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Telavancin's multifunctional mechanism of action, including inhibition of peptidoglycan synthesis and disruption of membrane potential, account for this enhanced activity as well as rapid bactericidal properties. In vitro activity has been demonstrated against a wide range of gram\u2010positive pathogens such as multidrug\u2010resistant <jats:italic>Streptococcus pneumoniae<\/jats:italic>, as well as methicillin\u2010resistant, glycopeptide\u2010intermediate, and vancomycin\u2010resistant <jats:italic>Staphylococcus aureus.<\/jats:italic> The agent also displays activity against many gram\u2010positive anaerobic organisms. Predictable linear pharmacokinetics have been demonstrated over a wide range of doses, with the most common adverse effects being taste disturbance and nausea. Clinical experience with telavancin in phase II and III studies for complicated skin and skin structure infections has shown it to have similar efficacy and tolerability compared with vancomycin and antistaphylococcal penicillins, and recently telavancin received an approvable letter from the United States Food and Drug Administration for this indication. Telavancin appears to be a promising agent for the treatment of serious infections caused by gram\u2010positive pathogens, including drug\u2010resistant pathogens. 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