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Journal of Antimicrobial Chemotherapy 2005 55(Supplement 2):ii15-ii20; doi:10.1093/jac/dki005
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JAC © The British Society for Antimicrobial Chemotherapy 2005; all rights reserved

Supplement

Origin, structure, and activity in vitro and in vivo of dalbavancin

Adriano Malabarba1 and Beth P. Goldstein2,*

1 Vicuron Pharmaceuticals, Via R. Lepetit 34-21040, Gerenzano, Varese, Italy; 2 Vicuron Pharmaceuticals, King of Prussia, PA, USA


* Corresponding author. Tel: +1-610-491-2209; Fax: +1-610-491-2229; Email: bgoldstein{at}vicuron.com

Dalbavancin is a novel semi-synthetic lipoglycopeptide that was designed to improve upon the natural glycopeptides currently available, vancomycin and teicoplanin. Chemical modification of natural glycopeptides has produced compounds with more potent antimicrobial activity and longer t1/2, while maintaining an excellent safety profile. Dalbavancin, prepared from a teicoplanin-like glycopeptide, has better activity, in vitro and in animal infection models, than vancomycin and teicoplanin. In particular, dalbavancin has excellent activity against staphylococci, including coagulase-negatives. A unique feature of dalbavancin is its pharmacokinetics, characterized by a long elimination t1/2 in humans which makes a once-weekly dosing regimen feasible. Dalbavancin recently completed Phase 3 clinical trials in skin and skin structure infection.

Keywords: glycopeptides , structure–activity relationships , Gram-positive , staphylococci


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