Radezolid

Radezolid is an oxazolidinone antibiotic and a derivative of linezolid (Item No. 15012).¹ It is active against a variety of bacterial clinical isolates, including strains of methicillin-sensitive and -resistant S. aureus, vancomycin-sensitive and -resistant E. faecalis and E. faecium, and linezolid-resistant S. aureus, S. epidermidis, E. faecalis, E. faecium, and S. pneumoniae (MICs = ≤0.25-64 µg/ml). Radezolid is also active against L. monocytogenes, S. aureus, L. pneumophila, and S. epidermidis in THP-1 macrophages (EC₅₀s = 0.62, 0.63, 8.45, and 2.99 mg/L, respectively).² It inhibits protein translation in isolated wild-type and linezolid-resistant S. aureus 70S ribosomes but not rabbit reticulocyte lysates (IC₅₀s = 0.02, 0.03, and >2 µM, respectively).³ Radezolid is efficacious in a mouse model of S. pneumoniae-induced peritonitis with a 50% protective dose (PD₅₀) value of 1.3 mg/kg per day.⁴

WARNING This product is not for human or veterinary use.

1. Lawrence, L., Danese, P., DeVito, J., et al. In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens. Antimicrob. Agents Chemother. 52(5), 1653-1662 (2008).

2. LeMaire, S., Kosowska-Shick, K., Appelbaum, P.C., et al. Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: Studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila. Antimicrob. Agents Chemother. 54(6), 2549-2559 (2010).

3. Skripkin, E., McConnell, T.S., DeVito, J., et al. Rx-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance. Antimicrob. Agents Chemother. 52(10), 3550-3557 (2008).

4. Zhou, J., Bhattacharjee, A., Chen, S., et al. Design at the atomic level: Design of biaryloxazolidinones as potent orally active antibiotics. Bioorg. Med. Chem. Lett. 18(23), 6175-6178 (2008).