{{Short description|Chemical compound}} {{Infobox drug | drug_name = | INN = | type = <!-- empty --> | image = Contezolid.svg | image_class = skin-invert-image | alt = | caption = <!-- Clinical data --> | pronounce = | tradename = Youxitai | Drugs.com = | MedlinePlus = | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> | pregnancy_AU_comment = | pregnancy_category= | routes_of_administration = | ATCvet = | ATC_prefix = <!-- 'none' if uncategorised --> | ATC_suffix = <!-- Legal status --> | legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled --> | legal_AU_comment = | legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F --> | legal_BR_comment = | legal_CA = <!-- OTC, Rx-only, Schedule I, II, III, IV, V, VI, VII, VIII --> | legal_CA_comment = | legal_DE = <!-- Anlage I, II, III or Unscheduled --> | legal_DE_comment = | legal_NZ = <!-- Class A, B, C --> | legal_NZ_comment = | legal_UK = <!-- GSL, P, POM, CD, CD Lic, CD POM, CD No Reg POM, CD (Benz) POM, CD (Anab) POM or CD Inv POM / Class A, B, C --> | legal_UK_comment = | legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> | legal_US_comment = | legal_EU = | legal_EU_comment = | legal_UN = <!-- N I, II, III, IV / P I, II, III, IV --> | legal_UN_comment = | legal_status = Rx in China <!-- Pharmacokinetic data --> | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action= | excretion = <!-- Identifiers --> | synonyms = MRX-I | CAS_number = 1112968-42-9 | ChEMBL = 3287379 | ChemSpiderID = 34217570 | DrugBank = DB12796 | IUPHAR_ligand = 10795 | KEGG = D11297 | PubChem = 25184541 | UNII = B669M62ELP <!-- Chemical and physical data --> | IUPAC_name = (5''S'')-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.<ref>{{cite journal | vauthors = Gordeev MF, Yuan ZY | title = New Potent Antibacterial Oxazolidinone (MRX-I) with an Improved Class Safety Profile | journal = Journal of Medicinal Chemistry | volume = 57 | issue = 11 | pages = 4487–4497 | date = June 2014 | pmid = 24694071 | doi = 10.1021/jm401931e }}</ref><ref>{{cite journal | vauthors = Zhao X, Huang H, Yuan H, Yuan Z, Zhang Y | title = 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 | journal = The Journal of Antimicrobial Chemotherapy | volume = 77 | issue = 6 | pages = 1762–1769 | date = May 2022 | pmid = 35265985 | doi = 10.1093/jac/dkac073 }}</ref> It is effective against ''Staphylococcus aureus'', methicillin-resistant ''Staphylococcus aureus'' (MRSA), ''Streptococcus pyogenes'', ''Streptococcus agalactiae'', and other bacteria.<ref name=Hoy>{{cite journal | vauthors = Hoy SM | title = Contezolid: First Approval | journal = Drugs | volume = 81 | issue = 13 | pages = 1587–1591 | date = September 2021 | pmid = 34365606 | pmc = 8536612 | doi = 10.1007/s40265-021-01576-0 }}</ref>
In 2021, it was approved by the National Medical Products Administration of China for the treatment of complicated skin and soft tissue infections (cSSTI).<ref name=Hoy/><ref>{{cite news | vauthors = Mak E | url = https://www.bioworld.com/articles/507790-micurx-wins-china-approval-for-antibacterial-contezolid | title = Micurx wins China approval for antibacterial contezolid | date = 3 June 2021 | work = BioWorld }}</ref>
A prodrug of contezolid, contezolid acefosamil, which is formulated for IV administration<ref>{{cite journal | vauthors = 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 | display-authors = 6 | title = Discovery of Antibacterial Contezolid Acefosamil: Innovative ''O''-Acyl Phosphoramidate Prodrug for IV and Oral Therapies | journal = ACS Medicinal Chemistry Letters | volume = 13 | issue = 7 | pages = 1030–1035 | date = July 2022 | pmid = 35859881 | pmc = 9290071 | doi = 10.1021/acsmedchemlett.2c00191 }}</ref> is in Phase III clinical trials for diabetic foot infection.<ref>{{cite news | url = https://www.pharmaceutical-technology.com/data-insights/contezolid-acefosamil-micurx-pharmaceuticals-diabetic-foot-infection-dfi-likelihood-of-approval | title = Contezolid acefosamil by MicuRx Pharmaceuticals for Diabetic Foot Infection (DFI): Likelihood of Approval | date = 31 May 2023 | work = GlobalData | via = Pharmaceutical Technology }}</ref>
:thumb|left|Chemical structure of contezolid acefosamil{{clear left}}
== References == {{reflist}}
Category:Oxazolidinone antibiotics Category:Oxazoles Category:Fluoroarenes Category:Secondary amines Category:Tetrahydropyridines