Ranbezolid

Ranbezolid (RBx7644 free base) is an orally active, oxazolidinone antibiotic against Gram-positive and Gram-negative anaerobes including Staphylococcus aureus, Staphylococcus epidermidis and Bacteroides fragilis. Ranbezolid can inhibit the 50s ribosomal subunit with an IC₅₀ of 17 μM for bacterial ribosomes. Ranbezolid interferes cell wall and lipid synthesis. Ranbezolid can rapidly kill bacteria, significantly reduce bacterial load, and has better cardiovascular safety. Ranbezolid can be used for the study of antibiotics for anaerobic bacteria^[1][2][3]. In Vitro:Ranbezolid (1 μg/mL) can effectively inhibit protein synthesis in S.aureus as well as in S. epidermidis, and additionally suppress the cell wall and lipid synthesis of Staphylococcus epidermidis^[1].
Ranbezoild (1-8 μg/mL) can cause concentration-dependent damage to the cell membrane of S. epidermidis^[1].
Ranbezoild exhibits a IC₅₀ value of 17 μM for bacterial ribosomes and safety index of 865^[1].
Ranbezolid exhibits the MICs against the anaerobic strains of B. fragilis, B. vulgatus, B. thetaiotaomicron, C. perfringens, C. difficile and P. magnus were 0.06, 0.015, 0.06, 0.06, 0.03 and 0.015 μg/mL, respectively^[2].
In Vivo:Ranbezoild (100 mg/kg, p.o., twice daily for 5 days) shows excellent antibacterial activity against B. fragilis in murine foreign-body infection model^[2].
Ranbezoild (≤ 50 mg/kg, p.o., single dose) does not significantly enhance the blood pressure-raising effect of Tyramine (HY-W007606) within the therapeutic dose range in the spontaneous hypertension model of rats^[3].