扎波沙星(Zabofloxacin Hydrochloride) - 药物靶点：VEGFR1_在研适应症：慢性阻塞性肺疾病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [2]

靶点

VEGFR1

作用方式

调节剂

作用机制

VEGFR1调节剂(血管内皮细胞生长因子受体1调节剂)

治疗领域

呼吸系统疾病

在研适应症

慢性阻塞性肺疾病

非在研适应症-

原研机构

DONG WHA PHARM Co., Ltd.

在研机构-

非在研机构

DONG WHA PHARM Co., Ltd.

权益机构

Austell Pharmaceuticals (Pty) Ltd.

DONG WHA PHARM Co., Ltd.

最高研发阶段批准上市

首次获批日期

韩国 (2015-03-20),

慢性阻塞性肺疾病

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C19H20FN5O4

InChIKeyZNPOCLHDJCAZAH-UHFFFAOYSA-N

CAS号219680-11-2

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关联

5

项与扎波沙星相关的临床试验

NCT02212795

/ Completed临床1期

Phase I Study of Pharmacokinetics and Bacteriocidal Activity

Phase I clinical study to compare the pharmacokinetic profiles and bactericidal activity of Zabofloxacin 183mg, 367mg and Levofloxacin 250mg after oral administration in healthy volunteer

开始日期2014-05-01

申办/合作机构

DONG WHA PHARM Co., Ltd.

NCT01658020

/ Completed临床3期

Clinical Trials to Evaluate Efficacy and Safety of Zabofloxacin Tablet 400mg and Moxifloxacin Tablet 400mg After Multi-dose Oral Administration in Patients With Acute Bacterial Exacerbation of Chronic Obstructive Pulmonary Disease.

The purpose of this study is to Evaluate the Efficacy and Safety Profiles of oral multiple dose of Zabofloxacin Tablet 400 mg.

开始日期2012-08-01

申办/合作机构

DONG WHA PHARM Co., Ltd.

[+24]

NCT01341249

/ Completed临床1期IIT

Clinical Trial to Compare the Pharmacokinetic Profiles of DW224aa (Aspartate) Tablet and DW224a (Hydrochloride) Capsule After a Single Oral Administration in Healthy Male Volunteers

The purpose of this study is to compare and explore pharmacokinetics of zabofloxacin, the main component of DW224aa(Test drug) and DW224a(Reference drug).

开始日期2011-04-01

申办/合作机构

Seoul National University Hospital

[+1]

100 项与扎波沙星相关的临床结果

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100 项与扎波沙星相关的转化医学

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100 项与扎波沙星相关的专利（医药）

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50

项与扎波沙星相关的文献（医药）

2023-10-12·Cureus

Advancements in the Management of Severe Community-Acquired Pneumonia: A Comprehensive Narrative Review

Review

作者: Carson, Bryan J ; Ali, Mujahaith ; Nausheem, Reem ; Choudhary, Vatsalya ; Nagarajan, Lavanya ; Thadhani, Jainisha ; Davis, Don ; Kanwal, Fnu ; Vallejo-Zambrano, Cristhian R ; Mohammad Arifuddin, Bushra

Pneumonia, classified as a lower respiratory tract illness, affects different parts of the bronchial system as well as alveoli and can present with varying severities depending on co-morbidities and causative pathogens. It can be broadly classified using the setting in which it was acquired, namely the community or hospital setting, the former being more common and spreading through person-to-person droplet transmission. Community-acquired pneumonia (CAP) is currently the fourth leading cause of death worldwide, and its high mortality makes continual insight into the management of the condition worthwhile. This review explores the literature specifically for severe CAP (sCAP) and delves into the diagnosis, various modalities of treatment, and management of the condition. This condition can be defined as pneumonia requiring mechanical ventilation in the ICU and/or presenting with sepsis and organ failure due to pneumonia. The disease process is characterized by inflammation of the lung parenchyma, initiated by a combination of pathogens and lowered local defenses. Acute diagnosis of the condition is vital in reducing negative patient outcomes, namely through clinical presentation, blood/sputum cultures, imaging modalities such as computed tomography scan, and inflammatory markers, identifying common causative pathogens such as Streptococcus pneumoniae, rhinovirus, Legionella, and viral influenza. Pathogens such as Escherichia coli should also be investigated in patients with chronic obstructive pulmonary disease. The mainstay of treating sCAP includes rapid ICU admission once a diagnosis has been confirmed, initiating sepsis protocol, and treatment with combined empiric antibiotic regimens consisting of beta-lactams and macrolides. Corticosteroid use alongside antibiotics shows promise in reducing inflammation, but its use has to be judged on a case-by-case basis. New drugs such as omadacycline, delafloxacin, and zabofloxacin have shown valid evidence for the treatment of resistant causative organisms. The main guidelines for preventing sCAP include maintaining a healthy lifestyle, and annual pneumococcal and influenza vaccines are recommended for the most vulnerable patient groups, such as those with COPD and immunosuppression.

2022-11-24·Journal of Biomolecular Structure and Dynamics

Virtual screening of quinoline derived library for SARS-COV-2 targeting viral entry and replication

Article

作者: Chaudhary, Vishakha ; Anju, Anju ; Mishra, Anil Kumar ; Chaturvedi, Shubhra ; Pant, Pradeep ; Hussain, Firasat

The COVID-19 pandemic infection has claimed many lives and added to the social, economic, and psychological distress. The contagious disease has quickly spread to almost 218 countries and territories following the regional outbreak in China. As the number of infected populations increases exponentially, there is a pressing demand for anti-COVID drugs and vaccines. Virtual screening provides possible leads while extensively cutting down the time and resources required for ab-initio drug design. We report structure-based virtual screening of a hundred plus library of quinoline drugs with established antiviral, antimalarial, antibiotic or kinase inhibitor activity. In this study, targets having a role in viral entry, viral assembly, and viral replication have been selected. The targets include: 1) RBD of receptor-binding domain spike protein S 2) M^pro Chymotrypsin main protease 3) P^pro Papain protease 4) RNA binding domain of Nucleocapsid Protein, and 5) RNA Dependent RNA polymerase from SARS-COV-2. An in-depth analysis of the interactions and G-score compared to the controls like hydroxyquinoline and remdesivir has been presented. The salient results are (1) higher scoring of antivirals as potential drugs (2) potential of afatinib by scoring as better inhibitor, and (3) biological explanation of the potency of afatinib. Further MD simulations and MM-PBSA calculations showed that afatinib works best to interfere with the the activity of RNA dependent RNA polymerase of SARS-COV-2, thereby inhibiting replication process of single stranded RNA virus. Communicated by Ramaswamy H. Sarma.

2022-07-01·Journal of Thoracic Disease

Bacterial etiology and pneumococcal urinary antigen in moderate exacerbation of chronic obstructive pulmonary disease

Article

作者: Jung, Chi Young ; Na, Ju Ock ; Oh, Yeon-Mok ; Yoo, Jungmin ; Ra, Seung Won ; Kim, Tae-Hyung

BackgroundThis study aimed to establish nationwide data for the distributions of typical and atypical bacterial pathogens in Korean patients with moderate acute exacerbations of chronic obstructive pulmonary disease (AECOPD) and evaluate the clinical usefulness of a urinary antigen test (UAT) to detect Streptococcus pneumoniae.MethodsThis study was a post hoc analysis of a randomized controlled trial designed to compare oral zabofloxacin with moxifloxacin for treating outpatients with moderate AECOPD. From clinics across South Korea, 342 subjects with AECOPD were enrolled, and their blood, sputum, and urine samples were collected at baseline. A serologic test, sputum culture and polymerase chain reaction (PCR), and UAT were performed to identify bacterial pathogens. Bacterial prevalence and regional distributions were analyzed. The patients' characteristics and clinical response between UAT-positive and UAT-negative groups were compared, as were the Streptococcus pneumoniae detection rates using conventional sputum culture and PCR versus UAT.ResultsThe most commonly isolated pathogen was Haemophilus influenzae (30.3%), followed by Streptococcus pneumoniae (24.7%) and Pseudomonas aeruginosa (14.0%), with no significant regional differences in bacterial distribution. Patients with positive UAT for Streptococcus pneumoniae showed no clinical failure when treated with respiratory quinolone (0.0%), whereas 11.8% of patients with negative UAT showed clinical failure (P=0.037). UAT showed moderate agreement with sputum culture by kappa coefficient (κ=0.476).ConclusionsThe bacterial prevalence in patients with moderate AECOPD in South Korea showed correlations with the global prevalence, without significant regional differences. In outpatient settings, UAT has the potential to be used as a supplemental tool with sputum culture as a guide for determining the suspicion of bacterial exacerbation.

100 项与扎波沙星相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	扎波沙星	J01MA	DB12479

研发状态

批准上市

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适应症	国家/地区	公司	日期
慢性阻塞性肺疾病	韩国	-	2015-03-20

未上市

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适应症	最高研发状态	国家/地区	公司	日期
慢性阻塞性肺疾病	临床前	韩国	DONG WHA PHARM Co., Ltd.	2012-08-01

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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


NCT01658020 (Pubmed \| Int J Chron Obstruct Pulmon Dis) 人工标引	临床3期	慢性阻塞性肺疾病	345	Zabofloxacin	(顧顧衊憲蓋糧遞願觸鹹) = 選築鑰醖鏇鏇鹹餘顧糧願艱獵獵選艱夢觸鏇繭 (選蓋壓壓膚遞繭網夢鬱 ) 更多	优效	2015-10-22
				moxifloxacin	(顧顧衊憲蓋糧遞願觸鹹) = 繭構遞鑰艱鏇廠醖鏇積願艱獵獵選艱夢觸鏇繭 (選蓋壓壓膚遞繭網夢鬱 ) 更多
NCT01658020 (DW224-III-3, CTgov)	临床3期	慢性阻塞性肺疾病	345	Zabofloxacin (DW224)	襯鹽衊選廠淵鹹顧繭顧(膚窪觸壓廠鹽製窪襯遞) = 憲廠蓋夢餘觸願顧蓋鬱窪夢淵顧壓鏇艱衊廠醖 (願範選襯鬱窪蓋顧製觸, 構築襯鑰遞鹽範憲願選 ~ 窪衊範範鹽糧糧夢憲獵) 更多	-	2014-09-17
				moxifloxacin (Avelox)	襯鹽衊選廠淵鹹顧繭顧(膚窪觸壓廠鹽製窪襯遞) = 壓膚網齋醖範積淵願構窪夢淵顧壓鏇艱衊廠醖 (願範選襯鬱窪蓋顧製觸, 蓋襯選醖淵壓壓製願選 ~ 膚夢齋齋構簾夢選蓋積) 更多