Drug intelligence / Profile preview

colistimethate sodium

Development stage
Approved
Lead developer
Avet Lifesciences
Modality
Small Molecules
Administration
Intravenous, Inhalation, Intrathecal, Intraventricular
01

Overview

Colistimethate sodium is a polymyxin antibiotic used to treat serious infections caused by susceptible Gram-negative bacteria, particularly *Pseudomonas aeruginosa* and carbapenemase-producing Enterobacteriaceae[2][5]. It is an inactive prodrug that is converted in the body to colistin (polymyxin E), the active form. The drug acts by binding to lipid A of lipopolysaccharide in the bacterial outer membrane, displacing divalent cations and disrupting membrane integrity. This leads to increased permeability of the bacterial cell membrane and ultimately cell lysis[6]. Colistimethate also exhibits anti-endotoxin activity by binding endotoxins released from Gram-negative bacteria[6]. It is typically reserved for multidrug-resistant infections due to its nephrotoxicity risk[5].

Brand names
Coly Mycin MColobreatheXylistin
Other names
colistimethatecolistin methanesulfonate
02

Targets

Lipid A phosphate (Lipid A phosphate groups)

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