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TR-701 di-sodium phosphate salt (tedizolid phosphate disodium) is a next-generation oxazolidinone prodrug developed by Dong-A Pharmaceutical, Trius Therapeutics, Bayer, Cubist, and Merck. It is rapidly converted in vivo by endogenous phosphatases to its active moiety, tedizolid (TR-700). Tedizolid acts as a bacterial protein synthesis inhibitor by binding to the 50S subunit of the bacterial ribosome, specifically interacting with the 23S ribosomal RNA. This mechanism prevents the formation of the translation initiation complex, exerting bacteriostatic activity against Gram-positive pathogens, including methicillin-resistant *Staphylococcus aureus* (MRSA), vancomycin-resistant enterococci (VRE), and various streptococci. The disodium phosphate salt formulation provides high aqueous solubility, making it suitable for both oral and intravenous administration. It is approved under the brand name Sivextro for the treatment of acute bacterial skin and skin structure infections (ABSSSI) and has been evaluated in Phase 3 trials for hospital-acquired and ventilator-associated bacterial pneumonia.
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