Drug intelligence / Profile preview

fosfomycin

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intravenous, Inhalation
01

Overview

Fosfomycin is a broad-spectrum, bactericidal antibiotic discovered from *Streptomyces fradiae* and now also produced synthetically. It is structurally unique among antibiotics, containing a phosphonic acid group and an epoxide ring. Fosfomycin acts by irreversibly inhibiting the enzyme UDP-N-acetylglucosamine enolpyruvyl transferase (MurA), which catalyzes the first committed step in bacterial cell wall synthesis—specifically, the formation of UDP N-acetylmuramic acid. This disruption leads to inhibition of peptidoglycan biosynthesis and ultimately bacterial cell death[1][8]. It is primarily indicated for uncomplicated urinary tract infections (UTIs) caused by susceptible strains of *Escherichia coli* and *Enterococcus faecalis*, typically administered as a single oral dose[2][3][7][8]. Intravenous formulations are available outside the US for more severe or complicated infections, including those caused by multidrug-resistant organisms such as MRSA and VRE[2][5][10]. Fosfomycin has notable activity against both Gram-positive and Gram-negative bacteria, including some resistant strains (e.g., ESBL-producing *E. coli*, MRSA)[2][10]. It also demonstrates antibiofilm properties[2][8].

Brand names
MonurolFosfocina
Other names
磷霉素phosphomycinfosfonomycin
02

Targets

MurA (UDP-N-acetylglucosamine 1-carboxyvinyltransferase)

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