Delving into the Latest Updates on Zabofloxacin Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [2]

Target

VEGFR1

Action

modulators

Mechanism

VEGFR1 modulators(Vascular endothelial growth factor receptor 1 modulators)

Therapeutic Areas

Respiratory Diseases

Active Indication

Pulmonary Disease, Chronic Obstructive

Inactive Indication-

Originator Organization

DONG WHA PHARM Co., Ltd.

Active Organization-

Inactive Organization

DONG WHA PHARM Co., Ltd.

License Organization

Austell Pharmaceuticals (Pty) Ltd.

DONG WHA PHARM Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

South Korea (20 Mar 2015),

Pulmonary Disease, Chronic Obstructive

Regulation-

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Structure/Sequence

Molecular FormulaC19H20FN5O4

InChIKeyZNPOCLHDJCAZAH-UHFFFAOYSA-N

CAS Registry219680-11-2

View All Structures (2)

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.

24 Nov 2022·Journal of Biomolecular Structure and Dynamics

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

Article

Author: 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.

01 Jul 2022·Journal of Thoracic Disease

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

Article

Author: 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 Deals associated with Zabofloxacin Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Zabofloxacin Hydrochloride	J01MA	DB12479

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Pulmonary Disease, Chronic Obstructive	South Korea	-	20 Mar 2015

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pulmonary Disease, Chronic Obstructive	Preclinical	South Korea	DONG WHA PHARM Co., Ltd.	01 Aug 2012

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01658020 (Pubmed \| Int J Chron Obstruct Pulmon Dis) Manual	Phase 3	Pulmonary Disease, Chronic Obstructive	345	Zabofloxacin	(wrzgyiqhcq) = lnmvmazvpu laasmjinxa (ghyeoxvuer ) View more	Superior	22 Oct 2015
				moxifloxacin	(wrzgyiqhcq) = okhnthhbxh laasmjinxa (ghyeoxvuer ) View more
NCT01658020 (DW224-III-3, CTgov)	Phase 3	Pulmonary Disease, Chronic Obstructive	345	Zabofloxacin (DW224)	tzzqtyozet(ilwrtkytgz) = irjchveaea nqbijqgqpj (hjedydxbdi, kbykqojqfi - lbiaseoafq) View more	-	17 Sep 2014
				moxifloxacin (Avelox)	tzzqtyozet(ilwrtkytgz) = msdiztvwtn nqbijqgqpj (hjedydxbdi, npzpdaxvvx - xlbzczwgmo) View more