SKU: T118  / 
    CAS Number: 856867-55-5

    Tedizolid Phosphate

    ฿7,334.40 - ฿11,345.40

    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.

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    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