Drug intelligence / Profile preview

pefloxacin

Development stage
Unknown
Lead developer
Sanofi
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Pefloxacin is a synthetic broad-spectrum fluoroquinolone antibiotic structurally related to nalidixic acid. It is effective against a wide range of gram-negative and gram-positive bacteria, including Escherichia coli, Neisseria gonorrhoeae, Staphylococcus aureus, Shigella, Salmonella, Campylobacter species, and multidrug-resistant Pseudomonas and Enterobacter. The drug acts by inhibiting bacterial DNA gyrase (a type II topoisomerase) and topoisomerase IV—enzymes essential for DNA replication and transcription. In gram-negative bacteria, DNA gyrase is the primary target; in gram-positive organisms, topoisomerase IV is preferentially inhibited. This disruption leads to strand breakage of the bacterial chromosome and ultimately inhibits cell division[1][2][5][6]. Pefloxacin can be administered orally or intravenously[5], penetrates well into tissues (including intracellular compartments), and has been used primarily for infections of the genitourinary tract (such as uncomplicated gonococcal urethritis in males) as well as gastrointestinal infections caused by susceptible organisms[4][5][7].

Brand names
PefloxPeflacin
Other names
pefloxacin mesylatepefloxacinum
02

Targets

TOP2A (DNA topoisomerase II)Topo IV (Bacterial Topoisomerase IV)GyrA (DNA gyrase subunit A)

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