Lefamulin (Synonyms: BC-3781)

Lefamulin is a pleuromutilin antibiotic.¹ It is active against methicillin-resistant S. aureus (MRSA), S. pyogenes, E. faecium, H. influenzae, M. catarrhalis, L. pneumonophilia, C. pneumoniae, and M. pneumoniae (MIC₅₀s = 0.006-1 µg/ml). Lefamulin is also active against fluoroquinolone- and macrolide-resistant strains of N. gonorrhoeae (MIC₉₀s = 1 mg/L for all). In vivo, lefamulin (10-40 mg/kg) reduces the number of colony-forming units (CFUs) in a mouse model of S. pneumoniae thigh infection.² It also reduces LPS-induced production of TNF-α, IL-6, IL-1β, and GM-CSF, bronchoalveolar lavage fluid (BALF) neutrophil infiltration, and lung matrix metalloproteinase-9 (MMP-9) levels in a mouse model of LPS-induced neutrophilia.³ Formulations containing lefamulin have been used in the treatment of community-acquired bacterial pneumonia (CABP).

1.Veve, M.P., and Wagner, J.L.Lefamulin: Review of a promising novel pleuromutilin antibioticPharmacotherapy38(9)935-946(2018) 2.Wicha, W.W., Craig, W.A., and Andes, D.In vivo pharmacodynamics of lefamulin, the first systemic pleuromutilin for human use, in a neutropenic murine thigh infection modelJ. Antimicrob. Chemother.74(Suppl 3)iii5-iii10(2019) 3.Hafner, M., Paukner, S., Wicha, W.W., et al.Anti-inflammatory activity of lefamulin versus azithromycin and dexamethasone in vivo and in vitro in a lipopolysaccharide-induced lung neutrophilia mouse modelPLoS One16(9)e0237659(2022)