The oxazolidinones are a new synthetic class of antimicrobials structurally unrelated to any agent presently marketed. Data pertaining to these compounds, with respect to their pharmacology, pharmacokinetics, pharmacodynamics, mechanism of action, and bacteriologic activity, focusing on the analogs linezolid (PNU 100766) and eperezolid (PNU 100592), were retrieved by MEDLINE search and review of relevant abstracts presented at recent clinical conferences. Since the drugs are still investigational, we obtained in vitro and animal data as well as available human studies. The oxazolidinones have bacteriostatic activity against a number of important pathogens including methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, and vancomycin-resistant enterococci. They appear to be efficacious and well tolerated both orally and parenterally. Their role remains to be elucidated by clinical trials.