Tedizolid Phosphate is a second-generation oxazolidone antibiotic. It is a phosphate ester precursor to Tedizolid, the active compound. It is bacteriostatic against Gram-positive organisms.
Tedizolid Phosphate was developed by Cubist Pharmaceuticals, following acquistion of Trius Pherapeutics. It 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 addiitonal binding site interactions. The compound was formerly known as Torezolid. Tedizolid is bacteriostatic against Gram-positive organisms. As with linezolid, Tedizolid is a weak, reversible MAO inhibitor.
Tedizolid Phosphate is slighty soluble in DMSO, but insoluble in water and ethanol.
We also offer:
- Tedizolid (T117)
| 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 is effective against Gram-positive bacteria including MRSA and VRE, and linezolid-resistant strains. |
| Microbiology Applications |
Tedizolid inhibited all 28 isolates of penicillin-resistant Streptococcus pneumoniae (PRSP) using an in vitro mouse model with 0.25 µg/mL, which was 4-fold more potent than Linezolid (Choi et al, 2012). In a murine model of hematogenous pulmonary ijfection, Tedizolid showed antimicrobial and immunomodulatory results superior to vancomycin (ref) Oxazolidinone antibacterials as a class are generally capable of overcoming resistance to other bacterial protein synthesis inhibitors. |
| Molecular Formula | C17H16FN6O6P |
| Solubility | Soluble in DMSO (36 mg/mL), sparingly soluble in water (0.1 mg/mL) |
| 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. 56(9):4713-4717 PMID 22713339 Kaku N, Morinaga Y, and Takeda K et al (2016) Antimicrobial and immunomodulatory effects of Tedizolid against methicillin-resistant Staphylococcus aureus in a murine model of hematogenous pulmonary infection. Int. J. Med. Microbiol. 306(6):421-428 PMID 27259840 Kisgen JJ, Mansour H, Unger NR, Childs LM (2014) Tedizolid:A new oxazolidinone antimicrobial. Am. J. Health Syst. Pharm. 71(8):621-633 PMID 24688035 Prokocimer P, Bien P, Deanda C, Pillar CM, Bartizal K (2012) In vitro activity and microbiological efficacy of tedizolid (TR-700) against Gram-positive clinical isolates from a phase 2 study of oral tedizolid phosphate (TR-701) in patients with complicated skin and skin structure infections. Antimicrob. Agents Chemother. 56(9):4608-4613 PMID 22687509 Rybak JM, Marx K, Martin CA (2014) Early experience with Tedizolid: Clinical efficacy, pharmacodynamics, and resistance. Pharmacother. 34(11):1198-1208 PMID 25266820 |
