Tedizolid is an oxazolidone-class antibiotic. It is an oxazolidinone, but differs from other oxazolidinones by having a modified side chain at the C-5 position of the oxazolidinone nucleus which confers activity against certain linezolid-resistant pathogens. It also has an optimized C- and D-ring system that improves its potency via additional binding site interactions. The compound was formerly known as Torezolid. Tedizolid was developed by Cubist Pharmaceuticals following acquisition of Trius Therapeutics. Tedizolid is bacteriostatic against Gram-positive organisms. As with linezolid, Tedizolid is a weak, reversible MAO inhibitor.
Tedizolid is slightly soluble in ethanol, DMSO, and DMF.
We also offer:
- Tedizolid Phosphate (T118)
| Mechanism of Action | Tedizolid binds to the 23S rRNA of the 50S ribosomal subunit, preventing the formation of the 70S initiation complex and inhibiting protein synthesis. |
| Spectrum | Tedizolid has activity against Gram-positive bacteria including MRSA and VRE, and linezolid-resistant strains with the cfr gene, in the absence of certain ribosomal mutations conferring reduced oxazolidinone susceptiibility. It has enhanced in vitro activity against Gram-positive aerobic bacteria. It also has activity against several Mycobacterium spp, including Mycobacterium tuberculosis and nontuberculous mycobacterium. |
| Microbiology Applications | Tedizolid is four- to eightfold more potent in vivo compared to linezolid against staphylocci, enterococci, and streptococci, including MRSA and vancomycin-resistant enterococci (VRE) and linezolid-resistant phenotypes. Tedizolid resistance is most commonly caused by mutations of the peptidyl transferase center (PTC) binding site on the 50S subunit of the bacterial ribosome. |
| Molecular Formula | C17H15FN6O3 |
| References |
Choi S, Im W, and Bartizal K (2012) Activity of Tedizolid phosphate (TR-701) in murine models of infection with penicillin-resistant and penicillin-sensitive Streptococcus pneumoniae. Antimicrob Agents Chemother. 2012 Sep;56(9):4713-4717 PMID 22713339 Kisgen JJ, Mansour H, Unger NR, Childs LM (2014) Tedizolid: A new oxazolidinone antimicrobial. Am. J. Health Syst. Pharm. 71(8):621-33 PMID 24688035 Rybak JM, Marx K, Martin CA (2014) Early experience with Tedizolid: Clinical efficacy, pharmacodynamics, and resistance. Pharmacother. 34(11):1198-1208 PMID 25266820 Zhanel GG et al (2015) Tedizolid: A novel oxazolidinone with potent activity against multidrug-resistant Gram-positive pathogens. Drugs. 75(3):253-270 PMID 25673021 |
