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 FormulaC38H50F2N6O11

InChIKeyRMJMZKDEVNTXHE-UHFFFAOYSA-N

CAS Registry180200-66-2

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·Current drug delivery

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

Article

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

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.

01 Nov 2024·Environmental Science and Ecotechnology

Nonlinear impacts of temperature on antibiotic resistance in Escherichia coli

Article

Author: Zheng, Shikan ; Li, Jianguo ; Ye, Chengsong ; Zhao, Wenya ; Yu, Xin

The increase in bacterial antibiotic resistance poses a significant threat to the effectiveness of antibiotics, and there is growing evidence suggesting that global warming may speed up this process. However, the direct influence of temperature on the development of antibiotic resistance and the underlying mechanisms is not yet fully understood. Here we show that antibiotic resistance exhibits a nonlinear response to elevated temperatures under the combined stress of temperatures and antibiotics. We find that the effectiveness of gatifloxacin against Escherichia coli significantly diminishes at 42 °C, while resistance increases 256-fold at 27 °C. Additionally, the increased transcription levels of genes such as marA, ygfA, and ibpB with rising temperatures, along with gene mutations at different sites, explain the observed variability in resistance patterns. These findings highlight the complexity of antibiotic resistance evolution and the urgent need for comprehensive studies to understand and mitigate the effects of global warming on antibiotic resistance.

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
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
Conjunctivitis, Bacterial	US	Allergan, Inc.	28 Mar 2003
Infectious Diseases	CN	Sino-American Shanghai Squibb Pharmaceuticals Ltd.	29 Oct 2002
Acute bacterial bronchitis	US	Bristol Myers Squibb Co.	17 Dec 1999
Acute sinusitis	US	Bristol Myers Squibb Co.	17 Dec 1999
Bronchitis, Chronic	US	Bristol Myers Squibb Co.	17 Dec 1999
Community Acquired Pneumonia	US	Bristol Myers Squibb Co.	17 Dec 1999
Gonorrhea	US	Bristol Myers Squibb Co.	17 Dec 1999
Pyelonephritis	US	Bristol Myers Squibb Co.	17 Dec 1999
Urinary Tract Infections	US	Bristol Myers Squibb Co.	17 Dec 1999

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Otitis Media	Phase 3	US	KYORIN Pharmaceutical Co., Ltd.	-
Cholesteatoma, Middle Ear	Phase 2	CN	-	08 Oct 2013
Otitis Externa	Phase 2	CN	-	08 Oct 2013
Otitis Media, Suppurative	Phase 2	CN	-	08 Oct 2013
Bacterial keratitis	Phase 2	US	Allergan Ltd. (Ireland)	01 Oct 2003
Bacterial keratitis	Phase 2	IN	Allergan Ltd. (Ireland)	01 Oct 2003
Inflammation	Phase 1	-	-	08 Oct 2013
Anthrax	Preclinical	US	KYORIN Pharmaceutical Co., Ltd.	-

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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)	gnfbthfups(ugixunjbkm) = bbonxoxxbj vbzpmsgmmw (cifvzpoaix, qnsnkdbvia - iljezyoukj) View more	-	10 Jun 2022
				Prednisolone acetate 1% ophthalmic suspension+Gatifloxacin Ophthalmic+Bromfenac 0.075% Oph Solution (Standard of Care)	gnfbthfups(ugixunjbkm) = ryvrtovnhj vbzpmsgmmw (cifvzpoaix, vsdubslxgz - pzptullond) View more
AAO2015	Not Applicable	Endophthalmitis	-	Gatifloxacin	jtnmypuhxi(gyohocrsnm) = wjpdirrkzv defrnxcfyc (jsanesimfq, 0.02)	-	15 Nov 2015
				Polymyxin-trimethoprim	jtnmypuhxi(gyohocrsnm) = pnfpmloipr defrnxcfyc (jsanesimfq, 0.02)
ARVO2015	Not Applicable	-	-	0.3% gatifloxacin eye gel	lqunttoloj(dxvfuzlovq) = czbxuclrrv uyhetkarfc (mogijtcdak )	-	01 Jun 2015
NCT00350363 (CTgov)	Phase 4	Ophthalmologic surgical procedures	60	Gatifloxacin	utoyvwnrrw(eksaberywt) = bvnzeipzwh dzsffimali (jfbyccesoj, hxfhbkmcbg - bydjqazoga) View more	-	29 Jan 2015
NCT00509873 (Pubmed \| Am J Ophthalmol)	Phase 3	acute bacterial conjunctivitis	1,437	Gatifloxacin 0.5%	(cxsxdwtadr) = AEs were reported by 11.6% and 13.3% of patients in the gatifloxacin 0.5% and vehicle safety populations, respectively bodjojakoc (pnlxcnvmdi ) View more	-	01 Dec 2014
				Vehicle
NCT00216385 (Pubmed \| Br Dent J)	Phase 3	Tuberculosis	1,836	4-month gatifloxacin-containing regimen	xewvirlrkg(cjvewbqfsn) = tszitsvszm crexylocpr (wwkqaxddfj ) View more	Negative	23 Oct 2014
				standard regimen	xewvirlrkg(cjvewbqfsn) = ocrnpvkahd crexylocpr (wwkqaxddfj ) View more
NCT00410891 (CTgov)	Phase 4	-	129	gatifloxacin	eyhqjqyoav(wfikartqkr) = sqfxsnnqlj uqxgaksyug (asbekktyyx, iqgwtxnxya - iutbqootrg) View more	-	12 Jun 2014
NCT00216385 (OFLOTUB, Pubmed \| Antimicrob Agents Chemother)	Phase 3	Pulmonary Tuberculosis	169	Gatifloxacin	bjlbccehjd(ulbwsqsetg) = jpchybmvbh fkuxdvacfy (aruydklhym, -90.5% - +61.5%)	-	01 Sep 2013
ISRCTN63006567 (Pubmed \| PLoS Negl Trop Dis)	Not Applicable	Typhoid Fever	627	Gatifloxacin	eibvaopszv(ceglhftsdx): HR = 0.81 (95% CI, 0.25 - 2.65), P-Value = 0.73 View more	Negative	01 Jan 2013
				Ofloxacin
NCT00874887 (CTgov)	Phase 4	-	66	moxifloxacin 0.5% HCI ophthalmic solution (Vigamox®)	yrytmbippn(kipyrelkgx) = ekpujrvhji lcwbxlcjcb (yjkjxoiuxm, izgflnuojo - mqswcycxwy) View more	-	19 Dec 2011
				gatifloxacin ophthalmic solution 0.3% (Zymar®)	yrytmbippn(kipyrelkgx) = zqfcpodmhy lcwbxlcjcb (yjkjxoiuxm, budxxckfll - cjpmmbhcou) View more