Drug intelligence / Profile preview

ciprofloxacin + linezolid

Development stage
Preclinical
Lead developer
Bayer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, RNA-Targeting Small Molecules → Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Ciprofloxacin + linezolid is a combination of two antibiotics used for the treatment of infections caused by susceptible bacteria, particularly in cases where multidrug-resistant organisms are suspected or confirmed. Ciprofloxacin is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase and topoisomerase IV, enzymes essential for DNA replication and transcription. Linezolid is an oxazolidinone antibiotic that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, preventing the formation of the initiation complex. This combination may be considered in severe or complicated infections such as those involving biofilms (e.g., prosthetic joint infections) or resistant Gram-positive pathogens like methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). The combination has been studied primarily in vitro; it can reduce bacterial load effectively but does not show strong synergy, and may even exhibit slight antagonism when used together against some strains[1][3][9]. Both drugs have distinct side effect profiles—ciprofloxacin can cause gastrointestinal upset, tendonitis/tendon rupture, CNS effects, QT prolongation[8], while linezolid carries risks of myelosuppression, serotonin syndrome (especially with serotonergic agents), neuropathy, lactic acidosis[6][10].

02

Targets

DNA gyraseTopo IV (Bacterial Topoisomerase IV)Bacterial 50S ribosomal subunit

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