1350636-82-6

Lefamulin acetate is a white to off-white solid. It is a stable compound (requiring no special storage conditions) which is highly soluble in water and 0.9% sodium chloride solution (>300mg/ml). The hydration level of lefamulin acetate at ambient conditions is typically below 1% w/w.

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

Lefamulin acetate is a single stereoisomer semi-synthetically derived from pleuromutilin, a homochiral, natural fermentation product of known absolute stereochemistry. Lefamulin acetate is a diastereomer with R-configuration at carbons of the cyclohexane moiety. The absolute configuration of the active substance has been confirmed by single-crystal structure determination.

Lefamulin acetate has activity against Gram-positive bacteria including MRSA, and atypical bacteria, especially those causing CAPB (i.e. Streptococcus pneumonia, Haemophilus influenzae, Mycoplasma pneumoniae, Legionella pneumophila, Chlamydophila pneumoniae). It also has activity against Gram-negative organisms.