Eperezolid
Eperezolid is a synthetic antibiotic that belongs to the oxazolidinone class of drugs. It was developed by Pharmacia and is a second-generation oxazolidinone, following the first-generation drug, linezolid.
Chemistry
Eperezolid is a synthetic compound that is structurally related to linezolid. Both drugs are part of the oxazolidinone class, which is characterized by a 1,3-oxazolidin-2-one core structure. The chemical formula of eperezolid is C16H20FN3O4.
Mechanism of Action
The mechanism of action of eperezolid is similar to that of other oxazolidinones. It inhibits protein synthesis in bacteria by binding to the 50S subunit of the bacterial ribosome. This prevents the formation of a functional 70S initiation complex, which is essential for the translational process in bacteria.
Clinical Use
Eperezolid was developed for the treatment of infections caused by Gram-positive bacteria, including those resistant to other antibiotics. However, it has not been as widely used as linezolid, primarily due to concerns about its potential for toxicity.
Safety and Efficacy
In clinical trials, eperezolid has been shown to be effective against a variety of Gram-positive bacteria. However, its use has been limited by concerns about potential side effects, including thrombocytopenia, anemia, and neuropathy. These side effects are believed to be related to the drug's mechanism of action and its effect on mitochondrial protein synthesis.
Development and Approval
Eperezolid was developed by Pharmacia, which later became part of Pfizer. It was one of the first oxazolidinones to be developed and was initially seen as a promising new class of antibiotics. However, its development was overshadowed by the success of linezolid, which was approved by the Food and Drug Administration (FDA) in 2000.
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Contributors: Prab R. Tumpati, MD