Linezolid (DB00601): A Comprehensive Pharmacological and Clinical Monograph

Executive Summary

Linezolid is a seminal synthetic antibiotic, representing the first member of the oxazolidinone class to be approved for clinical use in 2000.[1] Its introduction marked a significant therapeutic advance in the global effort to combat infections caused by multidrug-resistant (MDR) Gram-positive pathogens. In recognition of its critical role, the World Health Organization (WHO) has classified Linezolid as "critically important" for human medicine, reserving its use primarily for severe infections that are resistant to other antibiotics, most notably those caused by methicillin-resistant

Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE).[1]

The pharmacological distinction of Linezolid lies in its unique mechanism of action. Unlike many other ribosome-targeting antibiotics that interfere with later stages of protein production, Linezolid inhibits the very first step—the formation of the 70S initiation complex—thereby preventing bacterial protein synthesis at its origin.[1] This novel target site accounts for its activity against bacteria that have developed resistance to other protein synthesis inhibitors. A cornerstone of its clinical utility is its exceptional pharmacokinetic profile, characterized by approximately 100% oral bioavailability. This property allows for equivalent dosing between intravenous and oral formulations, facilitating a seamless transition of therapy that can shorten hospital stays and reduce overall healthcare costs.[1]