Lefamulin Acetate

- Overview
  - 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).
    
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    Background
    
    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.
- Properties
  - CAS Number
    
    1350636-82-6
    
    Molecular Formula
    
    C30H49NO7S
    
    Molecular Weight
    
    567.78
    
    Solubility
    
    Freely soluble in ethanol. Freely soluble in water (pH 1-6.8)
    
    Storage
    
    -20°C
    
    * For research use only
- Applications
  - Application Description
    
    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.