Daptomycin

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Daptomycin is the first commercially available drug from a new class of antibiotics, the lipopeptides, marketed as Cubicin. It is a natural metabolite of Streptomyces roseosporus. The drug is bactericidal against a number of Gram-positive organisms that often are multidrug resistant, such as Staphylococcus aureus Enterococcus faecalis and E. faecium, and Streptococcus pyogenes. It has no activity against Gram-negative organisms.

Structurally, it is a 13-member amino acid peptide linked to a 10-carbon lipophilic tail, which has a novel mechanism of action: formation of transmembrane channels, which "cause leakage of intracellular ions leading to depolarizing the cellular membrane and inhibition of macromolecular synthesis." The [1]

An in vitro study showed it to have bactericidal effects, superior to vancomycin and teicoplanin, against methicillin-resistant S. aureus.[2]

References

  1. Daptomycin (Cubicin, Cubist Pharmaceuticals), Infectious Diseases Management Program, University of California at San Francisco
  2. Karen E. Bowker, Alan R. Noel and Alasdair P. MacGowan ((epub) September 16, 2009), "(Abstract) Comparative antibacterial effects of daptomycin, vancomycin and teicoplanin studied in an in vitro pharmacokinetic model of infection", Journal of Antimicrobial Chemotherapy 64 (5): 1044-1051, DOI:10.1093/jac/dkp289