Drug intelligence / Profile preview

tedizolid phosphate disodium

Development stage
Approved
Lead developer
Dong-A Pharmaceutical
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

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.

Brand names
Sivextro
Other names
tedizolid phosphate disodium salttorezolid phosphate disodiumtorezolid phosphate disodium saltTR-701 di-sodium phosphate saltTR701 di-sodium phosphate saltTR 701 di-sodium phosphate saltTR-701 disodiumTR701 disodiumTR 701 disodiumTR-701 disodium phosphateTR701 disodium phosphateTR 701 disodium phosphate
02

Targets

70S ribosome (Bacterial protein synthesis ribosome complex)Mitoribosome (Mitochondrial ribosome)23S rRNA (23S ribosomal RNA)

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