FLEROXACIN

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H18F3N3O3
Molecular Weight	369.3383
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CN1CCN(CC1)C2=C(F)C=C3C(=O)C(=CN(CCF)C3=C2F)C(O)=O

InChI

InChIKey=XBJBPGROQZJDOJ-UHFFFAOYSA-N

InChI=1S/C17H18F3N3O3/c1-21-4-6-22(7-5-21)15-12(19)8-10-14(13(15)20)23(3-2-18)9-11(16(10)24)17(25)26/h8-9H,2-7H2,1H3,(H,25,26)

HIDE SMILES / InChI

Molecular Formula	C17H18F3N3O3
Molecular Weight	369.3383
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

Fleroxacin is an anti-bacterial agent developed for the treatment of uncomplicated cystitis in women, uncomplicated gonococcal infections, bacterial enteritis, and traveler's diarrea, urinary tract infection, pyelonephritis, skin, soft tissue, bone and joint infections, and lower respiratory tract infections. Fleroxacin acts on bacterials by inhibiting DNA gyrase and topoisomerase IV. Although the current status of the drug in Europe and in the USA is unknown, there is information about its approval and usage in China.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bacterial DNA gyrase 66	Inhibitor 8,297
Topoisomerase IV 62	Inhibitor 8,297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Bacterial infections 234	Curative		Approved 8,429	QUINODIS

PubMed

Show entries

Title	Date	PubMed
Activity of ciprofloxacin and other fluorinated quinolones against mycobacteria.	1987 Apr 27	3107379
Comparative in-vitro activity of fleroxacin and other 6-fluoroquinolones against mycobacteria.	1988 Oct	3144550
Adverse reactions in a dose-ranging study with a new long-acting fluoroquinolone, fleroxacin.	1989 Oct	2511802
The antimicrobial activity of Fleroxacin RO 23-6240, a third generation fluoroquinolone derivative, tested in vitro.	1990	2112571
Central nervous system toxicity of quinolones: human and animal findings.	1990 Oct	2124211

Showing 1 to 5 of 50 entries

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Patents

Sample Use Guides

In Vivo Use Guide

400mg once daily (uncomplicated cystitis in women, uncomplicated gonococcal infections, bacterial enteritis, and traveler's diarrhea), 200 mg administered for 3 days (uncomplicated urinary tract infection).

Route of Administration: Oral

In Vitro Use Guide

In vitro activity of fleroxacin was tested against different bacteria isolates. The drug inhibited E.Coli (MIC 0.06-0.12 ug/ml), Klebsiella pneumoniae and K. oxytoca (MIC 0.12-1 ug/ml), Enterobacter cloacae and E. aerogenes (MIC <= 0.06-0.5 ug/ml), Citrobacterfreundii and C. diversus (MIC 0.06-1), Streptococcus faecalis (MIC 4-16 ug/ml), Pseudomonas aeruginosa (MIC 0.5-32 ug/ml), Salmonella spp. (MIC 0.06-0.12 ug/ml), etc.