Drug Information

Drug (ID: DG01206) and It's Reported Resistant Information

• Name: Tedizolid
• Synonyms: Tedizolid; Torezolid; 856866-72-3; TR-700; Sivextro; DA-7157; Da 7157; UNII-97HLQ82NGL; TR 700; CHEBI:82717; 97HLQ82NGL; (5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one; (5R)-3-{3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)-1,3-oxazolidin-2-one; (R)-3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one; Tedizolid [USAN:INN]; previously torezolid; torezolid; Sivextro; Tedizolid (USAN/INN); SCHEMBL440398; CHEMBL1257051; GTPL10865; DTXSID10234975; TR700; 1431699-67-0; BCP02830; EX-A5826; BDBM50491954; MFCD19442562; s5278; ZINC43100956; AKOS025401974; CCG-268294; CS-0687; DB14569; NCGC00379072-02; (5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)-3-pyridyl]phenyl]-5-(hydroxymethyl)oxazolidin-2-one; AC-27738; AS-56108; HY-14855; A14965; D09685; Q7825683; (5R)-3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one; (5R)-3-{3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)-2-oxazolidinone; (R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-on; (R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one; 2-Oxazolidinone, 3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl)phenyl)-5-(hydroxymethyl)-, (5R)-; 3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one; 3-(3-fluoro-4-(6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-hydroxymethyloxazolidin-2-one; U7V
• Indication:
  In total 1 Indication(s)
  Skin infection [ICD-11: 1F28-1G0Z]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Gram-negative bacterial infection [ICD-11: 1B74-1G40]; [1]
• Target: Bacterial 50S ribosomal RNA (Bact 50S rRNA); NOUNIPROTAC; [1]
• Formula: C17H15FN6O3
• IsoSMILES: CN1N=C(N=N1)C2=NC=C(C=C2)C3=C(C=C(C=C3)N4C[C@@H](OC4=O)CO)F
• InChI: 1S/C17H15FN6O3/c1-23-21-16(20-22-23)15-5-2-10(7-19-15)13-4-3-11(6-14(13)18)24-8-12(9-25)27-17(24)26/h2-7,12,25H,8-9H2,1H3/t12-/m1/s1
• InChIKey: XFALPSLJIHVRKE-GFCCVEGCSA-N
• PubChem CID: 11234049
• ChEBI ID: CHEBI:82717
• TTD Drug ID: D08KBK

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-01: Infectious/parasitic diseases

Gram-negative bacterial infection [ICD-11: 1B74-1G40]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: DNA-directed RNA polymerase subunit beta (RPOB) [1]

• Molecule Alteration: Missense mutation; p.A1345G
• Resistant Disease: Gram-negative bacterial infection [ICD-11: 1B74-1G40]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: Gram-positive bacteria MRSA strain N315; N.A.
• Experiment for Molecule Alteration: Whole-genome sequencing assay
• Mechanism Description: Tedizolid resistance is uncommon and tedizolid's capacity to select for cross-resistance to other antimicrobials is incompletely understood. To the best of our knowledge, this is the first time that an rpoB mutation has been implicated in resistance to PhLOPSa antimicrobials.

References

• Ref 1: Identification of a novel tedizolid resistance mutation in rpoB of MRSA after in vitro serial passage .J Antimicrob Chemother. 2021 Jan 19;76(2):292-296. doi: 10.1093/jac/dkaa422. 10.1093/jac/dkaa422