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. 2021 Aug 7;81(13):1587–1591. doi: 10.1007/s40265-021-01576-0

Features and properties of contezolid

Alternative names MRX-I; Youxitai
Class Amines; anti-infectives; antibacterials; antituberculars; dihydropyridines; fluorinated hydrocarbons; oxazoles; oxazolidinones; skin disorder therapies
Mechanism of action Protein synthesis inhibitors
Route of administration Oral
Pharmacodynamics Prevents the formation of a functional bacterial 70S initiation complex, disrupting reproduction
Minimum inhibitory concentration required to inhibit the growth of 90% of isolates of ≤ 2 mg/L against methicillin-susceptible Staphylococcus aureus (398 isolates), methicillin-resistant S. aureus (208 isolates), Streptococcus pneumoniae (201 isolates), Streptococcus pyogenes (12 isolates), Enterococcus species (103 isolates) and vancomycin-resistant Enterococcus faecium (26 isolates)
Pharmacokinetics Non-linear pharmacokinetics at doses > 600 mg; contezolid should be taken with meals or within 30 min after a meal (as food promotes its absorption)
Adverse events Appears to be associated with less bone marrow suppression-associated toxicity than other oxazolidinone antibacterial agents; most treatment-emergent adverse events mild or moderate in severity
ATC codes
 WHO ATC code J01 (antibacterials for systemic use)
 EphMRA ATC code J1 (systemic antibacterials)
Chemical name (5S)-5-[(1,2-oxazol-3-ylamino)methyl]-3-[2,3,5-trifluoro-4-(4-oxo-2,3-dihydropyridin-1-yl)phenyl]-1,3-oxazolidin-2-one