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Lefamulin
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Lefamulin has antimicrobial activity against a wide range of Gram-positive bacteria. It is active against Staphylococcus aureus, with a similar susceptibility profile and minimum inhibitory concentration (MIC) distribution among -methicillin-susceptible Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus (MRSA) strains (Paukner et al., 2013b, 2013a). Lefamulin has good activity against coagulase-negative staphylococci. Both vancomycin-susceptible and vancomycin-resistant strains of Enterococcus faecium are susceptible to lefamulin. This is in contrast to Enterococcus faecalis, which exhibits only limited susceptibility to lefamulin. Beta-hemolytic and viridans group streptococci were highly susceptible to lefamulin. Lefamulin is active against strains of Streptococcus pneumoniae, and this activity is not affected by resistance to penicillin (Sader et al., 2012b).
Design, synthesis, biological evaluation and molecular docking studies of novel pleuromutilin derivatives containing nitrogen heterocycle and alkylamine groups
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Qi Wang, Jie Liu, Zi-Dan Zhou, Ke-Xin Zhou, Fei Li, Qi-Wen Zhang, Shou-Kai Wang, Wei Wang, Zhen Jin, You-Zhi Tang
Pleuromutilin (1, Figure 1) is a tricyclic diterpene natural product, which was first discovered and isolated from two basidiomycetes, Pleurotus mutilus and P. passeckerianus in 19517. Pleuromutilin exhibited antibacterial activity towards part of Gram-negative bacteria and most of Gram-positive bacteria, such as Staphylococcus aureus8. Pleuromutilin exerts antibacterial activity by binding to the V domain of the peptidyl transferase centre (PTC) of the 50S subunit of the bacterial ribosome9. Thus, pleuromutilin has aroused considerable research for this unique antibacterial mechanism. The structural optimizations of pleuromutilin on the C-14 side chain prompted the discovery of tiamulin (2, Figure 1) and valnemulin (3, Figure 1) which were authorised as veterinary medicines in 1979 and 1999, respectively10. Retapamulin (4, Figure 1) became the first pleuromutilin approved for human use by U.S Food and Drug Administration (FDA) in 200711. Lefamulin (5, Figure 1) is the first approved systemic pleuromutilin antibiotic for the treatment of community-acquired bacterial pneumonia (CABP)12.
Antimicrobial resistance of ocular microbes and the role of antimicrobial peptides
Published in Clinical and Experimental Optometry, 2021
Shyam Sunder Tummanapalli, Mark DP Willcox
Probably the newest antibiotic that has been approved by US Food and Drug Administration is called lefamulin which was approved in August 2019.139 Lefamulin is a semisynthetic pleuromutilin antibiotic indicated for community‐acquired bacterial pneumonia caused by S. pneumoniae, S. aureus (methicillin‐susceptible isolates), Haemophilus influenzae, Legionella pneumophila, Mycoplasma pneumoniae, and Chlamydophila pneumoniae.140 Lefamulin selectively inhibits the synthesis of bacterial protein.140 A recent in vitro study has shown that lefamulin was highly potent against Chlamydia trachomatis, the bacterium that causes ocular trachoma.141 However, to date, there have been no in vivo studies or reports on the use of this antibiotic to treat ocular infections in humans. Studies are needed to evaluate its efficacy and safety in human clinical trials in treating ocular trachoma and bacterial ocular infections.
Lefamulin: a promising new pleuromutilin antibiotic in the pipeline
Published in Expert Review of Anti-infective Therapy, 2019
Caroline Dillon, Anthony J. Guarascio, Jordan R. Covvey
Lefamulin is a novel pleuromutilin antibiotic candidate that could become the first in its class to be approved for treatment of a systemic bacterial infection. Lefamulin displays potent in vitro activity against various Gram-positive, Gram-negative, and atypical pathogens, although it notably lacks coverage for E. faecalis, Enterobacteriaceae, or P. aeruginosa. This relatively targeted spectrum (including coverage of S. pneumoniae, S. aureus, H. influenzae, M. catarrhalis, L. pneumophilia, C. pneumoniae, M. pneumoniae) makes it an ideal monotherapy candidate for treatment of CABP. While Phase II clinical trials have demonstrated efficacy for treatment of ABSSSIs, two Phase III studies (LEAP 1 and LEAP 2) have focused exclusively on the treatment of CABP (Table 2). Lefamulin has met all primary FDA and EMA efficacy endpoints within these Phase III trials and appears to be generally well tolerated. If lefamulin receives FDA approval, it would serve as a new and needed addition to the armamentarium for the empiric treatment of CABP.