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As an oxazolidinone, it has activity against several other gram-positive pathogens including methicillin-susceptible Staphylococcus aureus (MSSA), Streptococcus pyogenes, Streptococcus agalactiae, enterococci, coagulase-negative Staphylococci and Linezolid-resistant staphylococci. Tedizolid is marketed as a second-generation oxazolidinone that has potentially four-to-sixteen-fold potency against MRSA relative to Linezolid.

Tedizolid phosphate is a prodrug that is activated by plasma phosphatases to tedizolid. The prodrug tedizolid is called "TR-701", while the active moiety is called "TR-700".[3][4] As a member of the oxazolidinone class, Tedizolid exerts its microbial activity through inhibition of bacterial translation and protein synthesis.