Lefamulin(BC-3781)

Lefamulin (BC-3781) is an orally active antibiotic. Lefamulin inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome. Lefamulin has anti-inflammatory activity. Lefamulin can be used in the research of bacterial infections, such as bacterial pneumonia[1].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

Lefamulin (0-1 mg/L) shows inhibitory activity against C. trachomatis, N. gonorrhoeae, and M. genitalium[2]. Lefamulin shows potent activity against all M. pneumoniae strains with MIC values of ≤0.008 μg/mL[3]. Cell Viability Assay[1] Cell Line: C. trachomatis, N. gonorrhoeae, and M. genitalium Concentration: 0-1 mg/L Incubation Time: Result: Inhibited bacterial activity with MIC50s of 0.02 mg/L, 0.063 mg/L and 0.12 mg/L respectively.

Lefamulin (10-140 mg/kg, s.c.) shows anti-inflammatory effect on LPS-induced lung neutrophilia mouse model[4]. Lefamulin (1.25-160 mg/kg, s.c.) shows antibacterial effect in S. pneumoniae or S. aureus challenged lung infection mice[5]. Animal Model: LPS-induced lung neutrophilia mouse model[4] Dosage: 10-140 mg/kg Administration: Subcutaneous injection (s.c.) Result: Reduced BALF neutrophil cell counts. Reduced pro-inflammatory cytokine (TNF-α, IL-6, IL-1β, and GM-CSF), chemokine (CXCL-1, CXCL-2, and CCL-2) and MMP-9 levels in mouse lung tissue.