Solithromycin

A novel fluoroketolide with lower MICs than those of telithromycin and macrolides; binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis; exhibits MICs of 7.5, 40, and 125 ng/ml for Streptococcus pneumoniae, Staphylococcus aureus, and Haemophilus influenzae, respectively. Bacterial Infection Approved (In Vitro) :The IC50s values for Solithromycin on TNFα and CXCL8 release are 41.6 μM and 78.2 μM, respectively. Solithromycin markedly reduces MMP9 activity, with an IC50 of 14.9 μM.Solithromycin (0-333 μM; 72 hours; U937 and PBMC cells) suppresses lipopolysaccharide-induced TNFα release and phorbol 12-myristate 13-acetate (PMA) -induced matrix metalloproteinase 9 (MMP9) activity, and does not affect cell viability in monocytic U937 and PBMC cells. (In Vivo) :Solithromycin (100 mg/kg; oral administration; every day; for 8 days; C57BL/6J mice) treatment inhibits inflammatory cells accumulation and pro-MMP9 production in cigarette smoke-exposed mice.