Lefamulin Acetate is a pleuromutilin antibiotic, a group originally isolated from basidiomycetes and developed in the 1950s. Lefamulin was introduced by Nabriva Therapeutics and approved for use in US in 2019. In fact, it was the first pleuromutilin to be used for systemic treatment of bacterial infections. Chemically, it contains a tricyclic mutilin core which aids in its antimicrobial activity. Lefamulin is active against the bacteria causing CAPB (community-acquired bacterial pneumonia).
| Mechanism of Action | Lefamulin Acetate has a unique mechanism of action. It binds to the A- and P-sites of the peptidyl transferase center (PTC) in the central part of domain V of the 23S rRNA within the 50S bacterial ribosome, preventing the correct positioning of the tRNA, resulting in an inhibition of bacterial protein synthesis. |
| Molecular Formula | C30H49NO7S |
| Spectrum |
Lefamulin 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. |
| References |
Veve M and Wagner JL (2018) Lefamulin: Review of a promising novel pleuromutilin antibiotic. Pharmacother. 38(9):935-946 PMID 30019769 Chahine EB and Sucher AJ (2020) Lefamulin: The first systemic pleuromutilin antibiotic. Ann. Pharmacother.54(12):1203-1214 PMID 32493034 Yi Y et la (2017) Synthesis and biological activity evaluation of novel heterocyclic Pleuromutilin derivatives. Molecules 22(6):996 |
