Drug intelligence / Profile preview

contezolid

Development stage
Phase 4
Lead developer
MicuRx
Modality
Small Molecules
Administration
Oral
01

Overview

Contezolid is a novel, orally active oxazolidinone antibiotic developed for the treatment of complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), Streptococcus pyogenes, and Streptococcus agalactiae[1][2][5]. It was rationally designed to address the myelosuppression and monoamine oxidase inhibition limitations associated with linezolid[2]. Contezolid acts by inhibiting bacterial protein synthesis through binding to the V region of bacterial 23S rRNA in the 50S ribosomal subunit, thereby preventing formation of a functional 70S initiation complex essential for translation[2][5][8]. Compared to linezolid, contezolid demonstrates similar or improved antibacterial efficacy with reduced hematologic toxicity such as myelosuppression[3][6]. It was approved in China in June 2021 for cSSTI treatment[2][3].

Brand names
Youxitai
Other names
contezolid
02

Targets

23S rRNA (23S ribosomal RNA)

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