Delving into the Latest Updates on Gatifloxacin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

1-Cyclopropyl-1,4-dihydro-6-fluoro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro- 8-methoxy-7-(3-methylpiperazin-1-yl)- 4-oxo-quinoline-3-carboxylic acid, Bonoq

+ [101]

Target

Bacterial DNA gyrase x Bacterial top IV

Mechanism

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

Therapeutic Areas

Infectious DiseasesEye DiseasesOtorhinolaryngologic Diseases+ [2]

Active Indication

Conjunctivitis, BacterialBlepharitisCorneal Ulcer+ [7]

Inactive Indication

Acute bacterial bronchitisAcute sinusitisAnthrax+ [6]

Originator Organization

Bristol Myers Squibb Co.

Active Organization

Senju Pharmaceutical Co., Ltd.

AbbVie, Inc.

Sino-American Shanghai Squibb Pharmaceuticals Ltd.

Inactive Organization

Bristol Myers Squibb Co.Allergan Ltd. (Ireland)

KYORIN Pharmaceutical Co., Ltd.

+ [1]

Drug Highest PhaseApproved

First Approval Date

US (17 Dec 1999),

Acute bacterial bronchitisAcute sinusitisBronchitis, Chronic+ [4]

Regulation-

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Structure

Molecular FormulaC19H22FN3O4

InChIKeyXUBOMFCQGDBHNK-UHFFFAOYSA-N

CAS Registry112811-59-3

View All Structures (2)

Sensitive and selective detection of fluoroquinolones, especially from different sources, is challenging. This study reported an uncommon three-cage lanthanide metal-organic framework (1-Eu) with a Eu³⁺ cluster as its structural primitive using a C₂-symmetric 5,5-(Pyrazine-2,6-diyl) diisophthalic acid ligand. The 1-Eu probe effectively detected four fluoroquinolones through distinct color changes and spectral emission bands, demonstrating excellent performance with low detection limits: moxifloxacin (LOD: 9.3 nM), danofloxacin (LOD: 33.7 nM), gatifloxacin (LOD: 67.9 nM), and ofloxacin (LOD: 238.6 nM). Mechanistic studies revealed that internal filtration and photoinduced electron transfer (a-PET) effects were key factors. Furthermore, 1-Eu was successfully used to detect fluoroquinolones in food samples. Additionally, portable paper-based sensors were developed to quickly semi-quantify analyte concentrations using a smartphone color recognition app, underscoring the practical potential of this probe. This study introduces a novel methodology for the identification and detection of fluoroquinolones to enhance food safety.

01 Dec 2024·Bioorganic Chemistry

Copper(II) aromatic heterocyclic complexes of Gatifloxacin with multi-targeting capabilities for antibacterial therapy and combating antibiotic resistance

Article

Author: Li, Jin-Hao ; He, Liang ; Chen, Bai-Hua ; Pan, Zheng-Yin ; Liu, Qi-Yan ; Liu, Ya-Shu ; Wu, Xiao-Yin ; Jiang, Shan ; Dong, Jia-Hao ; Liu, Yingju

In recent years, the pace of novel antibiotic development has been relatively slow, intensifying the urgency of the antibiotic resistance issue. Consequently, scientists have turned their attention to enhancing antibiotic activity by coordinating antibiotics with metal elements. This study designs and synthesizes three novel antibacterial copper complexes based on Gatifloxacin. These complexes exhibit potent antibacterial activity, notably Cu-1, with a minimum inhibitory concentration (MIC) of only 0.063 μg/mL against Staphylococcus aureus (S.aureus), demonstrating potent bacteriostatic capabilities. Further investigations unveil the antibacterial mechanisms of complex Cu-1, revealing its ability not only to suppress the activities of DNA gyrase and topoisomerases IV, but also to effectively inhibit biofilm formation and disrupt the integrity of cell membrane. This multi-targeting action contributes to mitigating the risk of bacterial resistance emergence. Additionally, synergy between Cu-1 and conventional antibiotics is confirmed through checkerboard assays, offering novel strategies for antibacterial therapy. In vivo experiments using a murine model of S.aureus infection demonstrate the significant antibacterial efficacy of Cu-1, providing robust support for its potential in treating S.aureus infections. This study demonstrates that the coordination complexes formed by copper, Gatifloxacin and suitable aromatic heterocyclic ligands exhibit multi-targeting characteristics against bacteria, offering a new direction for combating antibiotic resistance in antibacterial therapy.

01 Dec 2024·Current Drug Delivery

Targeted Bacterial Keratitis Treatment with Polyethylene Glycol-Dithiothreitol-Boric Acid Hydrogel and Gatifloxacin

Article

Author: Wen, Jing ; Bai, Jianhai ; Huang, Chunlian ; Shen, Xiao

Introduction/Objective:To prolong the ocular residence time of gatifloxacin and enhance its efficacy against bacterial keratitis, this study developed a velocity-controlled polyethylene glycol-dithiothreitol-boric acid (PDB) hydrogel loaded with gatifloxacin.Methods:First, the basic properties of the synthesized PDB hydrogel and the gatifloxacin-loaded PDB hydrogel were assessed. Secondly, the in vitro degradation rate of the drug-loaded PDB was measured in a simulated body fluid environment with pH 7.4/5.5. The release behavior of the drug-loaded PDB was studied using a dialysis method with PBS solution of pH 7.4/5.5 as the release medium. Finally, a mouse model of bacterial keratitis was established, and tissue morphology was observed using hematoxylin-eosin staining. Additionally, mouse tear fluid was extracted to observe the antibacterial effect of the gatifloxacin-loaded PDB hydrogel.Results:The results showed that the PDB hydrogel had a particle size of 124.9 nm and a zeta potential of -23.3 mV, with good porosity, thermosensitivity, viscosity distribution, rheological properties, and high cell compatibility. The encapsulation of gatifloxacin did not alter the physical properties of the PDB hydrogel and maintained appropriate swelling and stability, with a high drug release rate in acidic conditions. Furthermore, animal experiments demonstrated that the gatifloxacin- loaded PDB hydrogel exhibited superior therapeutic effects compared to gatifloxacin eye drops and displayed strong antibacterial capabilities against bacterial keratitis.Conclusion:This study successfully synthesized PDB hydrogel and developed a gatifloxacin drug release system. The hydrogel exhibited good thermosensitivity, pH responsiveness, stability, and excellent biocompatibility, which can enhance drug retention, utilization, and therapeutic effects on the ocular surface.

100 Deals associated with Gatifloxacin

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External Link

KEGG	Wiki	ATC	Drug Bank
D00589	Gatifloxacin	S01AE06 J01MA16	DB01044

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Conjunctivitis, Bacterial	US	AbbVie, Inc.	18 May 2010
Blepharitis	JP	Senju Pharmaceutical Co., Ltd.	07 Sep 2004
Corneal Ulcer	JP	Senju Pharmaceutical Co., Ltd.	07 Sep 2004
Dacryocystitis	JP	Senju Pharmaceutical Co., Ltd.	07 Sep 2004
Hordeolum	JP	Senju Pharmaceutical Co., Ltd.	07 Sep 2004
Conjunctivitis	BR	-	27 Mar 2004
Infectious Diseases	CN	Sino-American Shanghai Squibb Pharmaceuticals Ltd.	29 Oct 2002

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Conjunctivitis, Bacterial	Phase 3	US	Allergan, Inc.	28 Mar 2003
Conjunctivitis	Discovery	CN	Senju Pharmaceutical Co., Ltd.	17 Feb 2005

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03578276 (CTgov)	Phase 4	Cataract	35	prednisolone acetate+gatifloxacin+bromfenac (LessDrops)	hwjnmlpcbs(kqrxbwuizc) = jerbpweyuj bnjsqvdbfv (cwtuthcdof, nvuqkwpzpd - kuvcdfolov) View more	-	10 Jun 2022
				Prednisolone acetate 1% ophthalmic suspension+Gatifloxacin Ophthalmic+Bromfenac 0.075% Oph Solution (Standard of Care)	hwjnmlpcbs(kqrxbwuizc) = zuzndvwnrw bnjsqvdbfv (cwtuthcdof, uiaihjksux - rdngasnbmd) View more
Not available (ARVO2021)	Not Applicable	Keratitis	794	Netilmicin	xsbpekjner(lkvnmffjaa) = jswztatbuz mbckxhktav (oxewbzrkmp ) View more	Positive	01 Jun 2021
				Moxifloxacin	xsbpekjner(lkvnmffjaa) = pmiqiuzqqn mbckxhktav (oxewbzrkmp ) View more
ARVO2017	Phase 2	Conjunctivitis, Bacterial	300	Pazufloxacin 0.09% BID	(hkooxiptvk) = oqiehtgxxd qeidngqibg (spfgukojvg )	Positive	07 May 2017
				Pazufloxacin 0.09% TID	(hkooxiptvk) = zmmohsroxq qeidngqibg (spfgukojvg )
Pubmed \| Elife	Not Applicable	-	-	Gatifloxacin	qkldwmkdjz(jlxhotulgu) = qpnggmsnju kqszswfxcc (nzqveassbe )	-	11 Mar 2016
AAO2015	Not Applicable	Endophthalmitis	-	Gatifloxacin	(hpstodwfra) = lcwwrvshhm bqlistjkol (ljvwlqfsuk, 0.02)	-	15 Nov 2015
				Polymyxin-trimethoprim	(hpstodwfra) = ovyeiclcjt bqlistjkol (ljvwlqfsuk, 0.02)
NCT01928693 (Eye02, CTgov)	Phase 2	Corneal Ulcer	2	Besivance 0.6% Ophthalmic Suspension (Besivance 0.6% Ophthalmic Suspension)	qtomyvdkmo(eksqfvjejt) = wmsxaqaqgx xfmwfxxoht (fjuvlmycyv, eawfznrbih - mtcwqeajoa) View more	-	13 Aug 2015
				Zymaxid 0.5% Ophthalmic Solution (Zymaxid 0.5% Ophthalmic Solution)	vovlnoscdv(rmdtbtlekx) = palsbpzvpa fqwmyosolh (xvqmilautg, jpyhykijbw - srzyrllqvy) View more
ARVO2015	Not Applicable	-	-	0.3% gatifloxacin eye gel	(qixrgxsolp) = kmceoifnvm flalygjyte (eycckfvtgo )	-	01 Jun 2015
NCT00350363 (CTgov)	Phase 4	Ophthalmologic surgical procedures	60	Gatifloxacin	oumboagdcx(zgmwiqwujy) = rzxnhimxpt qqfmwppewz (uyniwakgsm, vezgbwtvfw - zfpjdvnsxt) View more	-	29 Jan 2015
NCT00509873 (Pubmed \| Am J Ophthalmol)	Phase 3	acute bacterial conjunctivitis	1,437	Gatifloxacin 0.5%	(mhbclfkwlj) = AEs were reported by 11.6% and 13.3% of patients in the gatifloxacin 0.5% and vehicle safety populations, respectively pdwpntcjug (fojlzxnjfu ) View more	-	01 Dec 2014
				Vehicle
NCT00216385 (Pubmed \| Br Dent J)	Phase 3	Tuberculosis	1,836	4-month gatifloxacin-containing regimen	bkqjezqitv(slrkvmzhal) = tvqyhckkyn dcwivoxkfp (mffamuhuad ) View more	Negative	23 Oct 2014
				standard regimen	bkqjezqitv(slrkvmzhal) = pavbzmnctz dcwivoxkfp (mffamuhuad ) View more