Recent developments in glycopeptide antibacterials

The glycopeptide class of antibiotics, namely vancomycin and teicoplanin, are intravenously administered in the hospital setting for the treatment of the most severe of Gram-positive infections. Although a mainstay of the hospital formulary for over four decades, the rise of increasingly frequent high-level vancomycin resistance in enterococci and low-level resistance in staphylococci (as well as a few high-level vancomycin resistance cases) has highlighted the need for the identification of naturally occurring and semi-synthetically modified glycopeptide derivatives that have antibacterial activity against these resistant strains. Among the leading development candidates are dalbavancin, oritavancin, telavancin and ramoplanin, each of which provides a unique microbiological and pharmacological profile to fill an important unmet medical need.