Tedizolid phosphate (also known as TR-701 FA) is the prodrug form of the microbiologically active molecule Tedizolid(TR-700), a novel orally and intravenously administered oxazolidinone antibacterial agent. Tedizolid phosphate is rapidly converted by non-specific phosphatases to tedizolid, which inhibits the growth of S. aureus, S. epidermidis, E. faecalis, E. faecium, S. pneumoniae, and S. pyogenes (MICs = 0.25-1 μg/ml). In vivo, tedizolid phosphate (15 mg/kg) reduces vegetation titer in a rabbit model of aortic valve endocarditis caused by methicillin-resistant S. aureus (MRSA). It also reduces densities of methicillin-susceptible S. aureus and MRSA infection in a mouse model of catheter-related biofilm infection and increases survival in a rabbit model of MRSA necrotizing pneumonia.
In Vitro Activity of TR-700, the Active Ingredient of the Antibacterial Prodrug TR-701, a Novel Oxazolidinone Antibacterial Agent.
Cellular pharmacokinetics and intracellular activity of torezolid (TR-700): studies with human macrophage (THP-1) and endothelial (HUVEC) cell lines.
Absorption, distribution, metabolism, and excretion of the novel antibacterial prodrug tedizolid phosphate.
Comparative Efficacies of Tedizolid Phosphate, Vancomycin, and Daptomycin in a Rabbit Model of Methicillin-Resistant Staphylococcus aureus Endocarditis.
Comparative Efficacies of Tedizolid Phosphate, Linezolid, and Vancomycin in a Murine Model of Subcutaneous Catheter-Related Biofilm Infection Due to Methicillin-Susceptible and -Resistant Staphylococcus aureus.
Effects of Tedizolid Phosphate on Survival Outcomes and Suppression of Production of Staphylococcal Toxins in a Rabbit Model of Methicillin-Resistant Staphylococcus aureus Necrotizing Pneumonia.