Chemical compound
Pharmaceutical compound
Contezolid Trade names Youxitai Other names MRX-I Legal status
(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 CompTox Dashboard (EPA ) Formula C 18 H 15 F 3 N 4 O 4 Molar mass 408.337 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
^ 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 .
^ 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 .
^ a b Hoy SM (September 2021). "Contezolid: First Approval" . Drugs . 81 (13): 1587–1591. doi :10.1007/s40265-021-01576-0 . PMC 8536612 . PMID 34365606 .
^ Mak E (3 June 2021). "Micurx wins China approval for antibacterial contezolid" . BioWorld .
^ 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 .
^ "Contezolid acefosamil by MicuRx Pharmaceuticals for Diabetic Foot Infection (DFI): Likelihood of Approval" . GlobalData . 31 May 2023 – via Pharmaceutical Technology.