Abstract: Linezolid is the first oxazolidinone antibacterial drug approved by the FDA, which can effectively treat various gram-positive bacterial infections, including blood infections, skin and soft tissue infections, community and hospital-acquired pneumonia. It has become one of the most commonly used antibiotics in clinical. In addition to the recently launched tedizolid phosphate (TR701) and contezolid (MRX-I), several oxazolidinone anti-infective candidates are currently under clinical research. This review briefly introduces the oxazolidinone antibiotics that have been marketed and are in clinical trials, and recent progress on the structure optimization of oxazolidinone drugs is also summarized.