1: Curr Opin Pharmacol. 2004 Oct;4(5):471-8. 

Glycopeptides in clinical development: pharmacological profile and clinical

Van Bambeke F.

Unite de Pharmacologie Cellulaire et Moleculaire, UCL 7370 Avenue Mounier 73,
1200 Brussels, Belgium. vanbambeke@facm.ucl.ac.be

Vancomycin and teicoplanin are the two glycopeptides currently used in the
clinics for the treatment of multiresistant infections by Gram-positive
organisms. The development of resistance in enterococci and staphylococci has
stimulated the search for new derivatives with improved activity, particularly
against strains resistant to conventional derivatives. Three of these, obtained
by hemi-synthesis starting from natural compounds, are now in clinical
development (oritavancin and telavancin, as derivatives of vancomycin; and
dalbavancin, as a derivative of teicoplanin). The presence of a lipophilic tail
on these molecules results in them having a prolonged half-life. It also
modifies their mode of action, conferring to them a concentration-dependent
bactericidal activity. Their spectrum of activity includes
methicillin-susceptible or methicillin-resistant staphylococci,
penicillin-resistant pneumococci and enterococci (including vancomycin-resistant
strains for oritavancin and telavancin). Ongoing clinical studies are evaluating
the efficacy and safety of these molecules for the treatment of complicated skin
and soft tissue infections and bactereamia, in a once-daily (oritavancin,
telavancin) or once-weekly (dalbavancin) scheme of administration. Despite these
remarkable properties, the use of these potent molecules should be restricted to
severe infections by multiresistant organisms to limit the risk of selection of

PMID: 15351351 [PubMed - in process]