Drug intelligence / Profile preview

linezolid + rifampicin

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Linezolid + rifampicin is a combination of two antibiotics used primarily for the treatment of infections caused by multidrug-resistant Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). Linezolid is an oxazolidinone antibiotic that inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit, preventing formation of the 70S initiation complex. Rifampicin (also known as rifampin) is a broad-spectrum antibiotic that inhibits bacterial DNA-dependent RNA polymerase, thereby blocking RNA synthesis. The combination has shown synergistic activity against certain resistant strains and is considered particularly for implant-associated infections and bacteremia where monotherapy may be insufficient or resistance risk is high[1][2]. However, co-administration leads to significantly reduced plasma concentrations of linezolid due to increased metabolism induced by rifampicin, which may impact efficacy and increase risk for resistance development[3][5]. This interaction requires careful monitoring if both drugs are used together.

Other names
linezolid + rifampin
02

Targets

23S rRNA (23S ribosomal RNA)rpoB (DNA-directed RNA polymerase subunit beta)

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