Drug intelligence / Profile preview

grepafloxacin

Development stage
Discontinued
Lead developer
Taiho Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Grepafloxacin is an oral broad-spectrum fluoroquinolone antibiotic that was used to treat various gram-positive and gram-negative bacterial infections. It acts by inhibiting bacterial type II DNA topoisomerases—specifically DNA gyrase and topoisomerase IV—which are essential for the replication, transcription, and repair of bacterial DNA. Grepafloxacin demonstrated improved activity against certain Gram-positive organisms such as *Streptococcus pneumoniae* compared to other fluoroquinolones. The drug was indicated for acute exacerbations of chronic bronchitis, community-acquired pneumonia (including those caused by *Mycoplasma pneumoniae*), uncomplicated gonorrhea (urethral in males; endocervical and rectal in females), non-gonococcal urethritis and cervicitis (such as those caused by *Chlamydia trachomatis* or *Ureaplasma urealyticum*). Due to its potential to cause QT interval prolongation leading to potentially fatal cardiac arrhythmias, grepafloxacin was withdrawn from the market worldwide in 1999[2][3][4][5][6].

Brand names
RaxarGrepaxVaxarVorzan
Other names
grepafloxacin hydrochloride
02

Targets

DNA gyraseTopo IV (Bacterial Topoisomerase IV)

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