Contezolid

Contezolid (trade name Youxitai) is an antibiotic of the oxazolidinone class.[1][2] It is effective against Staphylococcus aureus, methicillin-resistant Staphylococcus aureus (MRSA), Streptococcus pyogenes, Streptococcus agalactiae, and other bacteria.[3]

Contezolid
Clinical data
Trade namesYouxitai
Other namesMRX-I
Legal status
Legal status
  • Rx in China
Identifiers
  • (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
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC18H15F3N4O4
Molar mass408.337 g·mol−1
3D model (JSmol)
  • C1CN(C=CC1=O)C2=C(C=C(C(=C2F)F)N3C[C@@H](OC3=O)CNC4=NOC=C4)F
  • InChI=1S/C18H15F3N4O4/c19-12-7-13(15(20)16(21)17(12)24-4-1-10(26)2-5-24)25-9-11(29-18(25)27)8-22-14-3-6-28-23-14/h1,3-4,6-7,11H,2,5,8-9H2,(H,22,23)/t11-/m0/s1
  • Key:SULYVXZZUMRQAX-NSHDSACASA-N

In 2021, it was approved by the National Medical Products Administration of China for the treatment of complicated skin and soft tissue infections (cSSTI).[3][4]

A prodrug of contezolid, contezolid acefosamil, which is formulated for IV administration[5] is in Phase III clinical trials for diabetic foot infection.[6]

Chemical structure of contezolid acefosamil

References
  1. Gordeev MF, Yuan ZY (June 2014). "New Potent Antibacterial Oxazolidinone (MRX-I) with an Improved Class Safety Profile". Journal of Medicinal Chemistry. 57 (11): 4487–4497. doi:10.1021/jm401931e. PMID 24694071.
  2. Zhao X, Huang H, Yuan H, Yuan Z, Zhang Y (May 2022). "A Phase III multicentre, randomized, double-blind trial to evaluate the efficacy and safety of oral contezolid versus linezolid in adults with complicated skin and soft tissue infections". The Journal of Antimicrobial Chemotherapy. 77 (6): 1762–1769. doi:10.1093/jac/dkac073. PMID 35265985.
  3. Hoy SM (September 2021). "Contezolid: First Approval". Drugs. 81 (13): 1587–1591. doi:10.1007/s40265-021-01576-0. PMC 8536612. PMID 34365606.
  4. Mak E (3 June 2021). "Micurx wins China approval for antibacterial contezolid". BioWorld.
  5. Liu J, Wang W, Wang C, Zhang L, Zhang X, Liu S, et al. (July 2022). "Discovery of Antibacterial Contezolid Acefosamil: Innovative O-Acyl Phosphoramidate Prodrug for IV and Oral Therapies". ACS Medicinal Chemistry Letters. 13 (7): 1030–1035. doi:10.1021/acsmedchemlett.2c00191. PMC 9290071. PMID 35859881.
  6. "Contezolid acefosamil by MicuRx Pharmaceuticals for Diabetic Foot Infection (DFI): Likelihood of Approval". GlobalData. 31 May 2023 – via Pharmaceutical Technology.
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