Oxazolidinone antibacterial agents: development of the clinical candidates eperezolid and linezolid

Abstract

Antimicrobial resistance is a significant nosocomial problem and is of increasing importance in community-acquired infections. One approach for overcoming resistance is the discovery and development of agents with new mechanisms of action. The oxazolidinones make up a relatively new class of antimicrobial agents which possess a unique mechanism of bacterial protein synthesis inhibition. Eperezolid and linezolid are two novel analogues that have demonstrated a variety of positive attributes. These agents inhibit many clinically-significant bacterial species both in vitro and in animal models of human infection. Furthermore they have oral bioavailability, and are well tolerated in humans at doses which produce plasma concentrations in excess of the levels predicted to be necessary for efficacy. In this review, we discuss the key information from the literature that supports the Phase II development of linezolid.

• antibacterial
• DuP 105
• DuP 721
• eperezolid
• linezolid
• oxazolidinone
• S-6123
• U-100592
• U-100766