂，四川药企获批了

精彩内容4月16日，NMPA官网显示，四川美大康佳乐药业的盐酸乌拉地尔注射液获批上市并视同过评。盐酸乌拉地尔注射液为静脉降压药，2022年在中国公立医疗机构终端销售额超过10亿元。乌拉地尔是由武田研发的一种选择性α1受体阻滞剂，具有外周和中枢双重降压作用。盐酸乌拉地尔注射液主要适用于高血压危象以及控制围手术期高血压，在临床上应用甚广，是急诊室常备急救药品之一。米内网数据显示，2022年中国城市公立医院、县级公立医院、城市社区中心以及乡镇卫生院（简称中国公立医疗机构）终端盐酸乌拉地尔注射液销售额超过10亿元，2023年上半年其销售额超过5亿元，同比增长8.77%。中国公立医疗机构终端盐酸乌拉地尔注射液销售情况（单位：万元）来源：米内网中国公立医疗机构药品终端竞争格局此前国内已有16家企业获得了盐酸乌拉地尔注射液的生产批文，包括西安利君制药、罗欣药业、河北一品制药、锦州奥鸿药业、石家庄四药、青峰药业等，四川美大康佳乐药业为该药国产第17家。该药还有科伦药业、正大丰海、天方药业等20家企业的上市申请在审中。四川美大康佳乐药业于2001年在成都市高新技术开发区西区注册成立，是一家以新药研发、液体制剂生产销售为主的综合性现代制药企业。四川美大康佳乐药业过评品种来源：米内网一致性评价进度数据库目前，四川美大康佳乐药业已有9款注射剂过评，包括盐酸乌拉地尔注射液、甘油果糖氯化钠注射液、甲磺酸帕珠沙星氯化钠注射液、伊班膦酸钠注射液、盐酸替罗非班氯化钠注射液、利奈唑胺葡萄糖注射液、多西他赛注射液、乳酸环丙沙星氯化钠注射液、碳酸氢钠林格注射液等。资料来源：米内网数据库、NMPA注：米内网《中国公立医疗机构药品终端竞争格局》，统计范围是：中国城市公立医院、县级公立医院、城市社区中心以及乡镇卫生院，不含民营医院、私人诊所、村卫生室；上述销售额以产品在终端的平均零售价计算。本文为原创稿件，转载请注明来源和作者，否则将追究侵权责任。投稿及报料请发邮件到872470254@qq.com稿件要求详询米内微信首页菜单栏商务及内容合作可联系QQ：412539092【分享、点赞、在看】点一点不失联哦

一致性评价上市批准

2021-02-22

·药融圈

来自东阳：低调API药企拟上市

▲速抢免费参会名额 | 大湾区(广州)生物医药创新者峰会 01 浙江海森药业股份有限公司地处东阳市六石街道，从事原料药、医药中间体研发、生产、经营，为国家高新技术企业。公司占地面积7万平方米，现有员工 400多人，其中专业技术人员 30%以上。公司2001年通过ISO9001：2000国际质量体系认证。2006年首次通过国内GMP认证，同年获得欧盟CEP证书，2014年首次通过美国FDA现场审计。公司现有主导产品为原料药：硫糖铝、安乃近、甲磺酸帕珠沙星、阿托伐他汀钙、盐酸帕罗西汀、草酸艾司西酞普兰 ; 中间体：PHBA 、甲基帕罗西汀等。目前已有多个品种获得美国、欧盟、日本、韩国、印度、巴西、墨西哥等国家的注册。其中硫糖铝产品世界市场的占有率达60％以上。遵循“顾客至上、环境为本、质量领先、持续改进”的质量环境方针，公司不断加大高新技术研发及投入力度，从中获取更多经济效益和增长点。公司与四川抗菌素工业研究所、上海医工院、天津药物研究院、浙江大学等科研机构多年来建立了良好的长期合作关系，浙江省级技术中心、浙江省海森药物研究院及海森药业院士专家工作站的先后组建，让公司技术中心研发水平达到同领域国内领先。浙江海森药业股份有限公司与浙江金华康恩贝生物制药有限公司联合开发的草酸艾司西酞普兰片（商标名泰齐）已上市，由海森药业安排全国销售、招商，欢迎合作发展。 02 药融圈获悉，公司目前情况：辅导备案就位，正在上市辅导中。 03 股东构成：更多信息，请扫免费的药融云数据或网站www.pharnexcloud.com 【关于药融圈】药融圈围绕我国生物医药产业链，针对生物医药大数据、技术和资本投资、药融园(产业园)等开展系列系统性工作，促进我国生物医药产业健康发展，完善产业链，共同面对全球合作和竞争。点分享点点赞点在看

合作IPO生物类似药创新药

100 项与甲磺酸帕珠沙星相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	甲磺酸帕珠沙星	J01MA18	DB11774

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
感染	中国	湖南华纳大药厂手性药物有限公司	2004-01-01
细菌感染	日本	FUJIFILM Toyama Chemical Co. Ltd.	2002-04-11

未上市

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
慢性化脓性中耳炎	临床1期	中国	广州博济新药临床研究中心有限公司	2018-07-27
中耳炎	临床1期	中国	广州博济新药临床研究中心有限公司	2015-07-24

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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


NCT03696342 (CTgov)	临床3期	急性细菌性结膜炎	46	Pazufloxacin (PRO-157)	築憲蓋憲憲遞顧淵淵遞(夢襯膚鬱願鏇淵遞窪積) = 鑰鑰遞繭蓋醖顧衊艱築淵願淵餘範積觸廠願鬱 (鑰積壓壓鬱築壓鹹醖繭, 廠襯網製憲糧艱構憲夢 ~ 願願糧鹹艱衊鬱觸鹽築) 更多	-	2021-08-24
				Zymar (Zymar)	築憲蓋憲憲遞顧淵淵遞(夢襯膚鬱願鏇淵遞窪積) = 構範鬱鏇餘鬱廠鏇獵夢淵願淵餘範積觸廠願鬱 (鑰積壓壓鬱築壓鹹醖繭, 憲鹹艱顧積網淵選膚醖 ~ 憲遞願餘製觸鬱遞膚網) 更多
NCT02980523 (CTgov)	临床2期	细菌性结膜炎	150	Lagricel Ofteno®+PRO-157 (PRO-157 BID (2 Times Per Day))	觸蓋鏇範艱獵獵壓鏇膚(窪糧夢鹹鹽築網衊鹹獵) = 鬱憲鏇餘蓋糧艱觸觸憲膚鹹鹹範願構繭範範觸 (鬱鑰鑰繭餘糧網憲壓簾, 餘鬱衊鏇淵積製獵築壓 ~ 窪醖製顧糧膚獵鬱築膚) 更多	-	2019-02-15
				Lagricel Ofteno®+PRO-157 (PRO-157 TID (3 Times Per Day))	觸蓋鏇範艱獵獵壓鏇膚(窪糧夢鹹鹽築網衊鹹獵) = 構鹽淵艱糧壓蓋鹹繭淵膚鹹鹹範願構繭範範觸 (鬱鑰鑰繭餘糧網憲壓簾, 選範鬱膚鏇鏇願蓋築簾 ~ 鑰願鹹齋遞遞遞繭鏇積) 更多