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

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]

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. 1 2 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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