Contezolid Explained
| Tradename: | Youxitai |
| Legal Status: | Rx in China |
| Synonyms: | MRX-I |
| Cas Number: | 1112968-42-9 |
| Chembl: | 3287379 |
| Chemspiderid: | 34217570 |
| Drugbank: | DB12796 |
| Iuphar Ligand: | 10795 |
| Kegg: | D11297 |
| Pubchem: | 25184541 |
| Unii: | B669M62ELP |
| Iupac 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 |
| Smiles: | C1CN(C=CC1=O)C2=C(C=C(C(=C2F)F)N3C[C@@H](OC3=O)CNC4=NOC=C4)F |
| Stdinchi: | 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 |
| Stdinchikey: | SULYVXZZUMRQAX-NSHDSACASA-N |
| C: | 18 |
| H: | 15 |
| F: | 3 |
| N: | 4 |
| O: | 4 |
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]
Notes and References
- Gordeev MF, Yuan ZY . New Potent Antibacterial Oxazolidinone (MRX-I) with an Improved Class Safety Profile . Journal of Medicinal Chemistry . 57 . 11 . 4487–4497 . June 2014 . 24694071 . 10.1021/jm401931e .
- Zhao X, Huang H, Yuan H, Yuan Z, Zhang Y . 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 . May 2022 . 35265985 . 10.1093/jac/dkac073 .
- Hoy SM . Contezolid: First Approval . Drugs . 81 . 13 . 1587–1591 . September 2021 . 34365606 . 8536612 . 10.1007/s40265-021-01576-0 .
- News: Mak E . Micurx wins China approval for antibacterial contezolid . 3 June 2021 . BioWorld .
- Liu J, Wang W, Wang C, Zhang L, Zhang X, Liu S, Xu Y, Wang H, Dai Q, Liu C, Wang X, Yuan Z, Gordeev MF . 6 . Discovery of Antibacterial Contezolid Acefosamil: Innovative O-Acyl Phosphoramidate Prodrug for IV and Oral Therapies . ACS Medicinal Chemistry Letters . 13 . 7 . 1030–1035 . July 2022 . 35859881 . 9290071 . 10.1021/acsmedchemlett.2c00191 .
- News: Contezolid acefosamil by MicuRx Pharmaceuticals for Diabetic Foot Infection (DFI): Likelihood of Approval . 31 May 2023 . GlobalData . Pharmaceutical Technology .
