Contezolid: First Approval

• Published in: Drugs (New York, N.Y.) N.Y.), 2021-09, Vol.81 (13), p.1587-1591
• Main Author: Hoy, Sheridan M.
• Format: Article
• Language: English
• Subjects: AdisInsight Report; Anti-Bacterial Agents - pharmacokinetics; Anti-Bacterial Agents - pharmacology; Anti-Bacterial Agents - therapeutic use; Antibacterial agents; Antibiotic resistance; Antiinfectives and antibacterials; Bacterial diseases; Bacterial infections; China; Diabetes; Diabetes mellitus; Drug Approval; Drug dosages; Drug Resistance, Multiple, Bacterial; Foot diseases; Gram-positive bacteria; Gram-Positive Bacterial Infections - drug therapy; Health services; Humans; Infections; Internal Medicine; Medical equipment; Medicine; Medicine & Public Health; Metabolites; Methicillin; Methicillin-Resistant Staphylococcus aureus; Multidrug resistance; Multidrug resistant organisms; Oral administration; Oxazolidinones - pharmacokinetics; Oxazolidinones - pharmacology; Oxazolidinones - therapeutic use; Pharmacokinetics; Pharmacology/Toxicology; Pharmacotherapy; Population; Pyridones - pharmacokinetics; Pyridones - pharmacology; Pyridones - therapeutic use; Skin; Soft tissues; Staphylococcus aureus; Staphylococcus infections; Streptococcus infections; Tuberculosis; Vancomycin; Vancomycin Resistance
• ISSN: 0012-6667; 1179-1950
• DOI: 10.1007/s40265-021-01576-0

Contezolid 康替唑胺 (Youxitai 优喜泰 ® ), an orally administered oxazolidinone antibacterial agent, is being developed by Shanghai MicuRx Pharmaceutical Co., Ltd. for the treatment of multidrug-resistant (MDR) Gram-positive bacterial infections, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci. In June 2021, it was approved by the National Medical Products Administration of China for the treatment of complicated skin and soft tissue infections (cSSTI), including, but not limited to, methicillin-susceptible S. aureus , MRSA, Streptococcus pyogenes and Streptococcus agalactiae . The recommended dosage of contezolid is 800 mg (i.e. two 400 mg tablets) every 12 h for 7–14 days. Contezolid is also undergoing clinical development for acute bacterial skin and skin structure infections (ABSSSI) in the USA, and for diabetic foot infections. This article summarizes the milestones in the development of contezolid leading to this first approval for the treatment of cSSTI.